American Chemical Society Division of Medicinal Chemistry
New York City, NY, United States June 26-29, 2022
Session 1: Integrating Novel Chemical Modalities in Hit-to-lead: a New Paradigm for Early Drug Discovery
Translating RNA Sequence into Lead Small Molecule Medicines
Prof. Matthew DISNEY
SCRIPPS RESEARCH INSTITUTE, Jupiter, United States Read more
Prof. Matthew DISNEY
Matt Disney is a native of Baltimore and is currently Professor in the Department of Chemistry at Scripps Research on the Florida Campus. His laboratory works in the area of small molecule targeting of RNA. The lab seeks to answer fundamental questions regarding molecular recognition events between RNA folds and small molecules to study problems of biomedical importance. Indeed, they have developed a strategies to: (i) design structure-specific small molecules from the RNA’s sequence; (ii) synthesize drugs on-site in disease-affected cells to affect their function and to image them; (iii) study the biology of coding and non-coding RNAs, with a focus on incurable rare diseases and difficult-to-treat cancers; and (iv) interface RNAs with quality control machinery using small molecules and chimeras thereof to eliminate them from cells and animal models of disease. The lab’s research has garnered various awards including the Sackler Prize in the Physical Sciences, Barry Cohen Award in Medicinal Chemistry, NIH Director’s Pioneer Award, the Tetrahedron Young Investigator Award, the Eli Lily Award in Biological Chemistry, the David W. Robertson Award in Medicinal Chemistry, and others.
Structural Approach to Identify Lead Scaffolds for Protein-Protein Interaction Targets
Prof. Kyle HADDEN
UNIVERSITY OF CONNECTICUT, Storrs, United States Read more
Prof. Kyle HADDEN
Professor Hadden received his BS in Chemistry from Wofford College in 2000 and his Ph.D. in Medicinal Chemistry from the Medical University of South Carolina in 2004. During postdoctoral studies at the University of Kansas, he worked on developing small molecule Hsp90 inhibitors as anti-cancer chemotherapeutics. Professor Hadden started his independent career in the Department of Pharmaceutical Sciences in the School of Pharmacy at the University of Connecticut in 2009. The overall research focus in the Hadden lab is to utilize a medicinal chemistry/chemical biology approach to understand the mechanisms through which dysregulation of cellular signaling contributes to the onset of human cancer and apply this knowledge to develop improved therapeutics. Major ongoing projects include the development of hedgehog pathway modulators as therapeutic agents and the identification and development of small molecule inhibitors of translesion synthesis.
Integrating DNA-Encoded Library Technologies in Lead Discovery
Dr Lisa Marcaurelle is a Senior Scientific Director of Chemistry at GlaxoSmithKline in Cambridge, MA where she leads the DNA-Encoded Library Technology platform. Prior to joining GSK in 2018, Lisa worked at various Cambridge-based biotech companies including Warp Drive Bio (Sr. Director, Chemistry 2016-2018), H3 Biomedicine (VP, Discovery Chemistry, 2011-2016) and Infinity Pharmaceuticals (Lead Sr. Scientist, 2002-2007). Lisa also spent some time in academia working at the Broad Institute (Director, Chemistry, 2007-2011) where she led the creation of the Broad’s diversity-oriented synthesis (DOS) screening collection. Lisa is an active member of the American Chemical Society and was named an ACS Fellow in 2021. She has served as Chair of the Division of Organic Chemistry, Councilor for the Northeastern Section of the ACS and is a member of the ACS Women Chemists Committee. Lisa obtained a Ph.D. in Chemistry in 2001 from UC Berkeley working with Carolyn Bertozzi and did post-doctoral work at MIT with Peter Seeberger (2001-2002). She received her undergraduate degree in Chemistry from the College of the Holy Cross in Worcester, MA.
Oral Peptides: Theory and Practice
Dr Lauren MONOVICH
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States Read more
Dr Lauren MONOVICH
Lauren Monovich received a B.A. in Chemistry from Kalamazoo College before completing her doctoral studies with Professor Gary Molander on the total synthesis of 8-membered ring-containing natural products. After joining Novartis, Lauren has been privileged to lead drug discovery projects across multiple disease areas, project stages, and modalities and to produce multiple clinical compounds and a marketed therapeutic agent (Isturisa/osilodrostat for Cushing’s Disease). As a member of the Global Discovery Chemistry leadership team and Head of Lead Generation, she specializes in advancing chemical diversity within hit and lead generation projects across the Novartis portfolio, as well as in ligands for especially challenging protein surfaces. In 2018, she received the Novartis Leading Scientist and Team Awards for her work on orally exposed macrocyclic peptides and was the Novartis recipient of the 2021 YWCA Union County’s Tribute to Women and Industry (TWIN) Award. She is an active recruiter, founding member of Novartis’ Women in Chemistry Group, co-lead of the Novartis Inclusion Council, and long-standing contributor to educational and community outreach.
Discovery of IRAKIMiDs: Dual-Mechanism Degraders Targeting IRAK4 and IMiD Substrates for Oncology
Dr Lewis PENNINGTON
KYMERA THERAPEUTICS INC., Watertown, United States Read more
Dr Lewis PENNINGTON
Lewis D. Pennington is Senior Director and Head of Platform Chemistry at Kymera Therapeutics. His research interests include drug discovery and defining strategies and tactics for multiparameter optimization in drug design. He previously served a variety of roles as a synthetic and medicinal chemist at Alkermes in Waltham, Massachusetts, Amgen in Thousand Oaks, California, Array BioPharma in Longmont, Colorado, and Eli Lilly & Co. in Indianapolis, Indiana. He earned a B.S. in Chemistry (with Highest Honors in Chemistry) under the guidance of Professor Masato Koreeda at the University of Michigan in Ann Arbor, Michigan and a Ph.D. in Chemistry under the mentorship of Professor Larry Overman at the University of California in Irvine, California.
Session 2: New Directions in Targeting DNA Damage Repair (DDR)
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9/cyclin T1 for MYC-dependent Cancers
Dr David FREEMAN
KRONOS BIO, INC. , Massachussetts, United States Read more
Dr David FREEMAN
David B. Freeman is an Associate Director of Chemical Biology at Kronos Bio, Inc. where he leads Small Molecule Microarray (SMM) screening and chemical tool development efforts. Dave obtained a B.S. in Chemistry from University of California, Santa Barbara before completing his doctoral studies focused on the total synthesis of natural products with Professor John Wood at Colorado State University. He then completed post-doctoral training with Corey Stephenson at Boston University, after which, he served in the US Army, Public Health Command, where he managed a molecular diagnostics lab charged with monitoring endemic diseases in the southern US. After serving, Dave returned to his passion for oncology small molecule drug development and worked with Angela Koehler at the Koch Institute for Integrative Cancer Research at MIT. He then joined Kronos Bio, Inc. as its first employee where he spearheaded medicinal chemistry efforts leading to the discovery of KB-0742, a highly selective, orally bioavailable small molecule CDK9 inhibitor.
M3541 and M4076: Discovery and Optimization of Potent and Selective ATM Kinase Inhibitors with Strong Anti-tumor Efficacy in Combination Therapies
Dr Thomas FUCHSS
MERCK KGAA, HEALTHCARE, Darmstadt, Germany Read more
Dr Thomas FUCHSS
Thomas Fuchss is Director in Global Medicinal Chemistry at Merck KGaA, Darmstadt, Germany. Thomas received his diploma in Chemistry and doctorate with honors from Universität Konstanz, Germany. After holding various positions of increasing responsibility in Medicinal Chemistry at ALTANA as well as its Research Institute in Waltham, MA, USA, where he worked on inflammation, respiration and oncology, Thomas joined Merck, initially in the field of metabolic disorders and osteoarthritis, before becoming involved mainly in oncology. He has a track record of delivering lead compounds and clinical candidates, among them the kinase inhibitor Peposertib as well as Ataxia-Telangiectasia Mutated kinase inhibitors in clinical development. Thomas has a passion for project leadership that has led him to Program Lead level within early development. Moreover, Thomas leads the Research Pharmaceutics Processing Group, which applies state-of-the-art synthesis technologies within Discovery & Development Technologies as part of Merck Biopharma’s global research. He is the author of more than 50 publications and patent applications.
Discovery of human DNA Polymerase theta (Polθ) Inhibitors
Dr Robert HEALD
ARTIOS PHARMA LTD, Cambridge, United Kingdom Read more
Dr Robert HEALD
Rob Heald obtained a degree in chemistry and PhD with Prof. Malcolm Stevens from the University of Nottingham in the UK before completing post-doctoral studies at the University of Arizona Cancer Center with Prof. Laurence Hurley. Following his return to the UK he held various positions at Argenta Discovery (latterly Charles River) over a 13-year period working on a broad range of drug discovery projects but focussing on respiratory, inflammation and oncology. A highlight over this period was his participation in a 10-year collaboration with Genentech on projects which delivered multiple clinical candidates including the PI3kinase portfolio members GDC-0084, GDC-0032 and GDC-0077. He has now been at Artios Pharma for 3 years where he is Head of Chemistry leading teams and projects targeting the DNA damage response for the treatment of cancer.
Harnessing CDK12 Inhibition of Transcriptional Machinery to Induce Dimerization between DDB1 and CDK12-cyclinK Complex for Targeted Protein Degradation
Prof. Andrii MONASTYRSKYI
MOFFITT CANCER CENTER & RESEARCH INSTITUTE, Tampa, United States Read more
Prof. Andrii MONASTYRSKYI
Dr Monastyrskyi obtained his Ph.D. in chemistry at the University of South Florida where he worked with Prof. Roman Manetsch on the synthesis of antimalarial agents based on a 3-aryl-4(1H)-quinolone core structure. His postdoctoral studies were carried out at The Scripps Research Institute under the direction of Prof. William R. Roush. As an NIH NRSA Fellow (F32) at Scripps Research, he developed novel methodologies for the synthesis of complex organic frameworks as well as led a number of medicinal chemistry optimizations primarily focusing on structure-based drug design, structure-activity relationship (SAR), as well as PK-driven hit-to-lead studies. He was recruited to the Moffitt’s Department of Drug Discovery as an Assistant Member/Professor in 2019. Dr. Monastyrskyi also serves as a Scientific Co-Director of Cancer Pharmacokinetic and Pharmacodynamic (PK/PD) Core since 2019. His research lab (funded by an NIH, DoD and foundation grants) focuses on drugging kinases, fragment-based drug discovery, and novel strategies for targeted protein degradation.
The Modification of Pyrazolopyrimidinones and their Effect on WEE1 Inhibition and the DNA Damage Response
Prof. Phil REIGAN
UNIVERSITY OF COLORADO, Aurora, United States Read more
Prof. Phil REIGAN
Dr Reigan completed his BSc in Chemistry at the University of Manchester in 1997. He then worked as an organic chemist at Oxford Asymmetry International/Evotec. He obtained his MSc in Pharmacology in 2000 and PhD developing small molecule inhibitors of thymidine phosphorylase in 2004 with Dr Sally Freeman at the University of Manchester. From 2004 to 2007 Dr Reigan performed post-doctoral research supporting the development of indolequinones and Hsp90 inhibitors as anticancer agents in Professor David Ross’ lab at the University of Colorado. Dr Reigan then worked as a consultant advising mid-to-large client pharmaceutical companies on their drug pipelines. In 2011 Dr Reigan returned to the University of Colorado as an Assistant Professor of Medicinal Chemistry and was promoted to Associate Professor in 2018. Dr Reigan also serves as the Director of Computational Chemistry and Biology core facility that supports drug discovery and development on the Anschutz Medical Campus. Dr Reigan has published over 60 peer-reviewed publications and has 8 patents. His current research focuses on the development of small molecules targeting adaptive proteins in cancer specifically those involved in DNA damage response and metabolic reprogramming which is funded by NIH, foundation, and innovation grants.
Session 3: Hot Targets from NYC Academic and Biotech Scene
Designing and Combining Cancer's Off Switches
Dr Karen AKINSANYA
SCHRODINGER, New York City, United States Read more
Dr Karen AKINSANYA
Karen Akinsanya has served as Chief Biomedical Scientist at Schrödinger since 2018. She has more than 25 years of experience spanning academia and pharmaceutical R&D. Prior to joining Schrödinger, Karen held positions of increasing responsibility at Merck Research Labs since 2005 in clinical pharmacology, therapeutic area leadership, and business development. She also served in a number of drug discovery roles in the US and the United Kingdom with Ferring Pharmaceutical starting in 1996. Karen received her Ph.D. from the Royal Postgraduate Medical School at Imperial College in London and completed post-doctoral training at Imperial and the Ludwig Institute for Cancer Research (UCL).
Rational Design of Inhibitors of Protein-Protein Interactions
Paramjit Arora obtained his B.S. in Chemistry from UC Berkeley and his earliest research experience synthesizing fluorescent dyes for the sequencing of the human genome. He received his Ph.D. degree in Organic Chemistry from UC Irvine and pursued an American Cancer Society Postdoctoral Fellowship at Caltech before joining the faculty of NYU in 2002. He is interested in using the principles of organic chemistry to miniaturize proteins with overall goal of creating a new class of synthetic therapeutics.
Dr. Steve Colletti has led drug discovery R&D for nearly 30 years across pharma and biotech. He is currently Senior Vice President of Drug Discovery R&D at Zymergen. Prior to acquisition by Zymergen, as CSO he led the portfolio at Lodo Therapeutics in natural products drug discovery for oncology and infectious diseases. Prior to Lodo, he was Executive Director and Head of Therapeutic Modalities at Merck, with experience and leadership in small molecule, natural products, oligonucleotide, peptide, and fusion protein drug discovery – targeting cardiovascular and respiratory disease, diabetes and obesity, immunological disorders, infectious diseases, neuroscience, and oncology. Dr. Colletti built and led the RNA Therapeutics Med Chem Department, and he was a core member of multiple development teams that were responsible for discovering more than a dozen preclinical candidate molecules and advancing them toward clinical development. His responsibilities also included working closely with licensing and business development, evaluating external opportunities, and helping to manage acquisitions. Dr. Colletti is an inventor and author of over 130 patents and publications. He completed his BS degree at Loyola University Chicago, received his PhD in Chemistry from Boston University, and was an NIH Postdoctoral Research Fellow in Chemistry at the Scripps Research Institute.
Optimization of Mycobacterium Tuberculosis (Mtb) Selective Inhibitors of Lipoamide Dehydrogenase (Lpd)
Dr John GINN
TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE, New York, United States Read more
Dr John GINN
Dr Ginn received a Bachelor of Science in Chemistry from Mercer University in Macon, Georgia. Subsequently, he attended Emory University in Atlanta, Georgia where he earned a Master’s degree studying titanocene mediated reductive cyclizations under the supervision of Professor William Crowe. He then completed his doctoral studies with Professor Albert Padwa developing intramolecular Diels-Alder cyclization of amino-thio-furans for generating the tricyclic core structure common to several classes of natural products. In 2001, Dr Ginn joined the Medicinal Chemistry department of Boehringer-Ingelheim Pharmaceuticals in Ridgefield, Connecticut where he focused on projects covering inflammatory, cardiovascular, and renal diseases. In 2017, he joined the Tri-Institutional Therapeutics Discovery Institute, in New York City as a Director of Chemistry where he leads projects as part of Tri-TDI’s mission to support the identification and development of small molecule and biologic therapeutics at its three affiliated academic institutions: Memorial Sloan Kettering, The Rockefeller University and Weill Cornell Medical College.
Iyassu is VP and Head of Chemistry at Kallyope, a New York-based biotech focused on using an industry-leading platform to harness the gut-brain axis. He joined the company in 2016 as a Senior Director to lead internal and external chemistry efforts, including the development of novel strategies to enable target engagement. Iyassu joined Kallyope from a position as Director in the Medicinal Chemistry department at Merck & Co. There he led programs in the areas of obesity (developing agonists of the central receptors MC4 and BRS3), hypertension, Alzheimer’s Disease, and diabetes. Iyassu is the author of 29 papers, and during his 18 years at Merck he contributed to over 30 patent applications and helped to develop 9 clinical candidates. He also led an Early Development Team to usher a clinical candidate through Phase 1 studies. Iyassu completed his Ph.D. at Imperial College, London under the supervision of Dr. David Widdowson. He went on to do postdoctoral research with Prof. Philip Magnus at the University of Texas at Austin where he completed a total synthesis of the antitumor alkaloid pancratistatin.
Session 4: Targeting Autophagy for Cancer, Neurodegeneration, or Autoimmune Disease
Chasing Challenging Targets: Development of Selective Inhibitors of the Autophagy Pathway to Impact Cancer Therapy
Prof. Leslie ALDRICH
UNIVERISTY OF ILLINOIS AT CHICAGO, Chicago, United States Read more
Prof. Leslie ALDRICH
Dr. Leslie N. Aldrich received a BS in Chemistry with minors in Biology and Spanish in 2008 from Mercer University. In 2012, Dr. Aldrich completed her PhD studies in Chemistry at Vanderbilt University where her research primarily focused on the total synthesis of polypyrrole natural products with anticancer activity and the development of selective M1 antagonists. From 2012-2015, Dr. Aldrich performed postdoctoral research at Harvard University and the Broad Institute to develop small-molecule autophagy activators that modulate cellular disease phenotypes. In 2015, Dr. Aldrich began her independent career in the Department of Chemistry at the University of Illinois at Chicago where her lab aims to discover small molecules that modulate the autophagy pathway through novel mechanisms and to evaluate the therapeutic potential of these new strategies in cancer, neurodegenerative diseases, and rare genetic diseases. Outside of the lab, Dr. Aldrich enjoys spending time with her two corgis and running long distances.
Revolutionizing Discovery and Development of ALS Therapeutics using Transformational, AI-powered 'All-in-Human' Platforms
Dr Irene CHOI
VERGE GENOMICS, South San Francisco, United States Read more
Dr Irene CHOI
Irene is the Sr. Director of Drug Discovery at Verge Genomics in South San Francisco, CA. She has over 14 years of experience leading multiple neuroscience drug discovery programs from idea to clinic. Prior to Verge, she led early discovery, pharmacology, and program teams at Nektar Therapeutics. There, she helped bring several drugs to the clinic, including NKTR-181, a first-in-class mu-opioid analgesic, filed for an NDA. Irene completed her post-doctoral training in Catherine Rivier's lab at the Salk Institute for Biological Studies and received her Ph.D. in Biomedical Science with a focus in Neurosciences from the University of New Mexico.
Necessary Complexity: The Discovery of Selective, CNS Penetrant LRRK2 Inhibitors for the Treatment of Parkinson’s Disease
Dr Peter FULLER
MERCK & CO. INC., Boston, United States
Chemical Activation of Chaperone-Mediated Autophagy for Protection against Neurodegeneration
Prof. Evripidis GAVATHIOTIS
ALBERT EINSTEIN COLLEGE OF MEDICINE, Bronx, United States Read more
Prof. Evripidis GAVATHIOTIS
Evripidis (Evris) Gavathiotis, Ph.D. is a Professor of Biochemistry and Medicine, a Co-Leader of the Cancer Therapeutics Program and an Investigator of the Institute for Aging Research at Albert Einstein College of Medicine. His research focuses on mechanisms of protein interactions in cell death and cell survival signaling and the discovery and optimization of small molecule modulators towards novel chemical tools and therapeutics. Dr. Gavathiotis has pioneered mechanistic insights of BCL-2 family proteins and other key signaling proteins and has developed approaches that enabled the discovery of first-in-class small molecules for several challenging targets. He has been honored with several prestigious awards including the Sidney Kimmel Scholar Award for Cancer Research, the Pershing Square Sohn Prize in Cancer Research and the Young Chemical Biologist Award by the International Chemical Biology Society. He has served on numerous NIH study sections and review panels in chemical and structural biology, drug discovery and mechanisms of therapeutics. He is a member of the American Chemical Society, the American Society for Biochemistry and Molecular Biology and the American Association for Cancer Research. Dr. Gavathiotis has co-authored numerous high impact publications, more than 40 United States patent applications and he is a co-founder of three biotechnology companies (BAKX Therapeutics, Selphagy Therapeutics, Stelexis Therapeutics). He has a PhD in Biological Chemistry from the University of Nottingham and received postdoctoral training at Rockefeller University and Dana Farber Cancer Institute-Harvard Medical School.
Activating Mitophagy by targeting PTEN-Induced Kinase 1 (PINK1) for Parkinson's Disease
Dr Nicholas HERTZ
MITOKININ INC, San Francisco, United States Read more
Dr Nicholas HERTZ
Dr Hertz’s graduate research with Kevan Shokat provided the foundation for Mitokinin’s PINK1 program. Dr Hertz leads a team of 12 scientists and research associates, along with 8 FTEs at CRO partners, pushing Mitokinin’s science and therapeutics forward. He has authored over 18 publications in journals such as Cell, Neuron and Nature. Dr Hertz has been an invited speaker at international conferences including the Michael J. Fox Parkinson’s Disease Therapeutics Conference in 2018 and holds several patents.
Dr Hertz received his Ph.D in Chemistry and Chemical Biology from UCSF with a Genentech graduate fellowship in the labs of Kevan Shokat and Al Burlingame. Following his Ph.D, he completed his post-doctoral training in neuroscience as a Helen Hay Whitney fellow in the lab of Marc Tessier-Lavigne at Stanford University. He graduated magna cum laude and Phi Beta Kappa from UCLA with a B.S. in Biochemistry.
Unraveling Autophagy in Cancer Using Chemical Genetics
Prof. Jeff MACKEIGAN
MICHIGAN STATE UNIVERSITY, East Lansing, United States Read more
Prof. Jeff MACKEIGAN
Dr Jeff MacKeigan is a Professor of Cancer Biology and Complex Diseases in the College of Human Medicine at Michigan State University. Dr MacKeigan also serves as Assistant Dean for Research in the College of Human Medicine. He earned his B.A. from the University of Colorado and his Ph.D. in Microbiology and Immunology at the University of North Carolina Comprehensive Cancer Center. His postdoctoral research in the Department of Cell Biology at Harvard Medical School was immediately followed by a position as project leader at Novartis Institutes for Biomedical Research in Cambridge, Massachusetts. Dr MacKeigan joined the faculty at the Van Andel Research Institute as an Assistant Professor; he was promoted to Associate Professor; and joined Michigan State University as a Professor in 2017. His lab seeks a systems-level understanding of cancer biology and cell signaling networks that encompass autophagy, the mTOR pathway and cancer metabolism. Their research involves a variety of cutting-edge technologies, and they use their tumor biology expertise and pathway knowledge to study complex diseases. All of their research projects have one common goal – to identify novel therapeutic targets.
Session 5: Next Generation Therapies Shaped by Clinical Data
Discovery of Inavolisib, a Highly Selective Inhibitor of PI3K-α that Induces Degradation of Mutant-p110α Protein
Marie-Gabrielle is currently a Principal Scientist in the Department of Discovery Chemistry at Genentech. After receiving her PhD in Organic Chemistry at Ecole Polytechnique in France and a postdoctoral fellowship in the lab of Abigail Doyle at Princeton, she started at Genentech as a Scientist in 2013. She has been involved in a number of oncology and infectious disease projects. She’s currently the chemistry team leader of a neuroscience project in Genentech’s small molecule drug discovery group.
Discovery of LPA1 antagonists for the treatment of Pulmonary Fibrotic Diseases
Dr Peter CHENG
BRISTOL-MYERS SQUIBB R & D, Hopewell, United States Read more
Dr Peter CHENG
Peter Cheng received his B.Sc. and Ph.D. from the University of Toronto (NSERC pre-doctoral fellowship), carried out postdoctoral research at the University of Rochester (NSERC post-doctoral fellowship) and then joined Bristol-Myers Squibb, where he is currently a Director in the Fibrosis Chemistry Department. At BMS, Peter has led multiple medicinal chemistry programs in the Metabolic and Fibrosis Disease therapeutic areas encompassing diverse targets (nuclear hormone receptors, GPCRs and kinases). These efforts have resulted in the discovery of multiple advanced clinical compounds, including the PPARα/γ dual agonists muraglitazar (Pargluva; completed Phase 3 clinical trials) and peliglitazar (completed Phase 2b clinical trials) for the treatment of type 2 diabetes. Most recently, his group’s work in the Fibrosis area has resulted in the discovery of the LPA1 antagonist BMS-986278, which is currently in clinical trials.
Discovery of Risdiplam, a Medicine for the Treatment of Spinal Muscular Atrophy
Luke Green joined Roche, Basel in 2003 as a medicinal chemist after performing a PhD with Prof. S.V. Ley at the University of Cambridge (in oligosaccharide synthesis and methodology) and a postdoc with Prof. K.B. Sharpless (Enzyme and copper catalysed 1,3-dipolar cycloadditions of azides/acetylenes). At Roche he has worked in a number of disease areas from Cardiovascular and Metabolic diseases, Neuroscience & Rare diseases now with a recent focus in oncology, in particular small molecule cancer immunotherapy.
Discovery of PF-07081532: a Small Molecule GLP-1 Receptor Agonist Suitable for Once-daily Oral Administration
David received his undergraduate degree from Harvey Mudd College and his PhD in Chemistry from Yale University in the laboratory of Professor Sam Danishefsky. Following postdoctoral studies at the University of California, Berkeley, with Professor Clayton Heathcock, he joined Pfizer in 1995. There he has led Medicinal Chemistry efforts and broader Project Teams against targets for Obesity, Osteoporosis, and Diabetes resulting in multiple candidates advanced for clinical testing including the Ph3 CB-1 antagonist Otenabant and the Ph2 GLP-1R agonist Danuglipron. He is an author on more than 46 publications and is an inventor on 40 patents.
Discovery of LY3154885, a Second Generation Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Drug-Drug Interaction Risk Profile
Dr Erik HEMBRE
ELI LILLY & CO., Indianapolis, United States Read more
Dr Erik HEMBRE
Erik graduated from St. Olaf College, Northfield, MN, in 1990 with a bachelor’s degree in chemistry and obtained his PhD in Organic Chemistry and the University of Michigan in the research group of Prof. Will Pearson, working on the total synthesis of poly-hydroxylated alkaloid natural products. In 1996, he joined the labs of Barry Trost at Stanford University as a NIH Post-doctoral fellow where he applied palladium catalyzed asymmetric allylic alkylation chemistry to the synthesis of natural products. In 1999, Erik moved to Indianapolis, Indiana to join Eli Lilly and Company as a Sr. Organic Chemist. Over the past 23 years, Erik has contributed to Lilly’s drug discovery efforts in the areas of neuropsychiatric disorders, obesity, diabetes, pain, and neurodegeneration. He has contributed to the discovery of 9 molecules that have advanced into human clinical development and is recognized as an expert in GPCR-targeted drug discovery. He is currently an Associate Vice President in Lilly’s Discovery Chemistry Research and Technologies group.
The Invention of MK-8262, a CETP Inhibitor for the Treatment of Coronary Heart Disease
Dr Petr VACHAL
MERCK & CO. INC (MSD), Kenilworth, United States Read more
Dr Petr VACHAL
Petr Vachal is an accomplished drug hunter and an executive manager with a track record of success, building successful teams and providing scientific leadership, working across therapeutically important areas, diverse modalities and enabling technologies, spanning from target & lead discovery to clinical candidate nomination and early clinical development. Petr is currently AVP Chemistry, Head of the NJ Discovery, Global Head of External Discovery Chemistry, Sample Management and Operations at Merck & Co (MSD). Petr is responsible for global drug discovery pipeline across all disease areas (cardiovascular, oncology, immuno-oncology, neuroscience, infectious diseases), capabilities (medicinal chemistry, HT-E, automation, engineering), and modalities (small molecules, peptides, oligos, degraders); accountable for hit-to-lead-to-clinical candidate deliverables. Prior responsibilities included creation and leadership of Screening, Target & Compound Profiling (STCP), an organization globally responsible for portfolio of screening platforms, chemical biology, biophysics, protein biochemistry, external sourcing partnerships, compound management and operations, as well as inception and leadership of Automation & Capabilities Enhancement (ACE), an organization dramatically accelerating discovery chemistry pipeline through development and application of enabling capabilities (first to develop the concept of high-throughput experimentation, late-stage functionalization, and micro purification). Under Petr’s leadership, the success rate for finding viable leads for all prioritized targets in the portfolio has increased dramatically (>95% success rate), several new targets have been identified from a portfolio of disease-relevant phenotypes, and >20 candidates were delivered into the clinic (>10 of these candidates are currently progressing through Ph1-2 clinical trials). Petr received Ph.D. from Harvard University (graduate advisor Eric N. Jacobsen).
Session 6: Lessons from Drug Hunters across Academia, NPOs and the Pharmaceutical Industry
Discovery of Nix-TB as a Novel Regimen that Significantly Shortens Treatment of Tuberculosis
Dr Christopher B. COOPER
TB ALLIANCE, GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT, New York, United States Read more
Dr Christopher B. COOPER
Christopher B. (Chris) Cooper joined the TB Alliance in January 2009, as Director of Chemistry. Chris received his BS (magna cum laude) in Chemistry from Clemson University in 1980, and his MS in Organic Chemistry at Stanford University with Professor Carl Djerassi in 1982. Following a two-year industry sabbatical at CIBA-Geigy Pharmaceuticals, he returned to Stanford in 1984 to earn his Ph.D. in Organic Chemistry with Professor Paul A. Wender. From 1988 through 1998, Dr. Cooper was engaged in medicinal chemistry research at Pfizer, Inc., in both their Groton, Connecticut, and Sandwich, England, laboratories. His areas of investigation included veterinary and human drug discovery programs (infectious disease, inflammation, immunology, oncology, and neuroscience), as well as applications of automated synthesis technologies for both lead generation and lead optimization purposes.
Dr Cooper joined Bristol-Myers Squibb, Inc., in Princeton, New Jersey, in 1998 to launch the Lead Synthesis Group directing the design, development, and synthesis of novel, drug-like medicinal chemistry arrays. His research team at BMS was directly responsible for the rapid pharmacological assessment of exploratory biological targets of interest, and the advancement of early- and full-phase discovery programs through hit-to-lead, lead optimization, and pre-development candidate selection medicinal chemistry approaches.
As Senior Director of Chemistry at the TB Alliance, Chris is responsible for all lead identification, lead optimization, preclinical, and clinical candidate chemistry efforts including medicinal chemistry, process chemistry, and cGMP drug substance manufacturing activities across the Alliance’s research and development portfolio. He currently oversees ~60 medicinal chemistry, analytical chemistry, process chemistry, and GMP manufacture FTE’s at 15 combined universities, biopharma, contract research organizations (CRO’s), and contract manufacturing organizations (CMO’s) for the advancement of ~25 discovery/preclinical/clinical programs. Dr. Cooper is the author of over 70 publications and is the inventor on twenty approved US and international (WO) patents.
Discovery of Upadacitinib: a Tricyclic Janus Kinase 1 (JAK1) Inhibitor
Kristine Frank received a B.S. in pharmacy from The Ohio State University (1993) and a PhD in medicinal chemistry from the University of Kansas (1998) working with Professors Lester A. Mitscher and Jeffrey Aubé. She began her industrial career at Pharmacia & Upjohn (Kalamazoo, MI) working on GPCRs for CNS indications. In 2003, Kristine moved to Abbott Bioresearch Center (Worcester, MA) to work predominantly on kinases in immunology. During this time, she was a co-inventor of Rinvoq® (upadacitinib), a Jak1 inhibitor. Kristine then transferred to the hit-to-lead group in Abbott (Abbott Park, IL) to pursue her passion for working in the early discovery space. Now in AbbVie’s centralized medicinal chemistry group, she balances her efforts on early and late stage projects with as much lab work and mentoring as time allows.
Anticancer Drug Discovery from Pets to People, the Story of PAC-1
Prof. Paul J. HERGENROTHER
UNIVERSITY OF ILLINOIS, Urbana, United States Read more
Prof. Paul J. HERGENROTHER
Paul J. Hergenrother was born in 1972 and raised in Akron, Ohio. He attended the University of Notre Dame, where he received his B.S. in Chemistry in 1994. From there Paul moved to the University of Texas at Austin, to conduct graduate research under the direction of Professor Stephen F. Martin. While in the Martin laboratory Paul elucidated the catalytic mechanism of phospholipase C, and completed the total synthesis of erythromycin B. He graduated with his PhD in Chemistry in 1999, and moved on as an American Cancer Society postdoctoral fellow to Harvard University, where he worked in the laboratory of Professor Stuart L. Schreiber in the Department of Chemistry and Chemical Biology. While at Harvard Paul was involved in the development of small molecule microarrays as a platform for high-throughput compound screening.
He established his own laboratory in the Department of Chemistry (and as an affiliate in the Department of Biochemistry) at the University of Illinois at Urbana-Champaign in 2001. He was promoted to associate professor with tenure in 2006, to full professor in 2010, and in 2013 was named the Kenneth L. Rinehart Endowed Chair in Natural Products Chemistry. Professor Hergenrother is the co-founder and Chief Scientific Officer of Vanquish Oncology, and through Vanquish an anticancer compound discovered by the Hergenrother lab (the procaspase-3 activator PAC-1) completed a Phase 1 clinical trial and in February 2021 began a Phase 1b/2 trial in patients with metastatic uveal melanoma. The Hergenrother lab also discovered the NQO1 substrate and anticancer compound IB-DNQ, which is scheduled for a Phase 1 clinical trial in late 2021. The Hergenrother lab, in collaboration with the laboratory of Prof David Shapiro (UIUC Biochemistry), also discovered the anticancer compound ErSO, with potent activity against ER+ breast tumors; ErSO was licensed to Systems Oncology who subsequently licensed it to Bayer in a ~$370M deal plus downstream royalties.
In spring of 2020, while UIUC was shut down due to the COVID-19 pandemic, Prof. Hergenrother led the team that developed a novel saliva-based assay for SARS-CoV-2, a simple protocol that bypasses the need for RNA isolation and as such is inexpensive, returns rapid results, and can be used on scale. The University of Illinois administered over 1,000,000 of these tests on its campus during Fall 2020, typically testing ~10,000 people a day, and this testing has been key to controlling the pandemic at the University of Illinois and enabling in-person classes and research, keeping positivity rates low. With Emergency Use Authorization (EUA) status, over 120 colleges, universities, schools, and businesses are now using this test. The ability of this saliva test to identify individuals in the early stage of infection is credited with preventing the spread of COVID-19 in many settings, including the UIUC athletic department and Illinois state legislature.
Professor Hergenrother has been the recipient of an NSF-CAREER Award, a Research Corporation Research Innovation Award, a Beckman Young Investigator Award, an Alfred P. Sloan Foundation Fellowship, the GlaxoSmithKline Chemistry Scholar Award, the ACS David Robertson Award for Excellence in Medicinal Chemistry, the Camille Dreyfus Teacher-Scholar Award, the ACS Eli Lilly Award in Biological Chemistry, was named as an American Cancer Society Research Scholar, was named by Technology Review magazine as one of the top innovators under the age of 35, and was the recipient of the 2016 Innovation Transfer Award from the University of Illinois. More recently he was named as the recipient of the 2016 UCB-Ehrlich Award for Excellence in Medicinal Chemistry, of the 2016 Akron Section Award from the ACS, a 2017 ACS Arthur C. Cope Scholar Award, and the 2018 ACS Sosnovsky Award for Cancer Research. Most recently he was named as a Fellow of the National Academy of Inventors.
At the University of Illinois Professor Hergenrother is the Leader of the IGB Theme “Anticancer Discovery from Pets to People”, and is the Director of the NIH Chemistry-Biology Interface Training Grant, and is Deputy Director of the Cancer Center at Illinois. Professor Hergenrother has served or serves on the editorial board/editorial advisory board for multiple journals, including ACS Central Science, Current Opinion in Chemical Biology, Journal of Medicinal Chemistry, Organic Reactions, and ChemBioChem. The Hergenrother laboratory seeks to use small molecules to identify and validate novel targets for the treatment of intractable diseases, including cancer and multi-drug resistant bacteria.
From Concept to Clinic: the Story of M1 and mGlu4 Positive Allosteric Modulators (PAMs)
Prof. Craig LINDSLEY
VANDERBILT UNIVERSITY, Nashville, United States Read more
Prof. Craig LINDSLEY
Craig W. Lindsley, Ph.D. is the Director of the Warren Center for Neuroscience Drug Discovery (WCNDD), University Professor of Pharmacology, Chemistry & Biochemistry, holds the William K. Warren Jr. Chair in Medicine and Editor-in-Chief of the Journal of Medicinal Chemistry. Together with Jeff Conn, Craig has pioneered the concept of GPCR allosteric modulation, developing key proof of concept compounds and clinical candidates. Craig holds over 110 issued US patents and has published over 550 manuscripts and another 225 published patent applications. Of the publications, there are numerous which detail the first-in-class tools and POC for M1 PAMs, mGlu5 PAMs, mGlu4 PAMs, M5 NAMs, M4 antagonists, PLD, multiple ion channels and transporters, as well as the first allosteric Akt kinase inhibitors. As co-founder and Director of the WCNDD, Craig has raised over $390 million in licensing and research support from NIH, Foundations and companies. In 2016, and without an industry partner, Craig oversaw IND-enabling studies of a novel M1 PAM that was awarded an open IND, and the Phase I trial (SAD) was completed at Vanderbilt prior to licensing to Acadia. In 2018, he was a founder of Appello Pharmaceuticals, and in 2021, saw his mGlu4 PAM entered Phase I clinical trials. Beyond this, Craig is the founding Editor-in-Chief of ACS Chemical Neuroscience (2009-2020), interim Editor-in-Chief of ACS Pharmacology & Translational Scinence (2020-2021) and current Editor-in-Chief of Journal of Medicinal Chemistry. He has been the recipient of major awards from ACS and ASPET, including induction into the ACS MEDI Hall of Fame, and named a Fellow of the Royal Society for Chemistry, the National Academy of Inventors and the American Association for the Advancement of Science.
Drug Discovery: Where are We Headed?
Dr Wendy YOUNG
MPM CAPITAL, Brisbane, CA, United States Read more
Dr Wendy YOUNG
Wendy Young is a biotechnology, pharma, and life sciences executive and board advisor with more than 25 years of experience in the discovery and development of innovative new medicines for patients. Wendy has held key senior roles at Genentech, Celera Genomics, and Johnson & Johnson Company.
Prior to joining MPM, Wendy was the Senior Vice President at Genentech where she actively built and led the small molecule drug discovery organization. Under her leadership, more than 25 clinical candidates, in the areas of oncology, immunology, neurology, and anti-infectives, progressed into development. Additionally, Wendy led the BTK discovery program and is co-inventor of fenebrutinib which is currently in Phase 3 trials for multiple sclerosis. Prior to joining Genentech, Wendy held roles of increasing scientific leadership at Celera Genomics and Scios, a J&J company. Wendy is an inventor and/or author on more than 70 published patents and manuscripts.
Known for her strong passion and contributions within the scientific community, Wendy has been involved with the American Chemical Society (ACS) for 20 years. In 2017, she was elected as the ACS National Chair of the Medicinal Chemistry Division (MEDI), and she currently serves as an associate editor of The Journal of Medicinal Chemistry. In 2018, Wendy was inducted as an ACS Fellow for her lifelong service to chemistry, society and medicine, and in 2019 highlighted as “One of the Top 20 Women in Biopharma” by Endpoint News. In 2020 she was awarded the prestigious Earle B. Barnes Award for Leadership in Chemical Research Management.
Wendy earned her Ph.D. from Princeton University, having studied in the laboratories of Edward C. Taylor. At Princeton, and in collaboration with Eli Lilly, Wendy worked on folate analogs as antitumor agents and Alimta® was an outcome of this collaboration. Thereafter, as an American Cancer Society Fellow, she performed post-doctoral studies in the laboratories of Samuel Danishefsky at Sloan-Kettering Cancer Center and was part of the team that completed the total synthesis of Taxol®.
2022 Division of Medicinal Chemistry Award Lecture
A Perspective on the Arc of Innovation in Drug Discovery over Three Decades
Dr Lawrence G. HAMANN
STEALTH NEWCO, San Francisco, United States Read more
Dr Lawrence G. HAMANN
Larry Hamann is currently Co-Founder, President and CEO of a new venture-backed stealth mode biotech company. Previously, Larry was Global Head, Drug Discovery Sciences at Takeda Pharmaceuticals, with responsibility for Medicinal & Computational Chemistry, Computational Biology, Omics platforms, Biochemistry and Biophysics, Structural & Chemical Biology and Compound Management/Screening. Prior to Takeda, he served as Corporate Vice President and Global Head of Small Molecule Drug Discovery at Celgene, where his teams built a state-of-the-art platform for both molecular glue and heterobifunctional protein degradation therapeutic discovery and development, with several molecules in clinical development. In over 30 years of drug discovery he has led or overseen teams responsible for more than 18 clinical stage compounds, including the FDA approved DPP4 inhibitor saxagliptin (Onglyza™) for type II diabetes, and the FDA approved first-in-class HCV NS5A inhibitor daclatasvir (Daklinza™) for hepatitis C. Prior to Celgene, Larry was Executive Director, Global Discovery Chemistry at Novartis, where among the molecules from these efforts is branaplam – an investigational drug for treatment of Huntington's Disease. Previously, Larry was at Bristol-Myers Squibb, where he led drug discovery teams in metabolic and musculoskeletal disease, and virology, after beginning his career at Ligand Pharmaceuticals, focusing on nuclear receptor-based therapeutics. Larry is co-inventor on > 70 patents, co-author on > 90 scientific publications, and serves as a standing member of the NIH Study Section for Synthetic and Biological Chemistry. In August of 2017, Larry was awarded the American Chemical Society’s Heroes of Chemistry Award for contributions to the discovery of the combination of the pioneering hepatitis C virus (HCV) NS5A inhibitor, Daklinza® (daclatasvir), and the HCV NS3 protease inhibitor, Sunvepra™ (asunaprevir), which together demonstrated for the first time that HCV infection could be cured with only orally administered direct-acting antiviral agents. Larry holds a BS in Chemistry from the University of Detroit and a PhD in Organic Chemistry from the University of Michigan.
2022 IUPAC-Richter Prize Lecture
Drug Discovery in Academia: Succesful Case Studies
Prof. Michael E. JUNG
UCLA CHEMISTRY & BIOCHEMISTRY, Los Angeles, United States Read more
Prof. Michael E. JUNG
Michael Jung received his BA in 1969 from Rice University and his PhD in 1973 from Columbia University, where he worked with Gilbert Stork as an NSF Fellow. After a NATO postdoctoral fellowship with Albert Eschenmoser at the ETH in Zurich, he joined the faculty at UCLA in 1974, where he is now a Distinguished Professor of Chemistry and the UC Presidential Chair in Medicinal Chemistry. He is an authority on synthetic medicinal chemistry and has more than 325 patents and/or applications arising from both his consulting activities and his own research. He has more than 12 ongoing collaborations with biologists at UCLA and elsewhere. Two compounds from his lab have been approved: 1) Xtandi, approved 8/31/12 for the treatment of castration-resistant prostate cancer (CRPC), and 2) Erleada, approved 2/14/18 for the treatment of non-metastatic CRPC. He has published over 370 articles and given over 650 lectures on his research.