Announcing the 2024 ACS Division of Medicinal Chemistry Award Recipients: Celebrating Excellence in Medicinal Chemistry

Abstract

We want to highlight and celebrate the outstanding achievements of the recipients of the 2024 ACS Division of Medicinal Chemistry awards and fellowships (Figure 1). These individuals have demonstrated innovation, dedication, and scientific prowess across a wide range of therapeutic areas, from antimicrobial resistance and cancer to Alzheimer’s disease and male contraception. Their contributions span novel drug discovery strategies, groundbreaking chemical biology, and the development of pioneering therapeutic compounds. As we honor the winners of these awards, we recognize the vital role that they have played in advancing medicinal chemistry and shaping the future of drug discovery. Figure 1. From left to right: Kevan Shokat, Maria-Jesus Blanco, Christa Müller, Wendy Young, Michael Jung, Michael Bollong, Stuart Conway, Jarvis Hill, Alicia Wagner, Erin DiMauro, Emma Kelley, Rui Shi, Laura Hirsch, Jed Kim, Louise Dow, Taimeng Liang. The 2024 MEDI Hall of Fame welcomed five outstanding scientists whose pioneering contributions have significantly advanced the field of medicinal chemistry. Together, they have pushed the boundaries of medicinal chemistry, paving the way for novel treatments addressing some of the most pressing medical challenges of our time. The prestigious awardees are: Prof. Kevan Shokat from the University of California, San Francisco, was recognized with the Edward E. Smissman Award, sponsored by the Maryanoff Endowment, which coincided with his induction. Prof. Shokat has dedicated his career to tackling one of the most challenging oncogenic proteins in cancer biology, K-Ras. Long deemed “undruggable” since its discovery in 1982, K-Ras resisted therapeutic intervention until Prof. Shokat and his team uncovered a novel binding pocket in the G12C mutant form of the protein. This pivotal discovery paved the way for the development of the first-ever drug targeting K-Ras, Sotorasib, now used clinically to treat G12C-positive nonsmall cell lung cancer. Dr. Maria-Jesus Blanco is the Chief Scientific Officer at Atavistic Bio and received the Division of Medicinal Chemistry Award, sponsored by the Thomas J. Perun Endowment Fund, which coincided with her induction into the Hall of Fame. With over 25 years of experience in drug discovery across both large pharmaceutical companies and biotech, Dr. Blanco has been driven by her passion for developing innovative medicines that address unmet medical needs. She has a track record of delivering 14 compounds to clinical studies, including two approved drugs. Dr. Blanco noted that she is “deeply grateful to the many talented colleagues she has had the privilege to work with in advancing promising compounds towards the clinic.” She is passionate about mentoring younger medicinal chemists and increasing the visibility of women in the field. She hopes her journey will inspire the next generation of scientists to continue advancing life-changing therapies for patients and their families. Prof. Christa Müller from the University of Bonn was the winner of the inaugural Gertrude Elion Medicinal Chemistry Award. Prof. Müller was deeply inspired by Gertrude Elion, one of the few women to receive the Nobel Prize in Physiology or Medicine. Dr. Elion’s work on intracellular purine metabolism motivated Prof. Müller to focus her research on extracellular purines and their targets, aiming to develop innovative drugs. Prof. Müller has opened new scientific fields, including ectonucleotidase inhibitor development, selective P2X and P2Y receptor ligands, including P2X4 antagonists for neuropathic pain treatment, tool compounds and drugs for orphan G protein-coupled receptors, and innovative prodrug concepts. Prof. Müller notes that being “the inaugural Gertrude Elion Award motivates me to go one step further and to aim high – towards the development of innovative drugs to cure patients.” Dr. Wendy Young is widely recognized for her >30 years of exceptional contributions to medicinal chemistry, leadership, and dedication to advancing women in STEM. During her tenure at Genentech, which was, at that time, focused on antibody R&D, she built and led the small molecule discovery organization, overseeing teams that advanced more than 30 drug candidates into clinical development, including Fenebrutinib, currently in Phase 3 trials for multiple sclerosis. Under her leadership, Genentech scientists discovered over 20 clinical candidates, including Divarasib (KRAS G12C), Inavolisib (mPI3K), and Giredestrant (SERD), all with best-in-class potential for treating various oncology indications. Dr. Young has a noted history of service to the medicinal chemistry community having served as the Division Chair in 2017. Prof. Michael Jung, of the University of California, Los Angeles, is a leader in organic synthesis and methodology development with over 50 years of groundbreaking contributions to the field. His lab first synthesized the androgen receptor antagonists Enzalutamide and Apalutamide, which were approved for the treatment of prostate cancer. Beyond his academic achievements, Prof. Jung has founded or cofounded 13 biotech companies and has four more drugs in clinical trials for glioblastoma, solid tumors, and autoimmune diseases. His extensive consulting work with over 70 pharmaceutical and biotech companies has further amplified his impact on medicinal chemistry. Dr. Michael Bollong, of The Scripps Research Institute, is the recipient of the David W. Robertson Award for Excellence in Medicinal Chemistry, recognized for his ability to combine the classical aspects of small molecule drug development with a deep understanding of cell biology and physiology. Dr. Bollong’s laboratory has become a leader in exploring new regenerative mechanisms, particularly in targeting the Hippo-YAP pathway─one of the few known regenerative transcriptional programs in mammals. His work has uncovered multiple pharmacological mechanisms for targeting this pathway, advancing drug discovery efforts in regenerative medicine. His group has made progress in understanding how endogenous stem cells can be harnessed to promote tissue repair, with notable success in demonstrating in vivo lung repair in mouse models of fibrosis using molecules discovered in his lab. In six years, Dr. Bollong developed a clinical candidate for treating pulmonary fibrosis, with a clinical trial that began in April 2024, and several other drug candidates nearing the IND-enabling stage, showcasing the immense potential of his research. Dr. Bollong notes that it is “[his] hope that receiving this award, brings greater attention to the need in academia and industry alike to focus on the generation of new regenerative medicines for treating age-related disease, an area in which we, as medicinal chemists, have a key role in advancing.” Prof. Stuart Conway, Michael and Alice Jung Endowed Chair of Medicinal Chemistry and Drug Discovery at UCLA, is the recipient of the Robert M. Scarborough Award. He leads an innovative program in chemical biology and medicinal chemistry with a focus on targeting epigenetics and harnessing biological redox processes. Prof. Conway has made pioneering contributions to the field, publishing some of the first inhibitors of the BET family of bromodomain-containing proteins, including OXFBD04, which laid the groundwork for Gilead’s BET bromodomain inhibitor, Alobresib, currently in clinical trials. Prof. Conway’s group was also the first to publish high-affinity ligands for the bromodomains of CREBBP and P300, a key discovery that has underpinned the development of Inobrodib by CellCentric, now in Phase 2 trials for multiple myeloma and acute myeloid leukemia. His research extends beyond oncology, with ongoing work in the neglected tropical disease space targeting bromodomain inhibitors for schistosomiasis, Chagas disease, and Leishmaniasis. In addition, Prof. Conway has significantly advanced the study and targeting of cellular redox, particularly hypoxia, contributing to the development of hypoxia-activated pro-drugs (HAPs) and novel tools for imaging tumor heterogeneity. His work continues to inform drug discovery across multiple therapeutic areas. Jarvis Hill was a fifth-year graduate student in Dr. David Crich’s laboratory at University of Georgia when he was awarded the Scarborough Award for Graduate Students and Postdoctoral Researchers. His work focused on developing synthetic methods to access trisubstituted hydroxylamines, a key bioisostere. After tackling a challenge that had stumped others for nearly a decade, Jarvis successfully pioneered a method involving the reaction of metalated secondary amines with peroxide derivatives, leading to a high yield of the desired compounds. Building on this success, Jarvis overcame further synthetic hurdles by developing a new route to create sterically hindered trisubstituted hydroxylamines. Jarvis’ work demonstrated the utility of the trisubstituted hydroxylamine moiety, including its ability to enhance blood–brain barrier penetration and its success in vivo, targeting mutation-activated EGFR and leukemias. His research has resulted in multiple patent applications and demonstrated the value of trisubstituted hydroxylamines in drug discovery. Alicia Wagner was a fifth-year graduate student in Dr. Roman Manetsch’s lab at Northeastern University when awarded the Scarborough Award for Graduate Students and Postdoctoral Researchers. Her work explored the development of chemical tool compounds to study the Plasmodium falciparum formate nitrite transporter (PfFNT), a key membrane protein responsible for effluxing lactic acid in malaria parasites. Alicia developed a research program to explore the hypothesis that PfFNT’s transporter function is coupled with conformational changes and set out to unravel its mechanism by combining biochemical, synthetic, and computational chemistry approaches. In her structure–activity relationship study, Alicia designed and synthesized over 220 compounds, leading to the discovery of low nanomolar inhibitors, some of which are now being advanced to in vivo POC studies. Her work represents the opportunity to advance a novel compound series for antimalarial drug discovery. Dr. Erin DiMauro, Executive Director of Discovery Chemistry at Merck & Co., was recognized with the Robert M. Scarborough Award for Excellence in Medicinal Chemistry. Dr. DiMauro leads a dynamic team of ∼80 chemists supporting a broad portfolio of programs, spanning target validation to early clinical development across three therapeutic areas (Oncology, Immunology, Neuroscience) and multiple modalities. Her teams have advanced numerous high-quality clinical candidates, and she has directly overseen the early clinical development of multiple assets for different disease indications. During her early career at Amgen, Dr. DiMauro was instrumental in leading challenging programs in Neuroscience and Oncology, including her pivotal role as an originator of the Nav1.7 inhibitor program for chronic pain. This decade-long effort yielded several clinical-quality leads. Dr. DiMauro is also recognized as an active supporter of her team members, who prioritizes and fosters their development. She champions a collaborative vision for the field, believing “scientific progress achieved by teams and organizations will not only lead to the development of impactful drugs and strategies but also inspire and empower future leaders in the field of medicinal chemistry.” Congratulations to Emma Kelley of Loyola University Chicago and Rui Shi of the University of Minnesota for being awarded ACS MEDI travel grants to attend the 2024 Fall ACS Meeting. This recognition is a testament to their research and dedication to the field of medicinal chemistry. They readily engaged with the programming at ACS and made valuable contributions to the medicinal chemistry community. Laura Hirsch was a fourth-year PhD student at the University of Minnesota program when awarded a MEDI Predoctoral Fellowship sponsored by Genentech. Under the mentorship of Prof. Daniel Harki, Laura is working on the development of heterobifunctional degrading compounds specifically targeting the N-Myc transcription factor. Her project focuses on creating next-generation Aurora-A/N-Myc degraders, using different linkers to optimize potency and reduce off-target toxicity, following issues observed with first-generation inhibitors. Additionally, Laura is exploring a novel approach to address toxicity concerns by developing nuclear-specific Aurora-A/N-Myc degraders that spare the cytosolic version of Aurora-A, necessary for cell cycle progression. Outside of her research, Laura is a passionate advocate for women in science, contributing significantly to outreach and advocacy efforts. Reflecting on her recognition, Laura expressed, ″I feel extremely honored to be awarded the ACS MEDI predoctoral fellowship. I am immensely thankful for the opportunity to attend the Medicinal Chemistry Gordon Research Conference and present my work at the ACS national meeting.” Jed Kim, a fourth-year PhD student at the University of Wisconsin under the mentorship of Prof. Jennifer Schomaker, was awarded a MEDI Predoctoral Fellowship. Jed’s research focuses on the development of novel inhibitors targeting KasA, a high-priority target for tuberculosis (TB) drug development that remains underexplored. His approach involves exploiting silver-catalyzed nitrene transfer reactions to transform C–H bonds into C–N bonds, generating a unique library of cyclic sulfamate analogs. These analogs display significant activity against Mycobacterium tuberculosis through an unusual mechanism of action, offering a promising new chemotype for TB treatment. Jed’s work aims to elucidate structure–activity relationships and optimize hit-to-lead compounds, providing a foundation for the development of novel KasA inhibitors to combat TB. Louise Dow, a fourth-year PhD student at the University of Nebraska Medical Center under the guidance of Prof. Paul Trippier, was awarded a MEDI Predoctoral Fellowship for her research targeting Alzheimer’s disease. Louise’s project focuses on the identification of small molecules capable of modulating hydroxysteroid 17-β dehydrogenase 10 (17β-HSD10), a mitochondrial enzyme linked to amyloid beta toxicity, tau phosphorylation and neuroinflammation. Her work has led to the identification of an inhibitor of 17β-HSD10 that has demonstrated its potential for rescuing amyloid beta-induced cytotoxicity in neuron-like cells. Louise expressed her gratitude, stating, “this award has provided invaluable opportunities for academic and professional growth, allowing me to present my research and receive critical feedback from experts in the field.″ Taimeng Liang, a fourth-year PhD student at the University of Minnesota working under the guidance of Prof. Gunda Georg, has been awarded a MEDI Predoctoral Fellowship for her groundbreaking research on developing BRDT-1 selective inhibitors for male contraception. Taimeng’s work focuses on creating a first-in-class inhibitor of the BRDT bromodomain (BD1), an important target for male contraception. She has synthesized a challenging fluorescent probe for the FP bromodomain assay and re-established this assay in her lab. Despite the challenge of developing selective inhibitors for the highly similar bromodomains of the BET family, Taimeng has made significant progress in generating a first-generation inhibitor scaffold with >10-fold selectivity toward BRDT. Her work, which combines structure-based drug design, advanced synthetic chemistry, and biophysical assays, is poised to make a major impact on the field. Congratulations to all of the 2024 MEDI awardees! These awards highlight impressive scientific contributions and serve as a testament to the exciting future of our field. We are always looking to recognize outstanding scientists in medicinal chemistry, so please consider nominating colleagues, and mentees so that we can celebrate their achievements (see Table 1 for important award deadlines). This article has not yet been cited by other publications.