April 20-21, 2023
Join Us: The Wertheim UF Scripps Institute Chemical Biology & 5th UF Drug Discovery Symposium
The 2023 symposium will be held at The Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology in Jupiter, Florida on April 20 & 21, 2023
RECAP THE EVENT
Symposium brings together two powerhouses in drug discovery
More than 180 scientists attended The Wertheim UF Scripps Institute Chemical Biology & 5th UF Drug Discovery Symposium, April 20-21, 2023, in Jupiter, Florida.
A Message from the Hosts
Professor of Chemistry
Thomas Kodadek, Ph.D.
Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology | Jupiter, FL
Professor and Chair, Department of Medicinal Chemistry
Hendrik Luesch, Ph.D.
UF College of Pharmacy Center for Natural Products, Drug Discovery and Development (CNPD3) | Gainesville, FL
It is our great pleasure to welcome you all to the UF Scripps Chemical Biology & 5th UF Drug Discovery Symposium (UFDDS). The Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology in Jupiter and the Center for Natural Products, Drug Discovery and Development (CNPD3) in Gainesville are joining forces this year to host the event.
The UF Drug Discovery Symposium was established in 2016 and the past four events, held in Gainesville, brought together roughly 200 participants from all Florida research institutions. This year the symposium is designed to celebrate the integration of the Jupiter campus as a new research arm of UF Health by showcasing the combined UF drug discovery expertise at the UF Scripps and the main campus.
The UF-centric 2023 symposium will feature speakers from both UF campuses and keynote speakers who are global leaders in chemical biology and drug discovery from academia and pharma.
The symposium will cover a range of topics on the use of both natural and synthetic small molecules to monitor and manipulate the proteome. The sessions will cover topics on Control of Protein Homeostasis and Degrader Development, Natural Products, Chemical Proteomics, Drug Development, and Integral Membrane Proteins. We warmly welcome our four keynote speakers: Nathanael Gray (Stanford), Dan Nomura (University of California at Berkeley), Ingrid Wertz (Lyterian), and William Fenical (Scripps Institution of Oceanography, University of California at San Diego) who are outstanding leaders in these fields. In addition, many of our own faculty from the UF Scripps and Gainesville campuses will demonstrate that together we are an even greater powerhouse in drug discovery. The program will include a poster session and an award ceremony recognizing the best poster presenters among our graduate students and postdoctoral researchers.
We hope you all enjoy the joint event this year and use the opportunity to connect with friends and colleagues from both campuses and across Florida. Go Gators!
Thomas Kodadek, Ph.D. & Hendrik Luesch, Ph.D.
Schedule of Events
April 20, 2023
|9:00-9:15 a.m.||Welcome Address and Introductory Remarks||Thomas Kodadek, Hendrik Luesch, Peter Swaan & Rolf Renne|
Session 1: Natural Products Chemistry (Moderators: Hendrik Luesch & Yousong Ding)
|9:15-10 a.m.||Keynote: Marine Polyketide Cancer Drug Candidates: Full Stereochemical Assignments by Genomic Bioinformatics||William Fenical|
|10-10:25 a.m.||Leverage a Large Actinobacterial Strain Collection for Natural Products and Drug Discovery||Ben Shen|
|10:25-10:35 a.m.||Coffee Break|
|10:35-11:00 a.m.||Behavior-guided Discovery of Natural Products||Sandra Loesgen|
|11:00-11:25 a.m.||Discovery, Biosynthesis, and Biological Roles of Hybrid Polyketide-Nonribosomal Peptidesfrom Animals||Rebecca Butcher|
|11:25-11:50 a.m.||Unlocking the Therapeutic Potential of Natural Products from Marine Cyanobacteria||Hendrik Luesch|
|11:50 a.m.-1:00 p.m.||Lunch||––|
Session 2: Manipulation of Protein Homeostasis (Moderators: Hendrik Luesch & Jianfeng Cai)
|1:00-1:45 p.m.||Keynote: Proximity Therapeutics as a New Drug Discovery Strategy||Nathanael Gray|
|1:45-2:10 p.m.||New Directions in Degrader Development||Tom Kodadek|
|2:10-2:35 p.m.||Discovery of Bcl-xL/Bcl-2 Dual Degraders||Guangrong Zheng|
|2:35-2:55 p.m.||Coffee Break||––|
Session 3: Medicinal Chemistry & Drug Development (Moderator: Tom Kodadek)
|2:55-3:40 p.m.||Keynote: Co-opting the Ubiquitin System for Therapeutic Benefit||Ingrid Wertz|
|3:40-4:05 p.m.||Rapid Generation of Ring Fusion Scaffolds from Indoles & Indole Alkaloids as a Platform for Discovery||Rob Huigens|
|4:05-4:30 p.m.||Targeting PRMT5 for MTAP-deleted Cancers||Chenglong Li|
|4:30-6:00 p.m.||Poster Session and Reception||––|
|7:00 p.m.||Speakers Dinner at home of Tom Kodadek||––|
April 21, 2023
Session 4: Chemical Proteomics & Metabolomics (Moderators: Tom Kodadek & Lina Cui)
|9:00-9:45 a.m.||Keynote: Reimagining Druggability using Chemoproteomic Platforms||Dan Nomura|
|9:45-10:10 a.m.||AI-driven Drug Discovery||Yanjun Li|
|10:10-10:35 a.m.||Photocatalytic Proximity Labeling for Chromatin Biology||Ciaran Seath|
|10:35-11 a.m.||What does Mycobacterium tuberculosis share with marine bacteria?||Luiz Carvalho|
|11-11:15 a.m.||Coffee Break||––|
Session 5: Receptors & Membrane Proteins (Moderator: Chengguo Xing)
|11:15-11:40 a.m.||Macrocyclic Peptides as Potential Treatments for Substance Abuse||Jane Aldrich|
|11:40 a.m.-12:05 p.m.||Kratom: Gas Station Garbage or Medical Magic||Chris McCurdy|
|12:05-12:30 p.m.||The Pharmacology of Mu Opiod Biased Agonists||Laura Bohn|
|12:30-12:45 p.m.||Closing Remarks||Hendrik Luesch|
|12:45-2 p.m.||Lunch & Departure||––|
Keynote Speakers & Abstracts
Scripps Institution of Oceanography
University of California
San Diego, CA
Marine Polyketide Cancer Drug Candidates: Full Stereochemical Assignments by Genomic Bioinformatics
Over the past few years, our interest in exploring marine type 1 polyketides and their applications in cancer drug discovery have involved studies of numerous strains of marine-derived bacteria. These bacteria are actinomycetes assigned to the genera Micromonospora, and Streptomyces, as well as a rare, undescribed new genus. The polyketides from these strains generally possess more than 16 chiral centers making their assignments one of the most difficult activities in natural products structure elucidation. With accurate genomic data now available, the stereospecificities of type 1 modular enzymes allows stereochemical assignments with relatively high levels of accuracy. This presentation illustrates these principles used to assign the full structures of three new classes of polyketides.
Nathanael S. Gray
Department of Chemical and Systems Biology
Proximity Therapeutics as a New Drug Discovery Strategy
Proximity Therapeutics refers to the development of potential therapeutic agents that work by inducing the physical proximity of two biomolecules. The most well-established classes of proximity therapeutics are bivalent antibodies and small molecule E3 molecular glues that induce protein degradation. A central challenge in proximity-based therapeutics is developing the appropriate chemical matter for inducing the desired protein-protein interactions. In this talk I will discuss addressing this challenge for protein degraders and transcription-factor chemical induce degrader (TCIPs). Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-dependent degradation of proteins. TPD is of interest in drug development, as it can address previously inaccessible targets. However, degrader discovery and optimization remains an empirical process due to a lack of understanding of the relative importance of the key molecular events required to induce target degradation. Here I describe our labs efforts to develop efficient methods to discover and characterize new degraders focused on protein kinase targets. I will also discuss our labs efforts to develop chemical inducers of proximity to re-wire cellular transcription. We developed bivalent compounds that recruit the transcriptional co-activator Brd4 to the transcriptional repressor Bcl6 which result in activation of a pro-apoptotic gene expression program.
CEO, Lyterian Therapeutics
Co-opting the Ubiquitin System for Therapeutic Benefit
The ubiquitin system is a primary conduit for the regulated degradation of cellular proteins. Ubiquitination describes the covalent modification of protein substrates with ubiquitin, a small protein that binds the proteasome and directs substrate degradation. Our goal is to co-opt the ubiquitin system, and more broadly protein homeostasis, to irreversibly regulate challenging therapeutic targets for enhanced clinical efficacy. Our efforts are focused on targets for which there is a clear rationale for homeostatic regulation over target inhibition. We will discuss strategies to co-opt protein homeostasis, highlight mechanisms for how selective targeting can be achieved, and review the cellular and physiological consequences of target regulation, with an emphasis on maximizing safety and therapeutic benefit for patients.
Berkeley College of Chemistry
University of California – Berkeley
Reimagining Druggability using Chemoproteomic Platforms
The Nomura Research Group is focused on reimagining druggability using chemoproteomic platforms to develop transformative medicines. One of the greatest challenges that we face in discovering new disease therapies is that most proteins are considered “undruggable,” in that most proteins do not possess known binding pockets or “ligandable hotspots” that small-molecules can bind to modulate protein function. Our research group addresses this challenge by advancing and applying chemoproteomic platforms to discover and pharmacologically target unique and novel ligandable hotspots for disease therapy.