6th UF Drug Discovery Symposium

April 15-16, 2024

Join us at the 6th UF Drug Discovery Symposium

The 2024 symposium will be held at the Hilton UF Conference Center in Gainesville, Florida on April 15-16, 2024

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A Message from the Hosts

Tom Kodadek Headshot

Professor of Chemistry

Thomas Kodadek, Ph.D.

Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology | Jupiter, FL

Hendrik Luesch headshot

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.

Directions


Schedule of Events

April 15, 2024

Welcome

Time Session Speaker
7:30 – 8:30 a.m. Registration and Breakfast
8:30 – 8:50 a.m. Welcome Address and Introductory Remarks Hendrik Luesch, Thomas Kodadek, Peter Swaan and Jon Licht

Session 1: Induced Proximity Drug Discovery (Moderators: Xingui Liu and Ciaran Seath)

Time Session Speaker
8:50 – 9:30 a.m. Keynote: How PROTAC Degraders Work: Molecular Recognition and Design Principles Alessio Ciulli
9:30 – 9:50 a.m. Chemical Manipulation of Protein Post-Translational Modifications Thomas Kodadek
9:50 – 10:10 a.m. Chemical Tools to Study Biological Systems Monika Raj
10:10 – 10:30 a.m. Leucine Rich Repeat Kinase 2 PROTACs Xingui Liu
10:30 – 10:50 a.m. Altering the H3 Methylation Landscape through Degradation of Methyl-Lysine Reader Proteins Lindsay James
10:50 – 11:05 a.m. BREAK

Session 2A: Emerging Voices in Drug Research (Moderators: TBA)

Time Session Speaker
11:05-11:30 a.m. Short talks by postdoctoral fellows Postdoctoral Fellows
11:35 a.m. – 12:35 p.m. LUNCH BREAK

Session 3: Drug Discovery for Infectiouis Diseases (Moderator: Luiz Carvalho and Robert Huigens)

Time Session Speaker
12:35 – 1: 15 p.m. Keynote: Using Complex-and-Diverse Small Molecules to Explore Drug-Resistant Bacteria and Develop Novel Antibiotics Paul Hergenrother
1:15 – 1:35 p.m. Targeting Klebsiella pneumoniae Extracellular Polysaccharides Facilitates Capsular Loss and Biofilm Matrix Collapse Renee Fleeman
1:35 – 1:55 p.m. Nature-Inspired Strategies to Overcome Mycobacterial Drug Resistance and Tolerance Kyle Rohde
1:55 – 2:15 p.m. A Multidisciplinary Approach to Developing a Targeted Therapy to Eliminate a Keystone Dental Pathogen from Oral Biofilms Jose Lemos
2:15 – 2:35 p.m. Repurposing of Type II Human Kinase Inhibitors: Discovery of Resistance-Refractory Prophylactic and Therapeutic Antimalarial Debopam Chakrabarti
2:35 – 2:50 p.m. BREAK

Session 4: Natural Products and Synthetic Biology (Moderators: Marc Chevrette and Matthew Disney

TIME SESSION SPEAKER
2:50 – 3:30 p.m. Keynote: TBA Brian Blagg
3:30 – 3:50 p.m. Advancing the Palmerolides Bill Baker
3:50 – 4:10 p.m. Genome Mining for Bacterial Terpenoids Jeff Rudolf
4:10 – 4:30 p.m. Unveiling and Engineering Nature’s Tools for Diketopiperazine Assembly Amy Lane
4:30 – 4:50 p.m. TBA Amor Menezes
4:50 – 6:30 p.m. Poster Session Modulators: Manyun Chen and Zhixing Wu

April 16, 2024

Welcome

Time Session speaker
7:30-8:40 a.m. Registration and Breakfast
8:40 – 8:50 a.m. Introduction to Day 2 Events Hendrik Luesch and Thomas Kodadek

Session 5: AI-driven Drug Discovery (Moderators: Chenglong Li and Yanjun Li)

Time Session Speaker
8:50 – 9:30 a.m. Keynote: Virtual Screening with GNINA and Pharmit David Koes
9:30 – 9:50 a.m. Rational Enzyme Engineering via AI for Therapeutic Development Wenjun Xie
9:50 – 1:10 a.m. Learning the Language of Life from DNA and Proteins Yana Bromberg
10:10 – 10:30 a.m. Exploring Vast Molecular Spaces with Instant Similarity Ramon Alain Miranda Quintana
10:30 – 10:50 a.m. A Machine Learning Framework for Cancer Drug Sensitivity Estimation Using Time-lapse Microscopy Imaging Wei Zhang
10:50 – 11:05 a.m. BREAK

Session 2B: Emerging Voices in Drug Research (Moderator: Gustavo Seabra)

Time Session Speaker
11:05 – 11:30 a.m. Short talks by graduate students Graduate Students
11:35 a.m. – 12:35 p.m. LUNCH BREAK with Sponsor Presentations

Session 6: Synthesis-driven Drug Discovery (Moderators: Jane Aldrich and Justin Lopchuk)

Time Session Speaker
12:35 – 1:15 p.m. Keynote: Adventures in Drug Hunting Wendy Young
1:15 – 1:35 p.m. Accelerating drug discovery through innovation in asymmetric S(VI) reagents and methods Justin Lopchuk
1:35 – 1:55 p.m. Late-Stage C-H Functionalization of Bioactive Compounds Masayuki Wasa
1:55 – 2:15 p.m. Terpene-Inspired Mevalonate Pathway Inhibitors James Frederich
2:15 – 2:35 p.m. Diversity-Oriented Synthesis and MS/MS-Based Analysis of Brain Glycosphingolipids Zhongwu Guo
2:35 – 3 p.m. Closing Remarks and Awards Hendrik Luesch and Thomas Kodadek

Keynote Speakers & Abstracts

William Fenical 

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. 

William Fenical

Nathanael S. Gray

Department of Chemical and Systems Biology
Stanford University
Stanford, CA

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. 

Ingrid Wertz

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.

Dan Nomura

Berkeley College of Chemistry
University of California – Berkeley
Berkeley, CA

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.

Dan Nomura

Thank You to Our Sponsors

6th UF Drug Discovery Sponsors

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