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High Throughput Chemistry and Chemical Biology

Gordon Research Conference

Advances in Chemistry and Chemical Biology to Expand the Druggable Proteome

June 2 - 7, 2019

Chair

Vice Chair

Colby-Sawyer College

541 Main Street

New London, New Hampshire, United States

Venue and Travel Information

Conference Description

Dear colleagues,

The 2019 High-Throughput Chemistry and Chemical Biology (HTCCB) GRC provides a unique forum for pioneering multidisciplinary science at the interface of Chemistry and Biology, in a welcoming, inspiring and inclusive environment. Diversity is the essence of our conference, with speakers and attendees from academia, industry and other research institutions, at different stages of their careers and from all corners of the world. New colleagues and old friends gather in a relaxed atmosphere for collegial, dynamic discussions of the latest advances in synthetic methodologies and reaction discovery, chemical biology, “omics”, biochemistry, high throughput experimentation and computational sciences. The overarching theme of the 2019 meeting is the application of these scientific disciplines to expand the druggable proteome, and better address the challenges associated with interrogation of human biology to impact drug discovery.

In addition to invited talks, poster sessions will continue to be an important part of the scientific and social exchange at the HTCCB GRC. We encourage conferees to present posters, to foster informal live discussions throughout the conference. A selection of poster authors will be invited to present short talks on their work. Please submit a poster abstract with your conference application.

We are also pleased to announce that Evijola Llabani (University of Illinois, USA) and Carlos Moreno Yruela (University of Copenhagen, Denmark) are organizing the 6th Gordon Research Seminar (GRS) on High-Throughput Chemistry and Chemical Biology. This GRS will be held on Saturday and Sunday June 1-2, immediately prior to the GRC, and will provide an opportunity for trainees to share science and interact with leading researchers in an intimate setting. Graduate students and postdoctoral fellows are encouraged to apply to both the GRS and GRC.

We look forward to receiving your application for a memorable meeting.

Ivan Cornella-Taracido (Cedilla Therapeutics) and Ann Rowley (AbbVie)
Chair and Vice-Chair, 2019 GRC on High-Throughput Chemistry and Chemical Biology

Related Meeting

This GRC will be held in conjunction with the "High Throughput Chemistry and Chemical Biology" Gordon Research Seminar (GRS). Those interested in attending both meetings must submit an application for the GRS in addition to an application for the GRC. Refer to the associated GRS program page for more information.

Conference Program

Sunday
2:00 pm - 9:00 pm	Arrival and Check-in
6:00 pm - 7:00 pm	Dinner
7:30 pm - 7:40 pm	Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm	Keynote Session: The Impact of Chemical Biology in Drug Discovery Discussion Leader:
7:40 pm - 8:25 pm	"Activity-Based Proteomics: Protein and Ligand Discovery on a Global Scale"
8:25 pm - 8:35 pm	Discussion
8:35 pm - 9:20 pm	"Small-Molecule Control of Transcription"
9:20 pm - 9:30 pm	Discussion
Monday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Chemical Matter Diversity for Probes and Therapeutics Discussion Leader:
9:00 am - 9:05 am	Introduction by Discussion Leader
9:05 am - 9:35 am	"New Synthetic and Biophysical Methodologies in Fragment-Based Cancer Drug Discovery"
9:35 am - 9:40 am	Discussion
9:40 am - 10:10 am	"Expanding DNA-Encoded Library Chemical and Target Space with Novel Chemistries"
10:10 am - 10:15 am	Discussion
10:15 am - 10:45 am	Coffee Break
10:45 am - 11:15 am	"Chemical Tools to Understand Mechanisms that Control the Physiological Distribution of Therapeutics"
11:15 am - 11:20 am	Discussion
11:20 am - 11:50 am	"DNA Recognition and Sensing with Designed Metal Complexes"
11:50 am - 11:55 am	Discussion
11:55 am - 12:25 pm	"Photo-Affinity Probes to Interrogate Protein-Protein and Protein-Drug Interactions"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
3:00 pm - 4:00 pm	The GRC Power Hour™ The GRC Power Hour™ is designed to address challenges women face in science and issues of diversity and inclusion. The program supports the professional growth of all members of our communities by providing an open forum for discussion and mentoring. Organizers: and
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	Novel Chemistries and Reaction Scouting Discussion Leader:
7:30 pm - 7:35 pm	Introduction by Discussion Leader
7:35 pm - 8:05 pm	"Synergistic Cooperation Between Mechanistic Investigation and Catalysis: Towards Rational Design"
8:05 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	"Recent Advances in Frustrated Acid/Base Complexes as Potential Cooperative Catalysts for Practical Synthetic Transformations"
8:40 pm - 8:45 pm	Discussion
8:45 pm - 8:55 pm	"Discovery of Novel, Small-Molecule Autophagy Inhibitors Through Phenotypic and Target-Based Approaches"
8:55 pm - 9:00 pm	Discussion
9:00 pm - 9:10 pm	"Modulation of NRF2 in Chemoprevention and Cancer Therapy"
9:10 pm - 9:15 pm	Discussion
9:15 pm - 9:25 pm	"Chemical Probes with a Unique Bioorthogonal Cleavage Site for Improved Metabolomic Analysis"
9:25 pm - 9:30 pm	Discussion
Tuesday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Chemical Probes and Cellular Assays for Upcoming Druggable Targets Discussion Leader:
9:00 am - 9:10 am	Introduction by Discussion Leader
9:10 am - 9:40 am	"Emerging Chemical Labeling Methods to Analyze and Control RNA"
9:40 am - 9:45 am	Discussion
9:45 am - 10:15 am	"CRISPR-Mediated Tagging of Endogenous Proteins with a Luminescent Peptide to Quantitate Expression Dynamics"
10:15 am - 10:20 am	Discussion
10:20 am - 10:50 am	Group Photo / Coffee Break
10:50 am - 11:20 am	"Mapping of Immunomodulatory Receptor Protein Interactions via Photocatalytic-Based Proximity Labeling of the Cell Surface"
11:20 am - 11:25 am	Discussion
11:25 am - 11:55 am	"Chemical Probes to Study Epigenetic Regulation by Histone Demethylases in Health and Disease"
11:55 am - 12:00 pm	Discussion
12:00 pm - 12:10 pm	"Bioinformatics-Guided Phenotypic Screen Discovers an AKR Prodrug to Target Oncogenic Transcription Factor Driven Lung Cancers"
12:10 pm - 12:15 pm	Discussion
12:15 pm - 12:25 pm	"Photoswitchable Chimeras Enable Optical Control of Targeted Protein Degradation"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	High Throughput Experimentation in Chemistry and Chemical Biology Discussion Leader:
7:30 pm - 8:00 pm	"Enabling and Accelerating Drug Discovery with High Throughput Technologies"
8:00 pm - 8:05 pm	Discussion
8:05 pm - 8:35 pm	"Zebrafish Behavioral Profiling for Neuroactive Drug Discovery"
8:35 pm - 8:40 pm	Discussion
8:40 pm - 8:50 pm	"Functional Signature Ontology (FUSION) Mapping for Rapid Mechanism of Action Discovery"
8:50 pm - 8:55 pm	Discussion
8:55 pm - 9:05 pm	"Activity-Based DNA-Encoded Library Screening"
9:05 pm - 9:10 pm	Discussion
9:10 pm - 9:20 pm	"Discovery of Small Molecule Inhibitors of SIRPa-CD47 Interaction"
9:20 pm - 9:25 pm	Discussion
9:25 pm - 9:30 pm	General Discussion
Wednesday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Computational Methods and Machine Learning in Target Identification and Structure-Activity Relationships Discussion Leader:
9:00 am - 9:05 am	Introduction by Discussion Leader
9:05 am - 9:35 am	"Ultra-Large Library Docking for Novel Ligand Discovery"
9:35 am - 9:40 am	Discussion
9:40 am - 10:10 am	"Applications of Artificial Intelligence-Driven Molecular Design in Drug Discovery Projects"
10:10 am - 10:15 am	Discussion
10:15 am - 10:45 am	Coffee Break
10:45 am - 11:15 am	"Informatics-Enabled Early Drug Discovery: From Screening Collection Design to Omics Data Integration"
11:15 am - 11:20 am	Discussion
11:20 am - 11:50 am	"Lessons from the Largest Prospective Study of Machine Learning for Hit Discovery"
11:50 am - 11:55 am	Discussion
11:55 am - 12:25 pm	"The Use of Machine Learning for Target and Drug Discovery"
12:25 pm - 12:30 pm	Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:00 pm - 7:30 pm	Business Meeting Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
7:30 pm - 9:30 pm	Omics-Enabled Chemical Biology and Drug Discovery Discussion Leader:
7:30 pm - 7:40 pm	Introduction by Discussion Leader
7:40 pm - 8:10 pm	"Multiplexed Parallelization of Binding Site Hotspot Mapping"
8:10 pm - 8:15 pm	Discussion
8:15 pm - 8:45 pm	"Small-Molecule Inhibitors, Degraders and Activators of CRISPR-Associated Nucleases"
8:45 pm - 8:50 pm	Discussion
8:50 pm - 9:20 pm	"Novel and Optimized Chemoproteomic Methods for Identifying and Mapping Small Molecule-Protein Interactomes"
9:20 pm - 9:25 pm	Discussion
9:25 pm - 9:30 pm	General Discussion
Thursday
7:30 am - 8:30 am	Breakfast
9:00 am - 12:30 pm	Exploring Protein Homeostasis to Expand the Druggable Proteome Discussion Leader:
9:00 am - 9:10 am	Introduction by Discussion Leader
9:10 am - 9:40 am	"Structure-Based PROTAC Design"
9:40 am - 9:50 am	Discussion
9:50 am - 10:20 am	"Proteomic Connectivity Maps for Characterization and Targeting of Drugs"
10:20 am - 10:30 am	Discussion
10:30 am - 11:00 am	Coffee Break
11:00 am - 11:30 am	"High-Throughput Chemical Proteomics for Chemical Biology"
11:30 am - 11:40 am	Discussion
11:40 am - 11:55 am	"Drugging the Core Particle of the Proteasome to Increase Protein Degradation Rates"
11:55 am - 12:00 pm	Discussion
12:00 pm - 12:15 pm	"Targeted Degradation of Aberrant Tau in Frontotemporal Dementia Patient-Derived Neuronal Cell Models"
12:15 pm - 12:20 pm	Discussion
12:20 pm - 12:30 pm	General Discussion
12:30 pm - 1:30 pm	Lunch
1:30 pm - 4:00 pm	Free Time
4:00 pm - 6:00 pm	Poster Session
6:00 pm - 7:00 pm	Dinner
7:30 pm - 9:30 pm	Keynote Session: New Mechanisms of Action in Therapeutics Discussion Leader:
7:30 pm - 8:15 pm	"Chemical Tools for Unraveling Parasite Biology"
8:15 pm - 8:25 pm	Discussion
8:25 pm - 9:10 pm	"Insights in the Membrane-Bound Proteasome in Health and Disease"
9:10 pm - 9:20 pm	Discussion
9:20 pm - 9:30 pm	Closing Remarks
Friday
7:30 am - 8:30 am	Breakfast
9:00 am	Departure

Contributors

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Conference History High Throughput Chemistry and Chemical Biology (GRS)

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