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Cambridge Healthtech Institute’s Tools & Technologies for HTS brings together experts from across many areas of lead discovery, focusing on topics such as strategies for hit triage to combining multiple label free platforms to improve hit identification success. Experts present unpublished data, results from technology comparisons and novel applications in front of an audience of peers from across pharmaceutical drug discovery high throughput screening & lead optimization organizations. 

TUESDAY, JUNE 7

7:45 am Registration and Morning Coffee

Keynote Session

8:45 Chairperson’s Opening Remarks

Daniel G. Sipes, Director of Advanced Automation Technologies, Genomics Institute of the Novartis Research Foundation

8:55 Strategies for Uncorking the Drug Discovery Process

Rathnam Chaguturu, Ph.D., Director, High-Throughput Screening Laboratories, University of Kansas; Editor-in-Chief, Combinatorial Chemistry and High-Throughput Screening

High-throughput screening has not been the panacea for drug discovery as one was led to believe at first. The talk will address the need for appropriate technology platforms to deorphanize the refractory targets, a critical expansion in chemical diversity of the screening libraries, and a radical paradigm shift in the judicial progression of the screen actives through the hit to probe to lead optimization stages. Academia has now entered the high-throughput screening arena which has long been the forte of the pharmaceutical industry. A strategic partnership between these two divergent institutions is certainly poised to take new lead drug discovery efforts to greater heights.

9:25 Improving Drug Candidate Optimization by Streamlining Processes and Harnessing Advanced Discovery Platforms

Litao Zhang, Ph.D., Executive Director, Applied Biotechnology, Lead Evaluation and Mechanistic Biochemistry, Bristol-Myers Squibb

During the past two decades, the process supporting lead optimization of drug discovery has been significantly challenged by two major trends. One trend is that explosion of the number of hits being identified using multiple high-throughput technology platforms. The other trend is the urgent needs to increase the success rate of drug candidates from pre-clinical research to clinical application. To manage these increased demands coming from both trends, researchers in the pharmaceutical companies have been forced to streamline the discovery process and apply innovative solutions to rapidly optimize compounds from hits to leads. This talk will outline the challenges and future directions how to harness advanced technology platforms and build efficient processes for selecting the best all-around drug candidates for drug development.

9:55 Networking Coffee Break

 

Hit Triage

10:25 Integrated Lead Finding

Peter Fekkes, Ph.D., Head, Open Access Medium Throughput Screening Center, Center for Proteomic Chemistry Lead Finding Platform, Novartis Institutes for BioMedical Research

10:55 Application of Label Free Technologies for Mechanistic-Based Assessment to Accelerate Hit Triage

William Metzler, Ph.D., Associate Director, Mechanistic Biochemistry, Bristol-Myers Squibb

We have selectively integrated several biophysical methods to create progressibility profiles for each hit, examining a compound’s propensity to aggregate, its specificity of binding, its stoichiometry of binding, and thermodynamic properties. Combined with the mapping of receptor:ligand interactions at the molecular level that is afforded by structural studies, the approach provides additional information for selecting hits that are the most likely to progress at a critical point in early-phase decision, thereby facilitating the delivery of high quality leads.

11:25 Strategies for Improving Hit Triage

Marina Nelen, Ph.D., Senior Scientist , Lead Discovery, Research Capabilities Organization , Janssen Pharmaceuticals

How can one avoid wasting time and resources on false hits and common artifacts? Exploiting automation, parallel processes, and various assay technologies, we have established an efficient method of hit triage by profiling compounds through multiple orthogonal assays in parallel. This approach of utilizing cross-assay data interpretation is general and can benefit any early discovery program.

11:55 Luncheon Presentations (Sponsorship Opportunities Available) or Lunch on Your Own

 

Ion Channels & Electrophysiology

1:30 pm Chairperson’s Remarks

Michael F.A. Finley, Ph.D., Assay Development Team Lead, Small Molecule Screening, Exploratory & Translational Sciences, Merck & Co.

1:35 Inter-Assay Correlation for Ion Channel Screening

Michael F.A. Finley, Ph.D., Assay Development Team Lead, Small Molecule Screening, Exploratory & Translational Sciences, Merck & Co.

Cell based high-throughput screening for ion channels largely relies on fluorescence assays to detect permeant ions or changes in membrane potential. Patch clamp electrophysiology remains the most direct approach for studying ion channel pharmacology, but its application to screening is limited due to extremely low-throughput and technical difficulty. We compare fluorescence-based and automated patch-clamp assays from distinct ion channel targets to help identify compounds with desirable activity.

2:05 Changing the Game in Ion Channels: Ultra High-Throughput Automated Electrophysiology

Adam Hendricson, Ph.D., Applied Biotechnology & Lead Evaluation, Bristol-Myers Squibb

To drive the next evolution in channel research, we sought an ultra high- throughput, high data fidelity, automation-adaptable EP platform to enable multi-parallel panel-based efficacy and selectivity screening. Using the SyncroPatch 96 from Nanion, we have developed the Ion FlexScreen platform, which revolutionizes hit-to-lead progression via massively parallel multi-channel panels. Through synergies with laboratory automation, we have enabled order-of-magnitude reductions in FTE resource on a per-program basis, and held costs flat. The presentation will discuss the functional outputs of Ion FlexScreening, and explore representative data and core technology innovations.

Sponsored by
Chantest 
2:35 High-Throughput Voltage-Clamp Assays of Ligand-Gated Ion Channels
Glenn E. Kirsch, Ph.D., Senior Director, Pharmacology and Program Management, ChanTest Corporation
Recent advances in planar array patch clamp systems have opened the door to large-scale screening of ligand-gated channels. Results will be presented from studies in a diverse group of ion channels, including ASIC1a, 5-HT3a, nAChR, and NMDAR.

 

HT-Mass Spectroscopy

3:05 Optimizing Lead Optimization Assays: Case Studies Using LC/MS

Lynn Abell, Ph.D., Senior Principal Scientist, Bristol-Myers Squibb

During the lifetime of a drug discovery program, the primary in vitro SAR assay undergoes continuous evolution. As compounds become more potent, increased sensitivity is needed; PD relationships may require assays with physiologically relevant substrates. With each change, a significant effort must be expended in assay development and cross validation. We sought to streamline this process by developing robust and sensitive assays with sufficient throughput to support large medicinal chemistry efforts, using physiologically relevant substrates, early in the lifetime of the program.

3:35 Grand Opening Refreshment Break in the Exhibit Hall

4:35 HTMS - From in vitro to ex vivo: 5-Lipoxygenase and Beyond

Robert Hills, Ph.D., Senior Scientist, Lead Discovery, East Coast RCO, Janssen Pharmaceutical Companies of Johnson & Johnson

Leukotreines play an essential role in eliciting and prolonging inflammation.  To interrogate this pathway, we have undertaken a translational assay approach, relying on LC/MS/MS and HT/MS to profile substrates, intermediates and products from in vitro enzyme assay to ex vivo challenge models.  Therefore, focusing on one set of key metabolites, assayed using one platform, for each phase of lead development

5:05 EXPERT PANEL: Translating Technologies Outside the HTS Lab

Moderator : Litao Zhang, Ph.D., Executive Director, Applied Biotechnology, Lead Evaluation and Mechanistic Biochemistry, Bristol-Myers Squibb

 

• The push for translational medicine

• ADME/Tox screening

• Biomarker discovery

5:35 - 6:30 Happy Hour in the Exhibit Hall



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