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SBS 12th Annual Conference and Exhibition
Advancing Drug Discovery: From Better Hits to Better Candidates
September 17-21, 2006 - Seattle, WA, USA
Meet TimTec at booth 248
The theme of the SBS 2006 annual conference in Seattle highlights the impact of screening and technology applications on drug discovery. With over a decade of HTS and combinatorial chemistry strategies now behind us, it is important to understand and critique the impact these technologies have had on providing better hits, better leads and most of all, better drug candidates to ultimately improve the quality of patient care.Technical Session Summaries
No matter what part of the drug-discovery process you’re involved in, you’ll find plenty to interest you in the 2006 SBS Technical Sessions. This professional program presents issues and information from the best minds in the industry—covering the latest developments at every stage of the process and in every area of drug discovery.
With an unparalleled professional program comprising more than 45 presentations, you’ll get useful information and valuable insights to take back to your lab or workplace.
* Advanced Technology for Drug Discovery
* Target Biology and Screening
* Cells & Protein Production: Keeping Pace with Drug Discovery
* Creating New Chemical Space for Lead Discovery
* Defining Target & Compound Specificity
* Hit to Lead Processes
* Imaging & High Content Assays
* Structural Biology & Lead Optimization
* ADME/Toxicology in Early Drug Discovery
* Knowledge Management & Extracting Value from Large Data Sets
* Biomarkers for Pre-clinical & Clinical Evaluation of New Drugs
* Drug Discovery for Diseases of the Developing World
* Systems Biology & Confluence with Drug Discovery
Advanced Technology for Drug Discovery
Session Chairs:
Scott Diamond, University of Pennsylvania, USA
David Weaver, Vanderbilt University, USA
HTS labs are now conducting a continually increasing number of assays per year and are also encountering more difficult and nontraditional assays. This session will focus on emerging platforms and detection systems relevant to high-throughput screening challenges, including flow cytometry based HTS, microfluidics, microsensing, chemical microarrays, and label-free detection using mass spectrometry. Attendees of this session will learn how experts in the field are applying new technologies for challenging applications.
Target Biology & Screening sponsored by
Gary Krishnan, Eli Lilly, USA
Peter Lander, Eli Lilly, USA
Many companies have established platform approaches to identify novel leads and drug candidates for protein families or classes such as GPCRs, enzymes and ion channels. These efforts have addressed target biology and screening and have presented exciting opportunities to address therapeutic opportunities. These platform approaches have enabled high-throughput assays that optimally address target biology and selectivity and seize synergies among the individual projects in the same target class. This session will focus on the application of novel and traditional approaches used to produce better leads and candidates that target the biology of these important target classes.
Cells & Protein Production: Keeping Pace with Drug Discovery
Session Chairs:
Tom Kost, GlaxoSmithKline, USA
Lorenz Mayr, Novartis Pharma AG, Switzerland
The timely development, production and supply of high quality protein and cell-based reagents for HTS and compound profiling assays present a continual challenge within drug-discovery programs in both Pharma and Biotech. In addition to validating that a large number of diverse reagents possess the desired biological properties, one often needs to consider biosafety, stability, delivery, storage and tracking requirements. These requirements take on increased importance in the framework of the dramatic increase in the number of screening assays being performed in automated facilities that may be carried out by different groups in geographically distinct locations. Furthermore, recent trends in industry towards targets with less target validation and detailed knowledge about target production, demand continual enhancements of reagent production technologies. Attendees will learn of current approaches and future challenges of keeping pace with the supply of biologically relevant proteins, membranes, viruses and cells required to conduct productive drug-discovery programs.
Creating New Chemical Space for Lead Discovery
Session Chairs:
Michael Sofia, Pharmassett, Inc., USA
Armen Boldi, Discovery Partners International, USA
The objective of lead discovery is to identify a series of chemotypes that can be further progressed into expanded lead optimization. The primary strategies that are employed to support lead generation include high-throughput screening, focused screening, and structure-based approaches. All of these approaches require access to novel and diverse sets of compounds from either natural or synthetic sources that can be evaluated against the biological target of interest. The development of the necessary chemical space to support productive lead generation has spawned new approaches in the areas of natural products and synthetic natural product-like molecules, the evolution of high-throughput chemistry, the application of lead-like versus drug-like concepts, and the development of fragment-based strategies. It has also led to significant efforts to understand the interface between chemical and biological space and what characteristics are important in making a collection of compounds productive for lead generation. This session will address current chemical and theoretical approaches that are being employed to ensure that lead discovery efforts are providing quality leads to support down stream lead optimization needs.
Defining Target & Compound Specificity
Session Chairs:
William Janzen, Amphora Discovery Corporation, USA
Doriano Fabbro, Novartis Institute for Biomedical Research, Switzerland
Target specificity can mean many different things. Protein families such as protein kinases, GPCRs and ion channels play an essential role in many signaling pathways, and have, therefore, the potential to contribute to diseases ranging from cancer, inflammation and diabetes to cardiovascular and infectious disorders. Specificity as it is related to disease involvement is key to defining druggable targets, but identification of specific interactions and functional validation of targets remains a challenge. This session will explore contextual usage of the term specificity as well as methods for exploring compound target interactions and innovative approaches that have been developed to address specificity.
Hit to Lead Processes
Session Chairs:
Michael Sofia, Pharmasett, Inc., USA
Raju Mohan, Exelixis, Inc., USA
Prior to committing significant lead optimization resources to a HTS, active extensive validation of the chemotype is required. Therefore, the “hit to lead” process has evolved as a distinct phase in medicinal chemistry, bridging the gap between lead generation and full medicinal chemistry lead optimization. This process typically entails assessment of the pool of screening actives, validation of progressible SAR within selected chemical series, an early understanding of potential toxicological or metabolic liabilities, a clear understanding of IP and freedom-to-operate scope, and demonstration of in vitro potency and early indications of in vivo efficacy where possible. New cheminformatics tools, high-throughput assays that support liability assessment and the application of rapid analoging to scope out SAR trends are only a few of the emerging technologies utilized in critical decision making in the hit-to-lead phase. This session will highlight real examples of hit to lead development and showcase the application of novel approaches and tools that help accelerate the process.
Imaging & High Content Assays
Session Chairs:
Tina Garyantes, Sanofi-Aventis, USA
Renata Schnitzer, Boehringer Ingelheim, Austria
As the pharmaceutical industry struggles to increase productivity, there is a move toward using more physiologically relevant cellular assays and acute in vivo models earlier in the drug-discovery process. Examples include the re-emergence of phenotypic screening, the use of translocation assays for GPCRs and tyrosine kinase receptors, acute models of metastasis, and MRI and PET scanning of bone damage during osteoporosis and arthritis. At the same time, imaging technologies are maturing and penetrating into more laboratories where they are helping to advance compounds to or toward candidate status. This session will highlight examples of how these techniques can drive drug discovery ranging from cellular HCS to whole animal studies both at the lead identification and lead optimization phases.
Structural Biology & Lead Optimization
Session Chairs:
Harren Jhoti, Astex Therapeutics Ltd., United Kingdom
Kendall Nettles, The Scripps Research Institute, USA
The use of structure-based drug design methods in the discovery of novel lead compounds has grown significantly in the last decade. This has been largely due to technology advances in structural biology that allow scientists to obtain protein/ligand structures in a timely manner to guide medicinal chemistry. As a consequence lead optimization programs are now able to more efficiently generate drug candidates with the desired properties. Furthermore, high-throughput methods in crystallography and NMR have also allowed structure-based methods to establish new approaches for lead generation, such as fragment-based discovery. This session will outline some of the key technology advances in structural biology and illustrate their application for structure-based lead generation and optimization.
ADME/Toxicology in Early Drug Discovery
Session Chairs:
Kirk McMillan, Exelixis, Inc., USA
Charles Crespi, BD Biosciences, USA
Early application of ADME/toxicology assays in support of lead validation/optimization has become a critical component of small molecule drug discovery in both pharma and biotech organizations. Implementation of in vitro assays for profiling metabolic stability, cytochrome P450 inhibition, cell (or membrane) permeability and physicochemical properties (solubility, lipophilicity, pKa, etc.), as well as assays for identifying hepatoxicity, reactive metabolites, HERG channel interaction and genotoxicity have become routine determinants of a candidate’s “drugability”. These profiling assays in conjunction with extensive in vivo DMPK/toxicology studies have resulted in the selection of better clinical candidates and reduced compound attrition. This session will address new technologies, current practices and future directions for this important aspect of preclinical drug discovery and development.
Knowledge Management & Extracting Value from Large Data Sets
Session Chair:
Robert Brown, SciTegic, USA
Access to accurate, comprehensive and up-to-date information is key to making good project decisions during the discovery process. This symposium will consider challenges and solutions in gathering, organizing, analyzing and presenting discovery information for a research organization, for both internal and externally generated data. The session will address new paradigms for information and knowledge management and the application of new techniques such as workflow to increase the efficiency and effectiveness of information organization and data analysis. We will also present the architecture, design and functionality of knowledge management systems and case studies of their operational effectiveness in the drug-discovery process. The impact of external resources such as target class knowledge bases in drug discovery and their integration into information and knowledge management systems will also be discussed.
Biomarkers for Pre-clinical & Clinical Evaluation of New Drugs
Session Chairs:
Nicholas Dracopoli, Bristol-Myers Squibb, USA
Thomas White, Celera Diagnostics, LLC, USA
Biomarkers are being increasingly used in all aspects of drug development from target discovery to life cycle management. Early implementation of biomarker discovery and assay development strategies into the clinical development plan is essential for clinical trial design and monitoring for first-in-class compounds, as well as for second generation compounds against the same target or pathways. The definition of biomarkers is very broad and encompasses genomic biomarkers (single nucleotide polymorphisms) used in genetic association studies to dynamic markers (quantitative gene expression assays by microarrays or qPCR, proteomics and the more traditional assay formats including immunochemistry and flow cytometry). Given the breadth of opportunities for the application of biomarkers in drug development from target identification to dose selection and prediction of drug efficacy and risk of adverse events, no single biomarker strategy exists for any therapeutic area, let alone an entire discovery and development portfolio. This symposium will focus on several successful applications of both genomic and dynamic biomarkers in drug development to illustrate possible strategies to reduce attrition and accelerate clinical development.
Drug Discovery for Diseases of the Developing World
Session Chairs:
Jose F. Garcia-Bustos, GlaxoSmithKline, Spain
Lisa Conte, Napopharma, USA
Pharmaceutical products and vaccines have revolutionized health care in industrialized countries during the last century. However, this progress has barely touched low-income countries where millions of people lack access to essential medicines that could potentially have a remarkable effect on the healthcare of a third of the world’s population. Closing the gap between potential and reality entails action in these areas: incentives for academic and industrial R&D in diseases endemic in low-income countries; financing and distribution in resource-constrained areas; drug affordability; effective drug regulation to avoid misuse and fake drugs; and multi-stakeholder community based education, training, and sustainability planning. The panel will explore (a) industry-based solutions to drug development, registration, and distribution in developing and emerging economies; (b) community health initiatives; (c) incentives for tropical disease R&D; and (d) non-profit initiatives to provide access to essential drugs.
Systems Biology & Confluence with Drug Discovery
Session Chairs:
John Aitchison, Institute for Systems Biology, USA
Ilya Shmulevich, Institute for Systems Biology, USA
Rapid technological advances in large-scale data collection coupled with model-driven mathematical and computational approaches are allowing scientists to gain a global and integrated view of physiology and pathophysiology. Unlike approaches that focus on individual molecules or small groups of interacting molecules, systems-scale approaches hold the promise of deciphering large dynamic molecular networks that dictate the phenotypic state and enable principled drug target identification, validation, and the development of targeted interventions. The systems approach to biology and medicine promises to transform the practice of medicine by changing it from a reactive discipline to a predictive, preventive and personalized discipline.
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