Scot Mente to Speak at Protein Kinases & Drug Design Conference (October 23-24, 2014 in Boston)

Top Quote Scot Mente, Senior Principal Scientist, Neuroscience Chemistry at Pfizer Research will give a presentation on, "Structure-Guided Design of CNS-Active CK1d Preferring Ligands" at the 3rd Protein Kinases & Drug Design Conference (October 23-24, 2014 in Boston, MA) by GTCbio. End Quote
  • (1888PressRelease) July 31, 2014 - Casein kinase 1 delta (CK1δ) inhibitors are potential therapeutic agents for a range of psychiatric disorders. The feasibility of developing a CNS kinase inhibitor has been limited by the ability to identify brain penetrant compounds with high selectivity and appropriate safety profiles. To address these issues, a novel computational method has been established to predict the maximum free brain concentrations of viable synthetic targets. In conjunction with structure-based drug design, potent CNS active CK1d inhibitors were identified.

    This talk will cover:
    • Getting the MAX out of computational models: the prediction of unbound-brain and unbound-plasma maximum concentrations.
    • Strategies to optimize whole-cell potency.
    • Structure-based efforts to target Kinome selectivity.
    • In vivo activity profiles of CNS-active CK1d preferring compounds.

    GTCbio's 3rd Protein Kinases & Drug Design Conference, to be held in October 23-24, 2014, Boston, MA, will bring together speakers representing world-leading academic centers and pharmaceutical companies to discuss how to overcome the many hurdles and answer exciting key questions. Experts will also share their positive and negative experiences on how predictive preclinical models are with clinical efficacy and toxicology.

    Sessions for 2014 Agenda:
    I. Advancements in Target Identification & Validation
    II. New Directions for Kinase Inhibitor Drug Discovery
    III. Kinase Drug Design & Medicinal Chemistry
    - Reversible vs. Irreversible Kinase Inhibitors
    - Allosteric Inhibitors
    IV. Selective vs. Non-selective Targeting of Protein
    V. Mechanisms of Resistance to Kinase Inhibitors
    VI. Lessons from Preclinical Model & Clinical Development

    This conference is part of our Protein Discovery Summit 2014, which consists of this and three additional parallel conferences shown below:

    - Protein-Protein Interaction
    - Antibody & Protein Therapeutics
    - Protein Expression, Purification & Characterization
    - Protein Kinases & Drug Design

    For more information, please visit www.gtcbio.com

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