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The chink in the armour: taking aim at metals in enzymes

Delve into the world of metalloproteins, vital for diseases like heart disease and cancer, and explore innovative drug design strategies targeting these enzymes with improved warheads from familiar compounds.

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The chink in the armour: taking aim at metals in enzymes

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  1. U.C.S.D. News Media Workshop Dec. 9, 2005 The chink in the armour: taking aim at metals in enzymes Seth M. Cohen Department of Chemistry and Biochemistry University of California, San Diego La Jolla, CA 92093-0358

  2. What are Metalloproteins? Hemoglobin - requires Iron • A metalloprotein is simply a protein that requires a metal to do its job.

  3. x Proteases • Proteases are proteins that ‘cut up’ other proteins. • Metalloprotein + Protease = Metalloprotease.

  4. Matrix Metalloprotease (MMP) = Zinc • MMP are important targets for heart disease.

  5. Histone Deacetylase (HDAC) • HDAC are important targets for cancer.

  6. Anthrax Lethal Factor (LF) • LF is an important target for anthrax. • In all three cases the drug binds to the zinc.

  7. Drug Design - A Guided Missile MMPi Warhead HDACi LFi Guidance System

  8. Goal – Better Warheads • A wide variety of guidance systems have been examined. • The ‘warhead’ is the focus of our research efforts (hydroxamic acid alternatives) – a more powerful warhead should generate a more potent drug.

  9. New Warheads • Using compounds already found in food and cosmetic products, we found improved warheads that are more effective at stopping metalloproteases.

  10. The Most Important Slide Current Members David T. Puerta Faith E. Jacobsen Jana A. Lewis Dr. Jay Stork Misha V. Golynskiy Sara R. Halper Sara Thoi Loi Do Former Members Ba L. Tran Talib C. Davis Scot A. Lieser Alexis Kaushansky Heather Delaney Carmen Velez David Tat Dr. Drew L. Murphy Prof. M.R. Malachowski Prof. G. Olivier-Lilley

  11. Acknowledgements Collaborators • Prof. J. Andrew McCammon • John Mongan • Julie Schames • Dr. Richard Henchman • Prof. Francisco Villarreal • Diego Romero-Perez • Michael Griffin • Dr. Ricardo Garcia • Prof. Arnold Rheingold • Dr. Lev Zakharov Funding • UCSD • American Heart Association • Research Corporation • Hellman Family Fund • NSF (CAREER award) • ACS-PRF (AC and G grant) • UCSD Moores Cancer Center • UCSD Academic Senate • ARCS, GAANN, and UC TSR&TP fellowships (J.A.L., F.E.J.) • NSF fellowship (S.R.H.) • NIH fellowship (D.T.P.)

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