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Meeting Report

Metabolic Diseases Drug Discovery World Summit

July 28 - 29, 2003, San Diego, CA, USA

Pages 1721-1726 | Published online: 02 Mar 2005

Bibliography

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  • •Potent and competitive PTP1B inhibitors with X-ray crystal structure are discussed.
  • LIU G, XIN Z, PIE Z et al: Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor. Med. Chem. (2003) (In press).
  • ZINKER BA, RONDINONE CM, TREVILLYAN JM et al: PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice. Proc. NatL Acad. Sci. USA (2002) 99(17):11357–11362.
  • •Good introduction and a nice example of ASO technology application.
  • GIANNOUKAKIS N: Exenatide. Amylin/ Eli Lilly. CLIFF. Opin. Investig. Drugs (2003) 4(4):459–465.
  • ••Good source for source references.
  • VILLHAUER EB, BRINKMAN J, NADERI GB et al: 1-[[(3-Hydroxy- 1-adamantyl) amino] acetyl]-2-cyano-(5)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J. Med. Chem. (2003) 46(13):2774–2789.
  • ••Excellent source of DPP IV inhibitor SARand in vivo data.
  • BEBERNITZ GR, AICHER TD, STANTON JL et al.: Anilides of (h) - trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.j. Med. Chem. (2000) 43(11):2248–2257.
  • ••Original publication with rationale for GKas a target for Type 2 diabetes, and in vivo efficacy on a representative GK activator.
  • GRIMSBY J, SARABU R, CORBETT WL et al.: Allosteric activators of glucokinase: potential role in diabetes therapy. Science (2003) 301:370–373.
  • GANTZ I, FONG TM: The melanocortin system. Am. J. Physiol EndocrinoL Metab. (2003) 284:E468–E474.
  • HIRST GC, AQUINO C, BIRKEMO L: Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II):u optimization of the C3 amino substituent. I Med. Chem. (1996) 39(26):5236–5245.
  • CLARK RV et al. ENDO 2002-84th Annual Meeting of Endocrine Society San Francisco, FL, USA (2002) (Abstract P3–441).

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