Synthesis and conformational analysis of peptide inhibitors of farnesyltransferase

…, Y Lelievre, M Duchesne, FF Clerc, D Scherman…

Index: Byk, Gerardo; Lelievre, Yves; Duchesne, Marc; Clerc, Francois F.; Scherman, Daniel; Guitton, Jean Dominique Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 1 p. 115 - 124

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Citation Number: 15

Abstract

Farnesylation of the ras oncogene product by Farnesyl Transferase (FTase) is known to be a critical step in cell transformation leading to uncontrolled proliferation. The peptide CysValTicMet is a potent FTase inhibitor, but its degradation by amino-peptidases and its only weak internalization into cells make it a bad candidate for a future cancer drug. We have prepared improved CysValTicMet analogues using several approaches:(i) amino ...

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Discovery of tetrahydroisoquinoline-based CXCR4 antagonists

[Truax, Valarie M.; Zhao, Huanyu; Katzman, Brooke M.; Prosser, Anthony R.; Alcaraz, Ana A.; Saindane, Manohar T.; Howard, Randy B.; Culver, Deborah; Arrendale, Richard F.; Gruddanti, Prahbakar R.; Evers, Taylor J.; Natchus, Michael G.; Snyder, James P.; Liotta, Dennis C.; Wilson, Lawrence J. ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 11 p. 1025 - 1030]

Synthetic investigations of (1, 3′)-bistetrahydroisoquinolin...

[Aubry, Sylvain; Pellet-Rostaing, Stephane; Fenet, Bernard; Lemaire, Marc Tetrahedron Letters, 2006 , vol. 47, # 8 p. 1319 - 1323]