Literature DB >> 9043662

Discovery of novel nonpeptide tricyclic inhibitors of Ras farnesyl protein transferase.

F G Njoroge1, R J Doll, B Vibulbhan, C S Alvarez, W R Bishop, J Petrin, P Kirschmeier, N I Carruthers, J K Wong, M M Albanese, J J Piwinski, J Catino, V Girijavallabhan, A K Ganguly.   

Abstract

A comprehensive structure-activity relationship (SAR) study of novel tricyclic amides has been undertaken. The discovery of compounds that are potent FPT inhibitors in the nanomolar range has been achieved. These compounds are nonpeptidic and do not contain sulfhydryl groups. They selectively inhibit farnesyl protein transferase (FPT) and not geranylgeranyl protein transferase-1 (GGPT-1). They also inhibit H-Ras processing in Cos monkey kidney cells.

Entities:  

Mesh:

Substances:

Year:  1997        PMID: 9043662     DOI: 10.1016/s0968-0896(96)00206-4

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

1.  Prediction and evaluation of protein farnesyltransferase inhibition by commercial drugs.

Authors:  Amanda J DeGraw; Michael J Keiser; Joshua D Ochocki; Brian K Shoichet; Mark D Distefano
Journal:  J Med Chem       Date:  2010-03-25       Impact factor: 7.446

2.  Cloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei.

Authors:  F S Buckner; K Yokoyama; L Nguyen; A Grewal; H Erdjument-Bromage; P Tempst; C L Strickland; L Xiao; W C Van Voorhis; M H Gelb
Journal:  J Biol Chem       Date:  2000-07-21       Impact factor: 5.157

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.