Development of Highly Potent Inhibitors of the Ras??Targeting Human Acyl Protein Thioesterases Based on Substrate Similarity Design

…, S Wetzel, N Vartak, C Gerding??Reimers…

Index: Hedberg, Christian; Dekker, Frank J.; Rusch, Marion; Renner, Steffen; Wetzel, Stefan; Vartak, Nachiket; Gerding-Reimers, Claas; Bon, Robin S.; Bastiaens, Philippe I. H.; Waldmann, Herbert Angewandte Chemie - International Edition, 2011 , vol. 50, # 42 p. 9832 - 9837

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Citation Number: 40

Abstract

Signal-transducing Ras guanine nucleotide binding proteins (GTPases) play important roles in decisive cellular processes, such as growth, division, and differentiation.[1, 2] Mutations in the S-farnesylated and S-palmitoylated H-and N-Ras isoforms result in oncogenic activation, which frequently occurs in melanoma, leukemia, and cancers of the bladder, liver, and kidney.[3]