title: Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design.
abstract: A matter of common sense: a common recognition motif consisting of a negatively charged group five to six bonds away (red) from the (thio)ester functionality (green) and a positively charged tail group ten to twelve bonds away (blue) was identified in two native acyl protein thioesterase 1 (APT1) substrates. This similarity led to the design of potent inhibitors of the Ras-depalmitoylating enzyme APT1.
authors: Max-Planck-Institut für molekulare Physiologie, Abt. Chemische Biologie, Dortmund, Germany.
authors: Christian
authors: C
authors: Hedberg
authors: Frank J
authors: FJ
authors: Dekker
authors: Marion
authors: M
authors: Rusch
authors: Steffen
authors: S
authors: Renner
authors: Stefan
authors: S
authors: Wetzel
authors: Nachiket
authors: N
authors: Vartak
authors: Claas
authors: C
authors: Gerding-Reimers
authors: Robin S
authors: RS
authors: Bon
authors: Philippe I H
authors: PI
authors: Bastiaens
authors: Herbert
authors: H
authors: Waldmann
mesh_terms: D000818:Animals; D002460:Cell Line; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013869:Thiolester Hydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020663:ras Guanine Nucleotide Exchange Factors / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D007783:Lactones; D020663:ras Guanine Nucleotide Exchange Factors; C402226:LYPLA1 protein, human; D013869:Thiolester Hydrolases