Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site

Journal of Medicinal Chemistry

Volumn 57, Issue 12, 2014, Pages 5435-5448

  Zimmermann, Gunther ^a,b   Schultz Fademrecht, Carsten ^c   Küchler, Philipp ^a,b   Murarka, Sandip ^a   Ismail, Shehab ^a,d   Triola, Gemma ^a,e   Nussbaumer, Peter ^c   Wittinghofer, Alfred ^a   Waldmann, Herbert ^a,b  

^a MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY   (Germany)

^b TU DORTMUND UNIVERSITY   (Germany)

^c Lead Discovery Center GmbH   (Germany)

^d BEATSON INSTITUTE FOR CANCER RESEARCH   (United Kingdom)

^e INSTITUTE OF ADVANCED CHEMISTRY OF CATALONIA IQAC CSIC   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

BENZIMIDAZOLE; BENZIMIDAZOLE INHIBITOR; BINDING PROTEIN; GUANOSINE TRIPHOSPHATASE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CELL LYSATE; CHEMICAL REACTION KINETICS; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG TARGETING; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION;

BENZIMIDAZOLES; BINDING SITES; CELL LINE, TUMOR; COMPUTER SIMULATION; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 6; DRUG DESIGN; ESTERS; ETHERS; HEPTANOIC ACIDS; HUMANS; KINETICS; MODELS, MOLECULAR; PROTEIN PRENYLATION; PYRROLES; RAS PROTEINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THERMODYNAMICS;

EID: 84903526984     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500632s     Document Type: Article

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