Exploring the chiral space within the active site of α-thrombin with a constrained mimic of D-Phe-Pro-Arg - Design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex

Bioorganic and Medicinal Chemistry Letters

Volumn 10, Issue 3, 2000, Pages 243-247

  Hanessian, Stephen ^a   Balaux, Elise ^a   Musil, Djorde ^b   Olsson, Lise Lotte ^c   Nilsson, Ingemar ^b  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b ASTRAZENECA R AND D   (Sweden)

^c UNIVERSITY OF GOTHENBURG   (Sweden)

Author keywords

Enzyme inhibitor complex; Thrombin inhibitor; X ray

Indexed keywords

DEXTRO PHENYLALANYLPROLYLARGINYL CHLOROMETHYL KETONE; DRUG ANALOG; INDOLIZIDINONE; THROMBIN; TRYPSIN; UNCLASSIFIED DRUG;

ARTICLE; CHIRALITY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG STRUCTURE; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITOR COMPLEX; INHIBITION KINETICS; MOLECULAR MIMICRY; PARTIAL DRUG SYNTHESIS; STRUCTURE ANALYSIS; X RAY ANALYSIS;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; MODELS, MOLECULAR; MOLECULAR MIMICRY; MOLECULAR PROBES; MOLECULAR STRUCTURE; OLIGOPEPTIDES; STEREOISOMERISM; THROMBIN;

EID: 0034615130     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00669-1     Document Type: Article

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