Design and identification of selective HER-2 sheddase inhibitors via P1′ manipulation and unconventional P2′ perturbations to induce a molecular metamorphosis

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 1, 2008, Pages 159-163

  Yao, Wenqing ^a   Zhuo, Jincong ^a   Burns, David M ^a   Li, Yun Long ^a   Qian, Ding Quan ^a   Zhang, Colin ^a   He, Chunhong ^a   Xu, Meizhong ^a   Shi, Eric ^a   Li, Yanlong ^a   Marando, Cindy A ^a   Covington, Maryanne B ^a   Yang, Gengjie ^a   Liu, Xiangdong ^a   Pan, Max ^a   Fridman, Jordan S ^a   Scherle, Peggy ^a   Wasserman, Zelda R ^a   Hollis, Gregory ^a   Vaddi, Kris ^a   Yeleswaram, Swamy ^a   Newton, Robert ^a   Friedman, Steve ^a   Metcalf, Brian ^a   more..

^a Drug Metabolism Pharmacokinetics Clinical Pharmacology   (United States)

Author keywords

ADAM 10; Global conformation; HER 2 sheddase; Hydroxamic acid; Metalloprotease; MMP; P1 group; P2 group; Piperidine; SAR

Indexed keywords

7 [(HYDROXYAMINO)CARBONYL] 6 CARBOXAMIDE 5 AZASPIRO[2.5]OCTANE 5 CARBOXYLIC ACID; ADAM 10 PROTEIN; ADAM PROTEIN; EPIDERMAL GROWTH FACTOR RECEPTOR 2; GELATINASE A; GELATINASE B; HER 2 SHEDDASE; INCB 3619; INTERSTITIAL COLLAGENASE; MATRIX METALLOPROTEINASE INHIBITOR; STROMELYSIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BREAST CANCER; CANCER CELL; CHEMICAL STRUCTURE; DRUG POTENCY; DRUG SELECTIVITY; ENZYME BINDING; ENZYME INHIBITION; HALF LIFE TIME; LUNG NON SMALL CELL CANCER; MOUSE; NONHUMAN; OVARY CANCER; STRUCTURE ACTIVITY RELATION;

ADAM PROTEINS; AMIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; AZA COMPOUNDS; DRUG DESIGN; HYDROXAMIC ACIDS; MEMBRANE PROTEINS; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, ERBB-2; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 37549051746     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.10.108     Document Type: Article

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