Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept

Journal of Medicinal Chemistry

Volumn 57, Issue 2, 2014, Pages 309-324

  Ashton, Kate S ^a   Andrews, Kristin L ^a   Bryan, Marion C ^a,b   Chen, Jie ^a   Chen, Kui ^a   Chen, Michelle ^a   Chmait, Samer ^a   Croghan, Michael ^a   Cupples, Rod ^a   Fotsch, Christopher ^a   Helmering, Joan ^a   Jordan, Steve R ^a   Kurzeja, Robert J M ^a   Michelsen, Klaus ^a   Pennington, Lewis D ^a   Poon, Steve F ^a   Sivits, Glenn ^a   Van, Gwyneth ^a   Vonderfecht, Steve L ^a,c   Wahl, Robert C ^a   Zhang, Jiandong ^a,d   Lloyd, David J ^a   Hale, Clarence ^a   St Jean, David J ^a   more..

^a AMGEN INC   (United States)

^b GENENTECH INC   (United States)

^c CITY OF HOPE NATIONAL MEDICAL CENTER   (United States)

^d JD Consulting   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,1,1 TRIFLUORO 2 [4 [2 (TETRAHYDRO 2H PYRAN 4 YLMETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1 TRIFLUORO 2 [4 [2 [(3 METHYL 4 MORPHOLINYL)METHYL] 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 (1 METHYLETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 (3 METHYL 4 MORPHOLINYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 (4 MORPHOLINYLMETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 (4 PYRIDINYLMETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 (TETRAHYDRO 2H PYRAN 4 YLMETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 METHYL 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [2 PHENYL 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [3 METHYL 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 1,1,1,3,3,3 HEXAFLUORO 2 [4 [4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 2 PROPANOL; 2 [4 [2 (CYCLOHEXYLMETHYL) 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL]1,1,1,3,3,3 HEXAFLUORO 2 PROPANOL; 2 [4 [2 BENZYL 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 1,1,1,3,3,3 HEXAFLUORO 2 PROPANOL; 2 [4 [2 ETHYL 4 (2 THIOPHENYLSULFONYL) 1 PIPERAZINYL]PHENYL] 1,1,1,3,3,3 HEXAFLUORO 2 PROPANOL; 2 [[4 (2 THIOPHENYLSULFONYL) 1 [4 [2,2,2 TRIFLUORO 1 HYDROXY 1(TRIFLUOROMETHYL)ETHYL]PHENYL] 2 PIPERAZINYL]METHYL]PHENOL; 3 [[4 (2 THIOPHENYLSULFONYL) 1 [4 [2,2,2 TRIFLUORO 1 HYDROXY 1 (TRIFLUOROMETHYL)ETHYL]PHENYL] 2 PIPERAZINYL]METHYL]PHENOL; 4 [[4 (2 THIOPHENYLSULFONYL) 1 [4 [2,2,2 TRIFLUORO 1 HYDROXY 1 (TRIFLUOROMETHYL)ETHYL]PHENYL] 2 PIPERAZINYL]METHYL]PHENOL; AMG 1694; ANTIDIABETIC AGENT; ENZYME ACTIVATOR; GLUCOKINASE; GLUCOKINASE REGULATORY PROTEIN; GLUCOSE; METFORMIN; MORPHOLINE DERIVATIVE; PIPERAZINE DERIVATIVE; REGULATOR PROTEIN; SULFONAMIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG IDENTIFICATION; DRUG POTENCY; ENZYME ACTIVITY; HIGH THROUGHPUT SCREENING; HYPERGLYCEMIA; IC 50; IN VIVO STUDY; NONHUMAN; PROTEIN PROTEIN INTERACTION; PROTEIN TARGETING; RAT; ZUCKER DIABETIC FATTY RAT;

ANIMALS; BINDING SITES; CARRIER PROTEINS; CRYSTALLOGRAPHY, X-RAY; GLUCOKINASE; HEPATOCYTES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; HYPOGLYCEMIA; HYPOGLYCEMIC AGENTS; PIPERAZINES; PROTEIN CONFORMATION; PROTEIN TRANSPORT; RATS; RATS, ZUCKER; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84893026568     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4016735     Document Type: Article

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