Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin

ACS Medicinal Chemistry Letters

Volumn 8, Issue 3, 2017, Pages 321-326

  Metcalf, Brian ^a   Chuang, Chihyuan ^b   Dufu, Kobina ^a   Patel, Mira P ^a   Silva Garcia, Abel ^a   Johnson, Carl ^a   Lu, Qing ^b   Partridge, James R ^a   Patskovska, Larysa ^c   Patskovsky, Yury ^c   Almo, Steven C ^c   Jacobson, Matthew P ^d   Hua, Lan ^d   Xu, Qing ^a   Gwaltney, Stephen L ^a   Yee, Calvin ^a   Harris, Jason ^a   Morgan, Bradley P ^b   James, Joyce ^b   Xu, Donghong ^b   Hutchaleelaha, Athiwat ^a   Paulvannan, Kumar ^e   Oksenberg, Donna ^a   Li, Zhe ^a   more..

^a Global Blood Therapeutics Inc ^*  (United States)

^b Cytokinetics Inc   (United States)

^c ALBERT EINSTEIN COLLEGE OF MEDICINE   (United States)

^d UNIVERSITY OF CALIFORNIA   (United States)

^e Tandem Sciences Inc   (United States)

Author keywords

aldehyde; allosteric modulator; oxygen affinity; red blood cell partitioning; Schiff base formation; Sickle cell disease; sickle cell hemoglobin

Indexed keywords

CYTOCHROME P450; GBT 440; HEMATOLOGIC AGENT; HEMOGLOBIN; HEMOGLOBIN S; OXYGEN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG SYNTHESIS; ELIMINATION HALF-LIFE; ENZYME INHIBITION; ERYTHROCYTE; HAPLORHINI; IC50; IN VITRO STUDY; MICROSOME; NONHUMAN; OXYGEN AFFINITY; PHASE 3 CLINICAL TRIAL (TOPIC); POLYMERIZATION; PRIORITY JOURNAL; PROTEIN STABILITY; RAT; STOICHIOMETRY; STRUCTURE ACTIVITY RELATION;

EID: 85014916782     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.6b00491     Document Type: Article

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