Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

Nature Structural and Molecular Biology

Volumn 25, Issue 4, 2018, Pages 333-340

  Jackson, Scott M ^a   Manolaridis, Ioannis ^a   Kowal, Julia ^a   Zechner, Melanie ^a   Taylor, Nicholas M I ^b,d   Bause, Manuel ^c   Bauer, Stefanie ^c   Bartholomaeus, Ruben ^a   Bernhardt, Guenther ^c   Koenig, Burkhard ^c   Buschauer, Armin ^c   Stahlberg, Henning ^b   Altmann, Karl Heinz ^a   Locher, Kaspar P ^a  

^a ETH ZURICH   (Switzerland)

^b UNIVERSITY OF BASEL   (Switzerland)

^c UNIVERSITY OF REGENSBURG   (Germany)

^d University of Copenhagen   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,3,4,6,7,12,12A OCTAHYDRO 6 ISOBUTYL 9 METHOXY 1,4 DIOXOPYRAZINO[1',2':1,6]PYRIDO[3,4 B]INDOLE 3 PROPANOIC ACID TERT BUTYL ESTER; ADENOSINE TRIPHOSPHATASE INHIBITOR; ADENOSINE TRIPHOSPHATE; BREAST CANCER RESISTANCE PROTEIN; CHOLESTEROL; IMMUNOGLOBULIN F(AB) FRAGMENT; MB 136; MZ 29; PHOSPHOLIPID; TARIQUIDAR; UNCLASSIFIED DRUG; 3-(6-ISOBUTYL-9-METHOXY-1,4-DIOXO-1,2,3,4,6,7,12,12A-OCTAHYDROPYRAZINO(1',2'-1,6)PYRIDO(3,4-B)INDOL-3-YL)PROPIONIC ACID TERT-BUTYL ESTER; ABCG2 PROTEIN, HUMAN; FUSED HETEROCYCLIC RINGS; INDOLE DERIVATIVE; LIPID; PIPERAZINEDIONE; PROTEIN BINDING; QUINOLINE DERIVATIVE; TRYPTOQUIVALINE; TUMOR PROTEIN;

ARTICLE; BINDING AFFINITY; CHEMICAL MODIFICATION; CONFORMATIONAL TRANSITION; CRYOELECTRON MICROSCOPY; DRUG PROTEIN BINDING; DRUG SYNTHESIS; HYDROLYSIS; IN VITRO STUDY; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN STRUCTURE; STOICHIOMETRY; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DESIGN; DRUG SCREENING; ENZYME SPECIFICITY; HUMAN; KINETICS; MULTIDRUG RESISTANCE; PROTEIN MULTIMERIZATION;

ADENOSINE TRIPHOSPHATE; ATP BINDING CASSETTE TRANSPORTER, SUBFAMILY G, MEMBER 2; BINDING SITES; CHOLESTEROL; CRYOELECTRON MICROSCOPY; DIKETOPIPERAZINES; DRUG DESIGN; DRUG RESISTANCE, MULTIPLE; DRUG SCREENING ASSAYS, ANTITUMOR; HETEROCYCLIC COMPOUNDS, 4 OR MORE RINGS; HUMANS; HYDROLYSIS; INDOLES; KINETICS; LIPIDS; MOLECULAR STRUCTURE; NEOPLASM PROTEINS; PHOSPHOLIPIDS; PROTEIN BINDING; PROTEIN MULTIMERIZATION; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 85044717562     PISSN: 15459993     EISSN: 15459985     Source Type: Journal    
DOI: 10.1038/s41594-018-0049-1     Document Type: Article

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