Psoromic acid is a selective and covalent rab-prenylation inhibitor targeting autoinhibited rabggtase

Journal of the American Chemical Society

Volumn 134, Issue 17, 2012, Pages 7384-7391

  Deraeve, Céline ^a,g   Guo, Zhong ^a,d   Bon, Robin S ^a,f   Blankenfeldt, Wulf ^a,e   DiLucrezia, Raffaella ^c   Wolf, Alexander ^c   Menninger, Sascha ^c   Stigter, E Anouk ^a   Wetzel, Stefan ^a   Choidas, Axel ^c   Alexandrov, Kirill ^a,d   Waldmann, Herbert ^a,b   Goody, Roger S ^a   Wu, Yao Wen ^a  

^a MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY   (Germany)

^b TU DORTMUND UNIVERSITY   (Germany)

^c Lead Discovery Center GmbH   (Germany)

^d UNIVERSITY OF QUEENSLAND   (Australia)

^e UNIVERSITY OF BAYREUTH   (Germany)

^f UNIVERSITY OF LEEDS   (United Kingdom)

^g LCC LABORATOIRE DE CHIMIE DE COORDINATION   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVE SITE; COVALENT BINDING; FUNCTIONAL SIMILARITY; HYDROPHOBIC INTERACTIONS; IN-VIVO; ISOPRENOIDS; N-TERMINALS; NATURAL PRODUCTS; PRENYLATION; RAB GTPASES; SELECTIVE INHIBITORS; STRUCTURE ACTIVITY RELATIONSHIPS; VESICULAR TRANSPORT; ZINC IONS;

ALDEHYDES; DISEASES; LIPIDS; REACTION RATES;

PROTEINS;

ENZYME INHIBITOR; NE 10790; PSOROMIC ACID; RAB GERANYLGERANYL TRANSFERASE; RAB GERANYLGERANYL TRANSFERASE ALPHA SUBUNIT; RAB GERANYLGERANYL TRANSFERASE BETA SUBUNIT; TRANSFERASE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; PROTEIN PRENYLATION; STRUCTURE ACTIVITY RELATION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; BENZOXEPINS; CARBOXYLIC ACIDS; CELL LINE; ENZYME INHIBITORS; HUMANS; MODELS, MOLECULAR; PROTEIN PRENYLATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84860792501     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja211305j     Document Type: Article

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