Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity

Journal of Medicinal Chemistry

Volumn 48, Issue 24, 2005, Pages 7535-7543

  Falgueyret, Jean Pierre ^a   Desmarais, Sylvie ^a   Oballa, Renata ^a   Black, W Cameron ^a   Cromlish, Wanda ^a   Khougaz, Karine ^a   Lamontagne, Sonia ^a   Massé, Frederic ^a   Riendeau, Denis ^a   Toulmond, Sylvie ^a   Percival, M David ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

BALICATIB; CATHEPSIN B; CATHEPSIN K; CATHEPSIN K INHIBITOR; CATHEPSIN L; CATHEPSIN S; CRA 013783; L 006235; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTIGEN PRESENTATION; ARTICLE; CELL ASSAY; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; ENDOSOME; ENZYME PURIFICATION; HUMAN; HUMAN CELL; LYSOSOME; NONHUMAN; OSTEOLYSIS; OSTEOPOROSIS; RAT;

ANIMALS; ANTIGEN PRESENTATION; AUTORADIOGRAPHY; BENZAMIDES; BONE DENSITY CONSERVATION AGENTS; CATHEPSIN B; CATHEPSINS; CELL LINE; CYSTEINE ENDOPEPTIDASES; FEMALE; HUMANS; LYSOSOMES; MICE; MICE, INBRED C57BL; MORPHOLINES; PIPERAZINES; RABBITS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; TISSUE DISTRIBUTION;

EID: 28144452675     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0504961     Document Type: Article

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