[EN] INHIBITORS OF PRENYL-PROTEIN TRANSFERASE<br/>[FR] INHIBITEURS DE LA PRENYL-PROTEINE TRANSFERASE
申请人:MERCK & CO INC
公开号:WO2001017992A1
公开(公告)日:2001-03-15
The present invention is directed to compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or alkycarboxylate group to provide said 4-substituted imidazole 2-one or thione.
Specific Force Deficit in Skeletal Muscles of Old Rats Is Partially Explained by the Existence of Denervated Muscle Fibers
作者:M. G. Urbanchek、E. B. Picken、L. K. Kalliainen、W. M. Kuzon
DOI:10.1093/gerona/56.5.b191
日期:2001.5.1
We tested the hypothesis that denervated muscle fibers account for part of the specific force (sF(0)) deficit observed in muscles from old adult (OA) mammals, Whole muscle force (F-0) was quantified for extensor digitorum longus (EDL) muscles of OA and young adult (YA) rats. EDL muscle sF(0) was calculated by dividing F-0 by either total muscle fiber cross-sectional area (CSA) or by innervated fiber CSA. Innervated fiber CSA was estimated from EDL muscle cross sections labeled for neural cell adhesion molecules, whose presence is a marker for muscle fiber denervation. EDL muscles from OA rats contained significantly more denervated fibers than muscles from YA rats (5.6% vs 1.1% of total CSA), When compared with YA muscle, oil muscle demonstrated deficits of 34.1% for F-0, 28.3% for sF(0), and 24.9 % for sF(0) calculated by using innervated CSA as the denominator, Denervated muscle fibers accounted for 11.3% of the specific force difference between normal YA and OA skeletal muscle, Other mechanisms in addition to denervation account for the majority of the sF(0) deficit with aging.
Lawson, Journal of the Chemical Society, 1957, p. 1443