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排序方式: 共有78条查询结果,搜索用时 15 毫秒
31.
Bruce J. Melancon Michael S. Poslusney Patrick R. Gentry James C. Tarr Douglas J. Sheffler Margrith E. Mattmann Thomas M. Bridges Thomas J. Utley J. Scott Daniels Colleen M. Niswender P. Jeffrey Conn Craig W. Lindsley Michael R. Wood 《Bioorganic & medicinal chemistry letters》2013,23(2):412-416
This Letter describes the continued optimization of an MLPCN probe molecule (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M1 PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M1 receptor was also maintained. 相似文献
32.
Isolation and characterization of a folate receptor from human placenta 总被引:13,自引:0,他引:13
A C Antony C Utley K C Van Horne J F Kolhouse 《The Journal of biological chemistry》1981,256(18):9684-9692
While folate binding proteins have been described in serum and a variety of tissues, the function of these proteins is unknown. A particulate folate binding protein from human placenta has been isolated and characterized following solubilization with Triton X-100. The protein was purified 61,000-fold using affinity chromatography on pteroylglutamic acid-Sepharose as the major purification step. On sodium dodecyl sulfate-polyacrylamide gel electrophoresis the purified protein gave a single band with a Mr = 38,500. Stoichiometry of binding indicated that 1 mol of folate was bound per mol of protein. The protein was a glycoprotein that contained 12% carbohydrate. Antiserum was raised in a rabbit, and on immunodiffusion, gave a single precipitin line with the purified placental folate binding protein. Immunoprecipitation studies using this antiserum indicated that the purified placental folate binding protein shared antigenic determinants with both the large Mr and small Mr folate binding proteins from human milk. Immunofluorescent studies with this antiserum and human erythrocytes revealed the presence of an immunologically similar protein on the plasma membrane of these cells suggesting that this protein may function as a folate receptor. 相似文献
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Melancon BJ Lamers AP Bridges TM Sulikowski GA Utley TJ Sheffler DJ Noetzel MJ Morrison RD Scott Daniels J Niswender CM Jones CK Conn PJ Lindsley CW Wood MR 《Bioorganic & medicinal chemistry letters》2012,22(2):1044-1048
This Letter describes the continued optimization of an MLPCN probe molecule (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at a more highly M(1)-selective antagonist, compound 13l (VU0415248). Muscarinic subtype selectivity across all five human and rat receptors for 13l, along with rat selectivity for the lead compound (ML012), is presented. 相似文献