Fluorine and Rhenium Substituted Ghrelin Analogues as Potential Imaging Probes for the Growth Hormone Secretagogue Receptor
作者:Dina Rosita、Matthew A. DeWit、Leonard G. Luyt
DOI:10.1021/jm8014519
日期:2009.4.23
prepared containing rhenium, as a surrogate metal for technetium-99m, with a cyclopentadienylrhenium tricarbonyl being situated at the terminus of the residue-3 side chain, yielding compounds the best of which had a 35 nM IC50. This represents a rare case of incorporating rhenium into a peptide structure where the metal complex is required for biological activity. These fluorine and rhenium derivatives demonstrate
在努力创建针对生长激素促分泌素受体(GHSR)的成像探针的过程中,我们现在报告了通过修饰正辛酰基Ser-3侧链设计和合成含氟和rh的生长素释放肽类似物的过程。使用二氨基丙酸(Dpr)作为残基-3,设计了氟类似物,使氟原子位于脂族链的末端。制备了截短的ghrelin(1-5)和ghrelin(1-14)含氟类似物,其中最好的类似物具有用于GHSR的28 nM IC 50。还制备了Ghrelin(1-14)类似物,其中含有rh,作为m 99m的替代金属,三羰基环戊二烯基r位于残基3侧链的末端,产生的化合物中最好的是35 nM IC50。这代表了将rh掺入肽结构的罕见情况,其中金属配合物是生物活性所必需的。这些氟和rh衍生物表现出修饰ghrelin的Ser-3侧链的能力,以便为GHSR创建成像探针。
Ghrelin analogues
申请人:Luyt Leonard G.
公开号:US08623326B2
公开(公告)日:2014-01-07
Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.
提供了对疾病细胞中靶受体具有高亲和力的胃饥饿素类似物,以及利用这些类似物进行诊断和治疗的方法。
US8623326B2
申请人:——
公开号:US8623326B2
公开(公告)日:2014-01-07
[EN] NOVEL GHRELIN ANALOGUES<br/>[FR] NOUVEAUX ANALOGUES DE GHRÉLINE
申请人:UNIV WESTERN ONTARIO
公开号:WO2009140763A1
公开(公告)日:2009-11-26
Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.
NOVEL GHRELIN ANALOGUES
申请人:Luyt Leonard G.
公开号:US20110110855A1
公开(公告)日:2011-05-12
Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.