Bivalent diketopiperazine-based tropomysin receptor kinase C (TrkC) antagonists.
نویسندگان
چکیده
Bivalent molecules containing two beta-turn mimics with side chains that correspond to hot-spots on the neurotrophin NT-3 were prepared. Binding assays showed the mimetics to be selective TrkC ligands, and biological assays showed one mimetic to be an antagonist of the TrkC receptor.
منابع مشابه
Combinatorial Assembly of Small Molecules into Bivalent Antagonists of TrkC or TrkA Receptors
A library of peptidomimetics was assembled combinatorially into dimers on a triazine-based core. The pharmacophore corresponds to β-turns of the neurotrophin polypeptides neurotrophin-3 (NT-3), nerve growth factor (NGF), or brain-derived neurotrophic factor (BDNF). These are the natural ligands for TrkC, TrkA, and TrkB receptors, respectively. The linker length and the side-chain orientation of...
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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 53 13 شماره
صفحات -
تاریخ انتشار 2010