P11 化学特性,用途語,生産方法
使用
P11 is a useful building block in the synthesis of various pharmaceuticals
酵素阻害剤
This potent PDZ motif-containing anti-angiogenic agent (FW = 720.78
g/mol; CAS 848644-86-0; Sequence: HSDVHK-NH2) targets the integrin
αvβ3-vitronectin interaction, blocking proliferation and inducing apoptosis in
human vascular endothelial cells (HUVECs). Arg-Gly-Asp (or RGD)
binding-site recognition by P11 is site-specific, showing a strong
antagonism against αvβ3-vitronectin interaction, IC50 = 26 nM. The
binding orientation of docked P11 in αvβ3 is similar to that for RGD,
suggesting a divalent metal-ion coordination is a common driving force for
the formation of both SDV·αvβ3 and RGD·αvβ3 complexes. P11 appears to
inhibit b-Fibroblast Growth Factor (or bFGF) -induced HUVEC
proliferation via mitogen-activated protein kinase kinase and extracellular-
signal regulated kinase inhibition as well as p53-mediated apoptosis related
with activation of caspases. (Note: Consisting of 80-90 amino-acids in
far-flung signaling proteins and binding to short C-terminal regions in
protein interaction partners, “PDZ” is an acronym that includes the first
letters of Post-synaptic density protein (PSD95), Drosophila Dlg1 tumor
suppressor, and Zonula occludens-1 protein (zo-1), the first proteins
discovered to share this domain.)
P11 上流と下流の製品情報
原材料
準備製品