(Trp⁶³,Trp⁶⁴)-C3a(63-77)是补体3a的合成超级拮抗剂类似物,在所有测试的肽中表现出最大的生物效力。
编号:170251
CAS号:130154-64-2
单字母:H2N-WWGKKYRASKLGLAR-OH
(Trp⁶³,Trp⁶⁴)-C3a(63-77)是补体3a的合成超级拮抗剂类似物,在所有测试的肽中表现出最大的生物效力。该肽的活性是天然C3a的12-15倍。这种最佳效力是通过引入体积庞大的疏水基团如Trp-Trp获得的,该疏水基团与受体上的疏水位点的结合比与天然配体上的相应位点的结合更强。
(Trp⁶³,Trp⁶⁴)-C3a (63-77), synthetic superagonist analog of complement 3a, exhibited the greatest biological potency of all peptides tested. The peptide was 12-15 times more active than natural C3a. Such an optimal potency was obtained by introducing a bulky hydrophobic group such as Trp-Trp which binds more strongly to the hydrophobic site on the receptor than does the corresponding site on the natural ligand.
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10.1021/bi00229a003 | Designing synthetic superagonists of C3a anaphylatoxin | 下载 |
10.1038/nchembio.690 | GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis | 下载 |