LeSauteur L, Maliartchouk S, Le Jeune H, Quirion R, Saragovi H U
Department of Pharmacology and Therapeutics, McGill University, Montréal, Québec, Canada.
J Neurosci. 1996 Feb 15;16(4):1308-16. doi: 10.1523/JNEUROSCI.16-04-01308.1996.
Monoclonal antibody (mAb) 5C3 directed against human p140 TrkA is a structural and functional mimic of nerve growth factor (NGF) and an artificial receptor agonist. mAb 5C3 binds in the NGF-docking site and, like NGF, it promotes TrkA internalization, TrkA and phosphatidylinositol-3 kinase tyrosine phosphorylation, and increased transformation of TrkA-expressing fibroblasts. More important, mAb 5C3 protects human TrkA-expressing cells from apoptotic death in serum-free media. Interestingly, agonistic activity is observed with monomeric F(ab) 5C3 fragments. mAb 5C3 (Kd approximately 2 nM) was used to study features of ligand binding by TrkA and the distribution of TrkA protein in normal human brain.
针对人p140 TrkA的单克隆抗体（mAb）5C3是神经生长因子（NGF）的结构和功能模拟物，也是一种人工受体激动剂。mAb 5C3结合在NGF对接位点，与NGF一样，它促进TrkA内化、TrkA和磷脂酰肌醇-3激酶酪氨酸磷酸化，并增强表达TrkA的成纤维细胞的转化。更重要的是，mAb 5C3可保护无血清培养基中表达人TrkA的细胞免于凋亡死亡。有趣的是，单体F(ab) 5C3片段也具有激动活性。mAb 5C3（解离常数约为2 nM）用于研究TrkA的配体结合特征以及TrkA蛋白在正常人类大脑中的分布。
