PT  - JOURNAL ARTICLE
AU  - Sergei Maliartchouk
AU  - Yangbo Feng
AU  - Ljubica Ivanisevic
AU  - Thomas Debeir
AU  - A. Claudio Cuello
AU  - Kevin Burgess
AU  - H. Uri Saragovi
TI  - A Designed Peptidomimetic Agonistic Ligand of TrkA Nerve Growth Factor Receptors
DP  - 2000 Feb 01
TA  - Molecular Pharmacology
PG  - 385--391
VI  - 57
IP  - 2
4099  - http://molpharm.aspetjournals.org/content/57/2/385.short
4100  - http://molpharm.aspetjournals.org/content/57/2/385.full
SO  - Mol Pharmacol2000 Feb 01; 57
AB  - A proteolytically stable small molecule β-turn peptidomimetic, termed D3, was identified as an agonist of the TrkA neurotrophin receptor. D3 binds the Ig-like C2 region of the extracellular domain of TrkA, competes the binding of another TrkA agonist, affords selective trophic protection to TrkA-expressing cell lines and neuronal primary cultures, and induces the differentiation of primary neuronal cultures. These results indicate that a small β-turn peptidomimetic can activate a tyrosine kinase neurotrophin receptor that normally binds a relatively large protein ligand. Agents such as D3 that bind the extracellular domain of Trk receptors will be useful pharmacological agents to address disorders where Trk receptors play a role, by targeting populations selectively. The American Society for Pharmacology and Experimental Therapeutics