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XIB4035, a Novel Nonpeptidyl Small Molecule Agonist for GFRalpha-1

XIB4035, a Novel Nonpeptidyl Small Molecule Agonist for GFRalpha-1

Kimiko Tokugawa, Kyoko Yamamoto, Mariko Nishiguchi, Takumi Sekine, Masahiko Sakai, Tomokazu Ueki, Shigeyuki Chaki, Shigeru Okuyama

Neurochem Int. 2003 Jan;42(1):81-6.

PMID: 12441171

Abstract:

We investigated the agonistic activities of N(4)-(7-chloro-2-[(E)-2-(2-chloro-phenyl)-vinyl]-quinolin-4-yl)-N(1),N(1)-diethyl-pentane-1,4-diamine (XIB4035), at the glial cell line-derived neurotrophic factor (GDNF) family receptoralpha-1(GFRalpha-1) in Neuro-2A cells, a mouse neuroblastoma cell line which is a suitable model for investigating functions mediated through GFRalpha-1. XIB4035 concentration-dependently inhibited [(125)I]GDNF binding in Neuro-2A cells with an IC(50) of 10.4 microM. GDNF induced autophosphorylation of Ret protein, and promoted neurite outgrowth in Neuro-2A cells. XIB4035, like GDNF, induced Ret autophosphorylation in the Neuro-2A cells. Moreover, XIB4035 promoted neurite outgrowth in a concentration-dependent manner. These results show that XIB4035 may act as an agonist at GFRalpha-1 receptor complex, and mimic neurotrophic effects of GDNF in Neuro-2A cells. This is an interesting finding showing that a nonpeptidyl small molecule is capable of inducing activation of a receptor that normally bind a relatively large protein ligand such as GDNF.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP529507844	XIB4035		529507-84-4	Price

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