Last update 01 Nov 2024

GFRA2

Last update 01 Nov 2024

Basic Info

Synonyms

GDNF family receptor alpha 2, GDNF family receptor alpha-2, GDNF receptor alpha-2

+ [14]

Introduction

Receptor for neurturin. Mediates the NRTN-induced autophosphorylation and activation of the RET receptor. Also able to mediate GDNF signaling through the RET tyrosine kinase receptor. Participates in NRTN-induced 'Ser-727' phosphorylation of STAT3.

Drugs associated with GFRA2

GFRα2/3 inhibitors(Cerevel)

Target

GFRA2 x GFRα3

Mechanism

GFRA2 antagonists [+1]

Active Org.

Cerevel Therapeutics LLC

Originator Org.

Cerevel Therapeutics LLC

Active Indication

Pain [+1]

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with GFRA2

100 Translational Medicine associated with GFRA2

0 Patents (Medical) associated with GFRA2

134

Literatures (Medical) associated with GFRA2

01 Sep 2024·Bioorganic & Medicinal Chemistry Letters

Discovery of the first selective, small-molecule GFRα2/3 inhibitors through DNA-encoded library technology

Article

Author: Missig, Galen ; Ho, Tammy Szu-Yu ; Nguyen, Hanh Nho ; Johnson, Shea L ; Choi-Sledeski, Yong Mi ; Lim, Jongwon ; Pin, Sokhom ; Toh, May Fern ; Gray, David ; Gupta, Kushali ; Ouk, Kosalvisal ; Wang, Minghua ; Stone, David J ; Barberis, Claude ; Zhang, Hongjun

Studies have shown that disrupting the formation of the ligand-RET-GFRα complex could be an effective way of treating pain and itch. Compared to traditional high-throughput screens, DNA encoded libraries (DELs) have distinguished themselves as a powerful technology for hit identification in recent years. The present work demonstrates the use of DEL technology identifying compound 16 as the first GFRa2/GFRa3 small molecule inhibitor (0.1/0.2 μM respectively) selective over RET. This molecule represents an opportunity to advance the development of small-molecule inhibitors targeting the GFRα-RET interface for the treatment of pain and itch.

01 Nov 2023·Cell Reports

GFRA2 Identifies Cardiac Progenitors and Mediates Cardiomyocyte Differentiation in a RET-Independent Signaling Pathway

Author: Yashiro, Kenta ; Miller, Duncan ; Sawa, Yoshiki ; Hadjantonakis, Anna-Katerina ; Dunkel, Leo ; Sakata, Yasushi ; Nowotschin, Sonja ; Sasaki, Hiroshi ; Shiraishi, Manabu ; Saba, Rie ; Suzuki, Ken ; Poliandri, Ariel ; Kokkinopoulos, Ioannis ; Ozono, Keiichi ; Kogaki, Shigetoyo ; Ishida, Hidekazu ; Harmer, Stephen ; Tinker, Andrew ; Hashimoto, Masakazu ; Yamaguchi, Osamu ; Ruchaya, Prashant

01 Oct 2023·Fish & shellfish immunology

Mechanisms underlying probiotic effects on neurotransmission and stress resilience in fish via transcriptomic profiling.

Article

Author: Lee, Ju-Yeop ; Kang, Hyoyeong ; Lee, Yoonhang ; Nguyen, Thanh Luan ; Sohn, Min-Young ; Kang, Yu-Ra ; Kim, Do-Hyung ; Park, Jiyeon ; Kim, Ahran ; Park, Chan-Il ; Roh, HyeongJin

In recent years, studies have highlighted the significant impact of probiotic treatment on the central nervous system (brain) and stress regulation through the microbiota-gut-brain axis, yet there have been limited knowledge on this axis in fish. Therefore, this study aimed to enhance the current understanding of the mechanisms underlying probiotic effects on neurotransmission and stress alleviation in fish through transcriptomic profiling. In this study, olive flounders (Paralichthys olivaceus) were subjected to two trial setups: a 1-month lab-scale trial and a 6-month field-scale trial, with and without the probiotic strain Lactococcus lactis WFLU12. RNA-Seq analysis was performed using liver samples collected from fish at one-month post-feeding (mpf) in both trials. Additionally, fish growth was monitored monthly, and serological parameters were measured at one mpf in the field-scale experiment. The results of the lab-scale trial showed that probiotic administration significantly upregulated genes related to neurotransmission, such as htr3a, mao, ddc, ntsr1, and gfra2. These findings highlight the impact of probiotics on modulating neurotransmission via the microbiota-gut-brain axis. In the field-scale experiment, fish growth was significantly promoted and the sera levels of AST, LDH, and cortisol were significantly higher in the control group compared to the probiotics group. Furthermore, genes involved in stress responses (e.g. hsp70, hsp90B1, hspE1, prdx1, and gss) and transcriptional regulators (e.g. fos, dusp1, and dusp2) exhibited significant upregulation in the control group compared to the probiotics group, indicating that probiotic administration can alleviate stress levels in fish. Overall, this study provides valuable insights into the mechanisms underlying the beneficial effects of probiotics in fish, specifically regarding their impact on neurotransmission and stress alleviation.

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GFRA2

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