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Interaction Network for CYSLTR2

CYSLTR2 Details

Related Pathways

Eicosanoid Signaling
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GPCR Pathway Map

Synonyms:2300001H05Rik, Cltr2, CYSLT2, CYSLT2 RECEPTOR, CYSLT2R, CYSLTR2, GPCR, HG57, hGPCR21, HPN321, KPG 011, PSEC0146

GPCR Pathway

G-protein coupled receptors (GPCR) are a large family of proteins that contain seven transmembrane domains. The extracellular N-terminal and exoloops create the interface for agonist interactions. The cytoplasmic C-terminal and cytoloops determine the binding to specific heterotrimeric G-proteins composed of alpha, beta and gamma subunits. GPCRs can associate into dimers and oligomers which enhances sensitivity and specificity of response. There are multiple genes for G-protein alpha, beta and gamma subunits leading to thousands of possible alpha:beta:gamma combinations. Both the Galpha and the Gbetagamma subunits have signaling roles.

G-protein Galpha subunits bind GDP/GTP. Galpha subunits belong to subfamilies such as Galphas; Galphai; Galphaq and Galpha12. Each subfamily has gene variants. Galphas (Gas) subunits are associated most often with the activation of adenylyl cyclase and/or calcium ion channels whereas the Galphai (Gai) subunits are typically adenylyl cyclase and calcium ion channel inhibitors. Galphaq (Gaq) family variants; aq, a11, a14, a15, a16 are generally associated with the activation of phospholipase C. Galpha12/13 subunits have been linked to the activation of specific Rho guanine nucleotide exchange factors (RhoGEF); LARG, p115 and PDZ. These GEFs activate the Rho/Rock pathway which is linked to cell proliferation, differentiation, migration and survival. Galpha12/13 is also linked to the induction of apoptosis via activation of JNK through two separate pathways involving ASK1 or MEKK-1 which are MAP3Ks.

Gbetagamma (Gbg) dimers also have critical roles in the regulation of GPCR linked effectors. Gbetagamma subunits mediate formation of Shc-Src complexes leading to activation of the Ras-Raf1-MEK-ERK pathway. They also affect PI3Kgamma, protein kinase D (PKD), calcium and potassium channels, adenylyl cyclase 2 (AC-2), phospholipase C-beta2 (PLCbeta2), and beta-adrenergic receptor kinase (betaARKinase) activation.


References:

  1. Filizola M. and Weinstein H. (2005) The structure and dynamics of GPCR oligomers: a new focus in models of cell-signaling mechanisms and drug design. Curr. Opin. Drug Discov. Devel. 8, 577-584.

  2. Luttrell L. M. (2006) Transmembrane signaling by G protein-coupled receptors. Methods Mol. Biol. 332, 3-49.

  3. Natarajan K. and Berk B.C. (2006) Crosstalk coregulation mechanisms of G protein-coupled receptors and receptor tyrosine kinases. Methods Mol. Biol. 332, 51-77.
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Content for this page is provided by Dennis R. Conrad, Ph.D., a Life Science industry consultant with over 25 years of experience in the formulation and optimization of cell culture media. Dr. Conrad's email address is biomediaexpert@earthlink.net