Chemokine Receptor
Chemokine receptors are GPCRs—integral membrane proteins composed of seven transmembrane helical segments. Different subsets of leukocytes express different arrays of chemokine receptors enabling them to respond to the appropriate ligands. Upon binding to their cognate chemokine ligands, the receptors undergo conformational changes giving rise to activation of intracellular effectors (G proteins or β-arrestins), initiation of signal transduction pathways and, ultimately, cellular responses. Mammalian genomes each encode approximately 20 chemokine receptors. Because the receptors were discovered after the chemokines and most of them are selective for members of one chemokine subfamily, they are classified according to the subfamily of chemokines to which most of their ligands belong. Thus, receptors are named using the prefixes CCR, CXCR, CX3CR, and XCR followed by an identifying number.
Upon activation, GPCRs function as guanine nucleotide exchange factors (GEFs), which allows the α subunit of the heterotrimeric G protein to transition from inactive (GDP-bound) to active (GTP-bound) and to dissociate from the βγ subunits. Gβγ can regulate ion channels and is also involved in phosphorylation of the extracellular signal-regulated kinases (ERK 1/2) via the protein kinase C/protein kinase A pathway. The arrestin family also includes four subtypes. Arrestin-1 (visual arrestin) and arrestin-4 (cone arrestin) are located exclusively in retinal rods and cones. Arrestin-2 (or β-arrestin 1) and arrestin-3 (or β-arrestin 2) are non-visual arrestins that are expressed in numerous cell types. G protein-independent β-arrestin mediated signaling is less well characterized, but it has been identified using GPCR mutants unable to bind to G proteins, which are still able to signal through the ERK phosphorylation pathway.
References
1.Stone MJ,et al. Int J Mol Sci. 2017 Feb 7;18(2). pii: E342.
Upon activation, GPCRs function as guanine nucleotide exchange factors (GEFs), which allows the α subunit of the heterotrimeric G protein to transition from inactive (GDP-bound) to active (GTP-bound) and to dissociate from the βγ subunits. Gβγ can regulate ion channels and is also involved in phosphorylation of the extracellular signal-regulated kinases (ERK 1/2) via the protein kinase C/protein kinase A pathway. The arrestin family also includes four subtypes. Arrestin-1 (visual arrestin) and arrestin-4 (cone arrestin) are located exclusively in retinal rods and cones. Arrestin-2 (or β-arrestin 1) and arrestin-3 (or β-arrestin 2) are non-visual arrestins that are expressed in numerous cell types. G protein-independent β-arrestin mediated signaling is less well characterized, but it has been identified using GPCR mutants unable to bind to G proteins, which are still able to signal through the ERK phosphorylation pathway.
References
1.Stone MJ,et al. Int J Mol Sci. 2017 Feb 7;18(2). pii: E342.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
Chemokine Receptor
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AZ 13381758
产品货号 : M17040
cas no: ——
一种有效的小分子 CXCR2 抑制剂,对 mCXCR2 和 hCXCR2 的 IC50 分别为 26 nM 和 30 nM。 -
CCR6 inhibitor 35
产品货号 : M17039
cas no: ——
CCR6抑制剂35是一种有效的选择性CCR6抑制剂,IC50为6.0 nM (hCCR6)。 -
Elubrixin tosylate
产品货号 : M16860
cas no: 960495-43-6
Elubrixin (SB-656933) 是一种有效的、选择性的、竞争性的、可逆的 CXCR2 拮抗剂。 -
Danirixin
产品货号 : M16816
cas no: 954126-98-8
Danirixin (GSK-1325756) 是一种高亲和力、选择性和可逆的 CXCR2 拮抗剂 (IC50=12.5 nM, CXCL8)。 -
LMD-009
产品货号 : M16794
cas no: 950195-51-4
LMD-009 (LMD 009, LMD009) 是一种有效的、选择性的非肽 CCR8 激动剂。