GPR
G protein-coupled receptors (GPCRs) comprise the largest family of cell surface receptors in the human genome, regulating a plethora of physiological responses and serving as frequent drug targets. Four main groups of GPCRs are recognized and classified according to their pharmacological properties: Class A is rhodopsin-like; Class B is secretin-like; Class C is comprised of metabotropic glutamate/pheromone; and Class D is comprised of frizzled receptors. While GPCRs regulate many aspects of tumorigenesis as well as many cancer-associated signaling pathways, only a few drugs aiming to inhibit GPCRs are currently used in cancer, these signal proteins are PARs, chemokine receptors, Gα12/13 proteins, lysophosphatidic acid (LPA), and GPCR-mediated pathways such as the WNT and Hippo signaling pathways.
References
1. Bar-Shavit R, et al. Int J Mol Sci. 2016;17(8):1320.
References
1. Bar-Shavit R, et al. Int J Mol Sci. 2016;17(8):1320.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
GPR
-
OX04528
产品货号 : M37520
cas no: 3028055-45-7
OX04528 is an orally active and potent GPR84 biased agonist.OX04528 inhibits cAMP signaling and may be useful in cancer research. -
NOX-6-18
产品货号 : M37363
cas no: 898211-21-7
GPR132antagonist 1 (GPR132-B-160, 化合物 25) 是一种 GPR132 拮抗剂,EC50 值为 0.075 μM。GPR132 antagonist 1 具有促进胰岛素分泌活性,EC50值为0.7 μM。 -
Ogremorphin
产品货号 : M37230
cas no: 352563-21-4
Ogremorphin (GPR68-IN-1) 是一种有效的 GPR68 抑制剂,其 EC50 为 170 nM。Ogremorphin 源自专利WO2020214896 (OGM1),可用于自身免疫性慢性炎症疾病研究。 -
WAY-298630
产品货号 : M36978
cas no: 303134-93-2
(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid is a prostaglandin-like CRTH2 antagonist with an IC50 < 10 μM, which can be used in studies of rhinitis, COPD, rheumatoid arthritis, eczema and conjunctivitis. -
BTB09089
产品货号 : M36055
cas no: 245728-44-3
BTB09089 是 T 细胞死亡相关基因 8 (TDAG8/GPR65) 特异性激动剂。BTB09089 增加 TDAG8 的表达,调节 T 细胞和巨噬细胞细胞因子的产生。