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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.

Cell Cycle/DNA Damage

ABC(7) AChR(5) Antifolate(8) ATM/ATR(23) Aurora Kinase(37) CLK(15) c-Myc(16) DHFR(4) DNA Alkylator(29) DNA gyrase(7) DNA Repair Protein(21) DNA/RNA Synthesis(85) DNA-PK(11) GPR(19) HDAC(111) Hec1/Nek2(9) Integrin(38) LIM Kinase (LIMK)(4) Mps1/TTK(1) Nucleoside Antimetabolite/Analog(19) Other Targets(2) PARP(30) PLK(11) Potassium Channel(55) RAD51(1) Rho(5) ROCK(13) Telomerase(4) Topoisomerase(40) Wee1(2)