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(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)