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(42) Antifolate(10) ATM/ATR(24) Aurora Kinase(46) CLK(15) c-Myc(22) DHFR(7) DNA Alkylator(33) DNA gyrase(10) DNA Repair Protein(21) DNA/RNA Synthesis(141) DNA-PK(13) GPR(66) HDAC(138) Hec1/Nek2(9) Integrin(55) LIM Kinase (LIMK)(7) Mps1/TTK(2) Nucleoside Antimetabolite/Analog(48) Other Targets(4) PAK(11) PARP(50) PLK(19) Potassium Channel(107) RAD51(1) Rho(10) ROCK(29) Telomerase(9) Topoisomerase(61) Wee1(4)