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(8) AChR(5) Antifolate(9) ATM/ATR(23) Aurora Kinase(38) CLK(15) c-Myc(16) DHFR(4) DNA Alkylator(30) DNA gyrase(8) DNA Repair Protein(21) DNA/RNA Synthesis(94) DNA-PK(11) GPR(29) HDAC(117) Hec1/Nek2(9) Integrin(41) LIM Kinase (LIMK)(5) Mps1/TTK(1) Nucleoside Antimetabolite/Analog(25) Other Targets(2) PAK(7) PARP(32) PLK(11) Potassium Channel(67) RAD51(1) Rho(6) ROCK(16) Telomerase(6) Topoisomerase(46) Wee1(2)