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DNA gyrase

DNA gyrase is a type IIA topoisomerase belonging to gyrase, heat-shock protein 90 (Hsp 90) histidine kinase MutL (GHKL), protein kinases and the DNA mismatch repair protein MutL (Mismatch from replication recognized by mutL)) family of enzymes. These enzymes are associated with many fundamental biological processes that involve DNA- they are involved in segregation of DNA after replication, initiation of DNA replication and gene expression. It comprises of two subunits-gyrase A and gyrase B that together form the catalytically active heterotetrameric enzyme (i.e. A2B2). The role of the A subunit is breakage and reunion of the double DNA strand, while the B subunit (DNA gyrase B) possesses the ATPase activity, providing a sufficient amount of energy for the DNA supercoiling. DNA gyrase being a highly appealing drug target, a large number of inhibitors have been synthesized and characterized with quinolones and aminocoumarins being the most widely studied compounds.

References

1.Khan T,et al. Biomed Pharmacother. 2018 Jul;103:923-938.

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)