title: Topoisomerase as target for antibacterial and anticancer drug discovery.
abstract: DNA topoisomerases comprise a major aspect of basic cellular biology and are molecular targets for a variety of drugs like antibiotics, antibacterials and anticancer drugs. They act by inhibiting the topoisomerase molecule from relegating DNA strands after cleavage and convert the topoisomerases molecule into a DNA damaging agent. Though drugs of various categories acting through different mechanisms are available for the treatment, there are still problems associated with the currently available drugs. Therefore, Structural biologists, Structural chemists and Medicinal chemists all around the world have been identifying, designing, synthesizing and evaluating a variety of novel bioactive molecules targeting topoisomerase. This review summarizes types of topoisomerase and drug treating each class along with their structural requirement and activity. The emphasis has been laid in particular on the new potential heterocyles and the possible treatments as well as the current ongoing research status in the field of topoisomerase as dual targeting.
authors.affiliation: Department of Pharmaceutical Chemistry, Sinhgad College of Pharmacy, Maharashtra, India. drmkkathir@gmail.com
authors.forename: Muthu K
authors.initials: MK
authors.lastname: Kathiravan
authors.forename: Madhavi M
authors.initials: MM
authors.lastname: Khilare
authors.forename: Kiana
authors.initials: K
authors.lastname: Nikoomanesh
authors.forename: Aparna S
authors.initials: AS
authors.lastname: Chothe
authors.forename: Kishor S
authors.initials: KS
authors.lastname: Jain
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors; D004264:DNA Topoisomerases, Type I / Q000145:classification; D004250:DNA Topoisomerases, Type II; D055808:Drug Discovery; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods; D059004:Topoisomerase I Inhibitors / Q000737:chemistry / Q000494:pharmacology; D059005:Topoisomerase II Inhibitors / Q000737:chemistry / Q000494:pharmacology; D059003:Topoisomerase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D001426:Bacterial Proteins; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D059003:Topoisomerase Inhibitors; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II