title: Tankyrase inhibitors as therapeutic targets for cancer.
abstract: Tankyrase 1 and 2 belonging to the family of poly(ADP-ribosyl)ases play an important role in PARsylation by utilizing NAD+ as a substrate in order to generate ADP-ribose polymers. Tankyrases are involved in a number of cellular functions, that includes telomere homeostasis, mitotic spindle formation, vesicle transport linked to glucose metabolism, Wnt/β-catenin signalling, and viral replication. These roles of tankyrases in disease-relevant cellular processes have made them attractive drug targets. Recently, several inhibitors have been identified as potential clinical leads. The current review covers the progress, mechanism and binding modes of recently known Tankyrase inhibitors and discusses the rational approaches that were used to identify the tankyrase inhibitors.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: Sd
authors.initials: S
authors.lastname: Riyaz
authors.forename: Ajay Kumar
authors.initials: AK
authors.lastname: Srivastava
authors.affiliation: Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad, 500 007, India. ahmedkamal@iict.res.in.
authors.forename: Abdul
authors.initials: A
authors.lastname: Rahim
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D038501:Tankyrases / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D038501:Tankyrases