title: Recent Progress in the Development of Transglutaminase 2 (TGase2) Inhibitors.
abstract: Transglutaminase 2 (TGase2, TG2) activity has been implicated in the pathogenesis of a number of unrelated disorders, including celiac, neurological, and renal diseases, and various forms of cancer. It has been suggested that TGase2 activity, such as cross-linking, deamidation, and GTP-related activity, is associated with each disease. Continuing efforts to develop small molecule TG2 inhibitors are ongoing. To develop a new class of TG2 inhibitors, the factors impeding the development of TG2 inhibitors have been identified. Additionally, the conformational effect of TG2 enzyme in regard to its pathological roles, in vitro screening methods, recently discovered TG2 inhibitors, and preclinical evaluations are discussed with a brief summary of current TG2 inhibitor pipelines under the clinical setting.
authors.affiliation: New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) , 80 Cheombok-ro, Dong-gu, Daegu 701-310, Korea.
authors.forename: Minsoo
authors.identifier: 0000-0002-2136-4618
authors.initials: M
authors.lastname: Song
authors.affiliation: New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) , 80 Cheombok-ro, Dong-gu, Daegu 701-310, Korea.
authors.forename: Hayoung
authors.initials: H
authors.lastname: Hwang
authors.affiliation: New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) , 80 Cheombok-ro, Dong-gu, Daegu 701-310, Korea.
authors.forename: Chun Young
authors.initials: CY
authors.lastname: Im
authors.affiliation: Cancer Cell and Molecular Biology Branch, Research Institute, National Cancer Center , Goyang-si, Gyeonggi-do 410-769, Korea.
authors.forename: Soo-Youl
authors.initials: SY
authors.lastname: Kim
mesh_terms: D000818:Animals; D001681:Biological Assay / Q000379:methods; D003543:Cysteamine / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D019204:GTP-Binding Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006801:Humans; D007555:Isoxazoles / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D017434:Protein Structure, Tertiary; D011503:Transglutaminases / Q000037:antagonists & inhibitors* / Q000737:chemistry
chemical_list: D004791:Enzyme Inhibitors; D007555:Isoxazoles; D003543:Cysteamine; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011503:Transglutaminases; D019204:GTP-Binding Proteins