title: TBK1 inhibitors: a review of patent literature (2011 - 2014).
abstract: TANK-binding kinase 1 (TBK1) is a noncanonical IκB kinase family member that regulates the innate immune response. Misregulation of TBK1 activity can promote inflammatory disorders and oncogenesis; therefore, TBK1 inhibitors are considered a promising therapy for inflammation and cancer.
  
  
  
  In this review, the authors provide information on the role of TBK1 in human health and on recently developed inhibitors from patents granted from 2011 to 2014. The reader will gain an understanding of the mechanisms of TBK1 function as well as the structure and biological activity of recently developed TBK1 inhibitors. Google and NCBI search engines were used to find relevant patents and clinical information using "TBK1 inhibitor" as the search term.
  
  
  
  The role of TBK1 in various diseases has prompted the further investigation of significant targets. Although research on TBK1 inhibitors has increased over the last few years, only a few inhibitors of this kinase have been identified. In addition, almost all of the chemical inhibitors are modified from different scaffolds and/or chemotypes of pyrimidine. Specifically, compound BX795 is the representative one, which was first patented as a potent TBK1 inhibitor. Even though some compounds have displayed interesting potential inhibition and selectivity of TBK1 in vitro and in in vivo trials, the development of more efficient and selective TBK1 inhibitors is still required.
authors: a 1 Qingdao University, Medical College , Qingdao 266071, China.
authors: Tao
authors: T
authors: Yu
authors: a 1 Qingdao University, Medical College , Qingdao 266071, China.
authors: Yanyan
authors: Y
authors: Yang
authors: b 2 Linyi Center for Disease Control and Prevention , Linyi 276000, China.
authors: De Qing
authors: DQ
authors: Yin
authors: c 3 Sungkyunkwan University, Department of Genetic Engineering , 300 Chuncheon-Dong, Suwon 440-746, Korea +82 312 907 868 ; +82 312 907 870 ; jaecho@skku.edu.
authors: Sungyoul
authors: S
authors: Hong
authors: d 4 Sunchon National University, Department of Pharmacy , Suncheon 540-742, Republic of Korea +82 617 503 755 ; +82 617 503 708 ; sony@sunchon.ac.kr.
authors: Young-Jin
authors: YJ
authors: Son
authors: e 5 Chonbuk National University, College of Veterinary Medicine, Biosafety Research Institute, Department of Veterinary Physiology , Jeonju 561-756, Republic of Korea +82 632 702 563 ; +82 632 703 780 ; jhkim1@chonbuk.ac.kr.
authors: Jong-Hoon
authors: JH
authors: Kim
authors: c 3 Sungkyunkwan University, Department of Genetic Engineering , 300 Chuncheon-Dong, Suwon 440-746, Korea +82 312 907 868 ; +82 312 907 870 ; jaecho@skku.edu.
authors: Jae Youl
authors: JY
authors: Cho
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; C403191:TBK1 protein, human
keywords: BX795; TBK1 inhibitor; cancer therapy; inflammation; inhibitory selectivity; pyrimidine derivatives