Small-molecule inhibitors targeting apoptosis signal-regulated kinase 1

被引：9
作者：
Wang, Tiantian [1 ,2 ]
Pang, Lidan [1 ]
He, Mengni [1 ]
Wang, Zengtao [1 ]
机构：
[1] Jiangxi Univ Chinese Med, Coll Pharm, Nanchang 330004, Peoples R China
[2] Jiangxi Univ Chinese Med, Natl Pharmaceut Engn Ctr Solid Preparat Chinese He, Nanchang 330006, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2023年 / 262卷
关键词：
ASK1; inhibitors; Reviews; Optimization strategies; Structure-activity relationships; ENDOPLASMIC-RETICULUM STRESS; ACTIVATED PROTEIN-KINASE; NECROSIS-FACTOR-ALPHA; NEURONAL CELL-DEATH; ASK1; INHIBITOR; INCREASED VULNERABILITY; DEPENDENT ACTIVATION; HIPPOCAMPAL-NEURONS; CRYSTAL-STRUCTURES; STRUCTURAL BASIS;
D O I：
10.1016/j.ejmech.2023.115889
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Apoptosis signal regulated kinase 1 (ASK1, also known as MAP3K5) is a member of the mitogen activated protein kinase kinase kinase (MAP3K) family. Since its first isolation from a human macrophage library in 1996, its research has been ongoing for over 25 years. A large number of reports have revealed that ASK1, as a key activator of the p38 mitogen-activated protein kinase and c-Jun N-terminal kinase (JNK) signaling cascade, responds to various stressors, and its inhibitors have important potential value in the treatment of diseases such as inflammation, cancer, and the nervous system and so on. This review summarizes the recent development in this field, including the structure and signaling pathways of ASK1, with a particular focus on the structureactivity relationships, and the hit-to-lead optimization strategies.
引用
收藏
页数：31
相关论文
共 163 条
  • [1] The Thioredoxin System Is Regulated by the ASK-1/JNK/p38/Survivin Pathway during Germ Cell Apoptosis
    Al-Kandari, Nora
    Fadel, Fatemah
    Al-Saleh, Farah
    Khashab, Farah
    Al-Maghrebi, May
    [J]. MOLECULES, 2019, 24 (18):
  • [2] Organ-based drug delivery
    Alsaggar, Mohammad
    Liu, Dexi
    [J]. JOURNAL OF DRUG TARGETING, 2018, 26 (5-6) : 385 - 397
  • [3] ASK1 inhibitor treatment suppresses p38/JNK signalling with reduced kidney inflammation and fibrosis in rat crescentic glomerulonephritis
    Amos, Liv A.
    Ma, Frank Y.
    Tesch, Greg H.
    Liles, John T.
    Breckenridge, David G.
    Nikolic-Paterson, David J.
    Han, Yingjie
    [J]. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE, 2018, 22 (09) : 4522 - 4533
  • [4] Mitogen-activated protein kinases in innate immunity
    Arthur, J. Simon C.
    Ley, Steven C.
    [J]. NATURE REVIEWS IMMUNOLOGY, 2013, 13 (09) : 679 - 692
  • [5] ASK1 and its role in cardiovascular and other disorders: available treatments and future prospects
    Baig, Mohammad Hassan
    Baker, Abu
    Ashraf, Ghulam M.
    Dong, Jae-June
    [J]. EXPERT REVIEW OF PROTEOMICS, 2019, 16 (10) : 857 - 870
  • [6] Heat shock protein gp96 and NAD(P)H oxidase 4 play key roles in Toll-like receptor 4-activated apoptosis during renal ischemia/reperfusion injury
    Ben Mkaddem, S.
    Pedruzzi, E.
    Werts, C.
    Coant, N.
    Bens, M.
    Cluzeaud, F.
    Goujon, J. M.
    Ogier-Denis, E.
    Vandewalle, A.
    [J]. CELL DEATH AND DIFFERENTIATION, 2010, 17 (09) : 1474 - 1485
  • [7] REDUCTION OF LIVER STEATOSIS AND FIBROSIS WITH AN ASK1 INHIBITOR IN A MURINE MODEL OF NASH IS ACCOMPANIED BY IMPROVEMENTS IN CHOLESTEROL, BILE ACID AND LIPID METABOLISM
    Budas, G.
    Karnik, S.
    Jonnson, T.
    Shafizadeh, T.
    Watkins, S.
    Breckenridge, D.
    Tumas, D.
    [J]. JOURNAL OF HEPATOLOGY, 2016, 64 : S170 - S170
  • [8] Structural and functional characterization of the human protein kinase ASK1
    Bunkoczi, Gabor
    Salah, Eidarus
    Filippakopoulos, Panagis
    Fedorov, Oleg
    Mueller, Susanne
    Sobott, Frank
    Parker, Sirlester A.
    Zhang, Haifeng
    Min, Wang
    Turk, Benjamin E.
    Knapp, Stefan
    [J]. STRUCTURE, 2007, 15 (10) : 1215 - 1226
  • [9] Chang E., 2009, APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS
  • [10] Crystal structures and mutagenesis of PPP-family ser/thr protein phosphatases elucidate the selectivity of cantharidin and novel norcantharidin-based inhibitors of PP5C
    Chattopadhyay, Debasish
    Swingle, Mark R.
    Salter, Edward A.
    Wood, Eric
    D'Arcy, Brandon
    Zivanov, Catherine
    Abney, Kevin
    Musiyenko, Alla
    Rusin, Scott F.
    Kettenbach, Arminja
    Yet, Larry
    Schroeder, Chad E.
    Golden, Jennifer E.
    Dunham, Wade H.
    Gingras, Anne-Claude
    Banerjee, Surajit
    Forbes, David
    Wierzbicki, Andrzej
    Honkanen, Richard E.
    [J]. BIOCHEMICAL PHARMACOLOGY, 2016, 109 : 14 - 26
12345678910