Discovery of novel and highly selective PI3Kδ inhibitors based on the p110δ crystal structure

被引：2
|
作者：
Jia, Wen-Qing [1 ]
Liu, Ya-Ya [1 ]
Feng, Xiao-Yan [1 ]
Xu, Wei-Ren [2 ]
Cheng, Xian-Chao [1 ]
机构：
[1] Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, Tianjin 300070, Peoples R China
[2] Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug Discovery, Tianjin, Peoples R China
来源：
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS | 2020年 / 38卷 / 08期
基金：
中国国家自然科学基金;
关键词：
D O I：
10.1080/07391102.2019.1635531
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
引用
收藏
页码：2499 / 2508
页数：10
相关论文
共 50 条
  • [41] Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3Kγ
    Sha, Shao
    Han, Hong-Wei
    Gao, Fei
    Liu, Tian-Bao
    Li, Zhen
    Xu, Chi
    Zhong, Wei-Qing
    Zhu, Hai-Liang
    MEDCHEMCOMM, 2015, 6 (11) : 2029 - 2035
  • [42] Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors
    Hoegenauer, Klemens
    Soldermann, Nicolas
    Stauffer, Frederic
    Furet, Pascal
    Graveleau, Nadege
    Smith, Alexander B.
    Hebach, Christina
    Hollingworth, Gregory J.
    Lewis, Ian
    Gutmann, Sascha
    Rummel, Gabriele
    Knapp, Mark
    Wolf, Romain M.
    Blanz, Joachim
    Feifel, Roland
    Burkhart, Christoph
    Zecri, Frederic
    ACS MEDICINAL CHEMISTRY LETTERS, 2016, 7 (08): : 762 - 767
  • [43] Dominant Role of the p110β Isoform of PI3K over p110α in Energy Homeostasis Regulation by POMC and AgRP Neurons
    Al-Qassab, Hind
    Smith, Mark A.
    Irvine, Elaine E.
    Guillermet-Guibert, Julie
    Claret, Marc
    Choudhury, Agharul I.
    Selman, Colin
    Piipari, Kaisa
    Clements, Melanie
    Lingard, Steven
    Chandarana, Keval
    Bell, Jimmy D.
    Barsh, Gregory S.
    Smith, Andrew J. H.
    Batterham, Rachel L.
    Ashford, Michael L. J.
    Vanhaesebroeck, Bart
    Withers, Dominic J.
    CELL METABOLISM, 2009, 10 (05) : 343 - 354
  • [44] PI3K p110δ controls the differentiation and function of regulatory T cells
    Patton, D. T.
    Emery, J. L.
    Rowan, W. C.
    Okkenhaug, K.
    IMMUNOLOGY, 2008, 125 : 129 - 129
  • [45] The structure of a human p110α/p85α complex elucidates the effects of oncogenic PI3Kα mutations
    Huang, Chuan-Hsiang
    Mandelker, Diana
    Schmidt-Kittler, Oleg
    Samuels, Yardena
    Velculescu, Victor E.
    Kinzler, Kenneth W.
    Vogelstein, Bert
    Gabelli, Sandra B.
    Amzel, L. Mario
    SCIENCE, 2007, 318 (5857) : 1744 - 1748
  • [46] Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110α
    Zunder, Eli R.
    Knight, Zachary A.
    Houseman, Benjamin T.
    Apsel, Beth
    Shokat, Kevan M.
    CANCER CELL, 2008, 14 (02) : 180 - 192
  • [47] Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis
    Yu, Mengyao
    Wang, Xian
    Tang, Yongmei
    Wang, Longling
    Hu, Xueping
    Weng, Qinjie
    Wang, Jiajia
    Cui, Sunliang
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (11) : 9628 - 9644
  • [48] Cardiac PI3K p110α attenuation delays aging and extends lifespan
    Abdellatif, Mahmoud
    Eisenberg, Tobias
    Heberle, Alexander Martin
    Thedieck, Kathrin
    Kroemer, Guido
    Sedej, Simon
    CELL STRESS, 2022, 6 (08) : 72 - 75
  • [49] PI3K p110δ expression in Merkel cell carcinoma cell lines
    Chteinberg, E.
    Rennspiess, D.
    Tauchmann, S.
    Winnepenninckx, V.
    Speel, E. -J.
    Kurz, A. K.
    Zenke, M.
    Hausen, A. Z.
    JOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY AND VENEREOLOGY, 2017, 31 : 96 - 97
  • [50] Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors
    Bandarage, Upul K.
    Aronov, Alex M.
    Cao, Jingrong
    Come, Jon H.
    Cottrell, Kevin M.
    Davies, Robert J.
    Giroux, Simon
    Jacobs, Marc
    Mahajan, Sudipta
    Messersmith, David
    Moody, Cameron S.
    Swett, Rebecca
    Xu, Jinwang
    ACS MEDICINAL CHEMISTRY LETTERS, 2021, 12 (01): : 129 - 135
12345