The SAR of UK-78,282: A novel blocker of human T cell Kv1.3 potassium channels

被引：22
|
作者：
Burgess, LE
Koch, K
Cooper, K
Biggers, MS
Ramchandani, M
Smitrovich, JH
Gilbert, EJ
Bruns, MJ
Mather, RJ
Donovan, CB
Hanson, DC
机构：
[1] PFIZER INC,DIV CENT RES,DEPT MED CHEM,GROTON,CT 06340
[2] PFIZER INC,DIV CENT RES,DEPT IMMUNOL,GROTON,CT 06340
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 08期
关键词：
D O I：
10.1016/S0960-894X(97)00163-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
UK-78,282 was identified in a human T cell Rb-86 efflux high-throughput screen of our compound libraries. This compound was found to be a potent and selective blacker of human T cell voltage-gated K+ channels and to inhibit T cell activation. The SAR around UK-78,282 and a general pharmacophore hypothesis are presented in this communication. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：1047 / 1052
页数：6
相关论文
共 50 条
  • [31] Assembly and suppression of endogenous Kv1.3 channels in human T lymphocytes.
    Panyi, G
    Deutsch, C
    BIOPHYSICAL JOURNAL, 1996, 70 (02) : SUA10 - SUA10
  • [32] Kv1.3 and Kv1.5 Channels as Novel Targets for the Prevention of Restenosis in Human Vessels
    Teresa Perez-Garcia, M.
    Arevalo-Martinez, Marycarmen
    Angel de la Fuente, Miguel
    Simarro, Maria
    Alonso, Esperanza
    Ramon Lopez-Lopez, Jose
    Cidad, Pilar
    FASEB JOURNAL, 2017, 31
  • [33] Stimulation of Kv1.3 potassium channels by death receptors during apoptosis in Jurkat T lymphocytes
    Storey, NM
    Gómez-Angelats, M
    Bortner, CD
    Armstrong, DL
    Cidlowski, JA
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2003, 278 (35) : 33319 - 33326
  • [34] Curcumin Serves as a Human Kv1.3 Blocker to Inhibit Effector Memory T Lymphocyte Activities
    Lian, Yi-Tian
    Yang, Xiao-Fang
    Wang, Zhao-Hui
    Yang, Yong
    Yang, Ying
    Shu, Yan-Wen
    Cheng, Long-Xian
    Liu, Kun
    PHYTOTHERAPY RESEARCH, 2013, 27 (09) : 1321 - 1327
  • [35] STABLE EXPRESSION OF HUMAN KV1.3 POTASSIUM CHANNELS RESETS THE RESTING POTENTIAL OF CHO CELLS
    LEONARD, RJ
    STEVENS, SP
    DEFARIAS, FP
    BIOPHYSICAL JOURNAL, 1994, 66 (02) : A136 - A136
  • [36] Voltage-Dependent Conformational Changes of KV1.3 Potassium Channels are an Essential Element for KV1.3-induced cell proliferation
    Teresa Perez-Garcia, M.
    Cidad, Pilar
    Alonso, Esperanza
    Fernandez-Velasco, Pablo
    de la Fuente, Miguel A.
    Lopez-Lopez, Jose R.
    BIOPHYSICAL JOURNAL, 2018, 114 (03) : 378A - 378A
  • [37] The influence of zinc on the modulatory effect of sphingosylphosphorylcholine on Kv1.3 channels in human T lymphocytes
    Teisseyre, A
    Michalak, K
    EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS, 2004, 33 (06): : 543 - 548
  • [38] The influence of zinc on the modulatory effect of sphingosylphosphorylcholine on Kv1.3 channels in human T lymphocytes
    Andrzej Teisseyre
    Krystyna Michalak
    European Biophysics Journal, 2004, 33 : 543 - 548
  • [39] Inactivation mechanism of an immunoglobulin modulator of the T-cell potassium channel Kv1.3
    Selvakumar, Purushotham
    Fernandez-Marino, Ana I.
    Wang, Bing
    Rice, William J.
    Meyerson, Joel R.
    Swartz, Kenton J.
    BIOPHYSICAL JOURNAL, 2023, 122 (03) : 13A - 14A
  • [40] Blockage of human T lymphocyte Kv1.3 channels by Pi1, a novel class of scorpion toxin
    Peter, M
    Hajdu, P
    Varga, Z
    Damjanovich, S
    Possani, LD
    Panyi, G
    Gaspar, R
    BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2000, 278 (01) : 34 - 37
12345