Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

被引：0
|
作者：
Yi Zheng
Ling Qin
Natalia V. Ortiz Zacarías
Henk de Vries
Gye Won Han
Martin Gustavsson
Marta Dabros
Chunxia Zhao
Robert J. Cherney
Percy Carter
Dean Stamos
Ruben Abagyan
Vadim Cherezov
Raymond C. Stevens
Adriaan P. IJzerman
Laura H. Heitman
Andrew Tebben
Irina Kufareva
Tracy M. Handel
机构：
[1] Skaggs School of Pharmacy and Pharmaceutical Sciences,Division of Medicinal Chemistry
[2] University of California San Diego,Departments of Chemistry and Physics & Astronomy
[3] 9500 Gilman Drive,Departments of Biological Sciences and Chemistry
[4] ,undefined
[5] Leiden Academic Centre for Drug Research (LACDR),undefined
[6] Leiden University,undefined
[7] Leiden 2333 CC,undefined
[8] The Netherlands,undefined
[9] Bridge Institute,undefined
[10] University of Southern California,undefined
[11] Bristol-Myers Squibb Company,undefined
[12] Vertex Pharmaceuticals Inc.,undefined
[13] The Bridge Institute,undefined
[14] University of Southern California,undefined
来源：
Nature | 2016年 / 540卷
关键词：
D O I：
暂无
中图分类号：
学科分类号：
摘要：
The crystal structure of CCR2 chemokine receptor in a complex with two different antagonists—one orthosteric the other allosteric—which functionally cooperate to inhibit CCR2.
引用
收藏
页码：458 / 461
页数：3
相关论文
共 50 条
  • [1] Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists
    Zheng, Yi
    Qin, Ling
    Zacarias, Natalia V. Ortiz
    de Vries, Henk
    Han, Gye Won
    Gustavsson, Martin
    Dabros, Marta
    Zhao, Chunxia
    Cherney, Robert J.
    Carter, Percy
    Stamos, Dean
    Abagyan, Ruben
    Cherezov, Vadim
    Stevens, Raymond C.
    Ijzerman, Adriaan P.
    Heitman, Laura H.
    Tebben, Andrew
    Kufareva, Irina
    Handel, Tracy M.
    NATURE, 2016, 540 (7633) : 458 - +
  • [2] Allosteric and Orthosteric Sites in CC Chemokine Receptor (CCR5), a Chimeric Receptor Approach
    Thiele, Stefanie
    Steen, Anne
    Jensen, Pia C.
    Mokrosinski, Jacek
    Frimurer, Thomas M.
    Rosenkilde, Mette M.
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2011, 286 (43) : 37543 - 37554
  • [3] Crystal Structure of CC Chemokine Receptor 2A in Complex with an Orthosteric Antagonist Provides Insights for the Design of Selective Antagonists
    Apel, Anna-Katharina
    Cheng, Robert K. Y.
    Tautermann, Christofer S.
    Brauchle, Michael
    Huang, Chia-Ying
    Pautsch, Alexander
    Hennig, Michael
    Nar, Herbert
    Schnapp, Gisela
    STRUCTURE, 2019, 27 (03) : 427 - +
  • [4] Internalization of the chemokine receptor CCR4 can be evoked by orthosteric and allosteric receptor antagonists
    Ajram, Laura
    Begg, Malcolm
    Slack, Robert
    Cryan, Jenni
    Hall, David
    Hodgson, Simon
    Ford, Alison
    Barnes, Ashley
    Swieboda, Dawid
    Mousnier, Aurelie
    Solari, Roberto
    EUROPEAN JOURNAL OF PHARMACOLOGY, 2014, 729 : 75 - 85
  • [5] Advances in the Discovery of CC Chemokine Receptor 2 Antagonists
    Carter, Percy H.
    Cherney, Robert J.
    Mangion, Ian K.
    ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 42, 2007, 42 : 211 - 227
  • [6] Orthosteric and allosteric action of the C5a receptor antagonists
    Liu, Heng
    Kim, Hee Ryung
    Deepak, R. N. V. Krishna
    Wang, Lei
    Chung, Ka Young
    Fan, Hao
    Wei, Zhiyi
    Zhang, Cheng
    NATURE STRUCTURAL & MOLECULAR BIOLOGY, 2018, 25 (06) : 472 - +
  • [7] Orthosteric and allosteric action of the C5a receptor antagonists
    Heng Liu
    Hee Ryung Kim
    R. N. V. Krishna Deepak
    Lei Wang
    Ka Young Chung
    Hao Fan
    Zhiyi Wei
    Cheng Zhang
    Nature Structural & Molecular Biology, 2018, 25 : 472 - 481
  • [8] Labeling of CC Chemokine Receptor 2 with a Versatile Intracellular Allosteric Probe
    den Hollander, Lisa S.
    Beerkens, Bert L. H.
    Dekkers, Sebastian
    van Veldhoven, Jacobus P. D.
    Zacarias, Natalia V. Ortiz
    van der Horst, Cas
    Sieders, Elisabeth G.
    de Valk, Bert
    Wang, Jianhui
    Ijzerman, Adriaan P.
    van der Es, Daan
    Heitman, Laura H.
    ACS CHEMICAL BIOLOGY, 2024, 19 (09) : 2070 - 2080
  • [9] A Novel, Intracellular, Allosteric Site for Antagonists at CC and CXC Chemokine Receptors
    Wreggett, Keith
    JOURNAL OF BIOMOLECULAR SCREENING, 2009, 14 (07) : 902 - 902
  • [10] Spiroindenes and spiroindanes as antagonists of CC chemokine receptor 2: WO 2009023754
    Carter, Percy H.
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2010, 20 (02) : 283 - 289
12345