Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

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 () and Tracy M. Handel ()
Additional contact information
Yi Zheng: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Ling Qin: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Natalia V. Ortiz Zacarías: Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands
Henk de Vries: Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands
Gye Won Han: Bridge Institute, University of Southern California
Martin Gustavsson: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Marta Dabros: Bristol-Myers Squibb Company
Chunxia Zhao: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Robert J. Cherney: Bristol-Myers Squibb Company
Percy Carter: Bristol-Myers Squibb Company
Dean Stamos: Vertex Pharmaceuticals Inc.
Ruben Abagyan: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Vadim Cherezov: Bridge Institute, University of Southern California
Raymond C. Stevens: The Bridge Institute, University of Southern California
Adriaan P. IJzerman: Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands
Laura H. Heitman: Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands
Andrew Tebben: Bristol-Myers Squibb Company
Irina Kufareva: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,
Tracy M. Handel: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,

Nature, 2016, vol. 540, issue 7633, 458-461

Abstract: 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.

Date: 2016
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DOI: 10.1038/nature20605

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