Structure-based mechanism of cysteinyl leukotriene receptor inhibition by antiasthmatic drugs

Luginina, Aleksandra; Gusach, Anastasiia; Marin, Egor; Mishin, Alexey; Brouillette, Rebecca; Popov, Petr; Shiriaeva, Anna; Besserer-Offroy, Élie; Longpré, Jean -Michel; Lyapina, Elizaveta; Ishchenko, Andrii; Patel, Nilkanth; Polovinkin, Vitaly; Safronova, Nadezhda; Bogorodskiy, Andrey; Edelweiss, Evelina; Hu, Hao; Weierstall, Uwe; Liu, Wei; Batyuk, Alexander; Gordeliy, Valentin; Han, Gye Won; Sarret, Philippe; Katritch, Vsevolod; Borshchevskiy, Valentin; Cherezov, Vadim

doi:10.1126/sciadv.aax2518

Title: Structure-based mechanism of cysteinyl leukotriene receptor inhibition by antiasthmatic drugs

Journal Article · 09 October 2019 · Science Advances

DOI: https://doi.org/10.1126/sciadv.aax2518 · OSTI ID:1577320

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^[2]; Popov, Petr ^[3]; Shiriaeva, Anna ^[4];

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^[1]; Ishchenko, Andrii ^[5];

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^[1]; Bogorodskiy, Andrey ^[1]; Edelweiss, Evelina ^[7];

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^[8]; Liu, Wei ^[8];

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Moscow Inst. of Physics and Technology, Dolgoprudny (Russia)
Univ. de Sherbrooke, Quebec (Canada)
Moscow Inst. of Physics and Technology, Dolgoprudny (Russia); Skolkovo Inst. of Science and Technology, Moscow (Russia)
Univ. of Southern California, Los Angeles, CA (United States)
Univ. of Southern California, Los Angeles, CA (United States); Merck Research Labs, West Point, PA (United States)
Inst. of Complex Systems, Juelich (Germany); Univ. Grenoble Alpes-CEA-CNRS, Grenoble (France); Czech Academy of Sciences, Prague (Czech Republic)
Univ. Grenoble Alpes-CEA-CNRS, Grenoble (France)
Arizona State Univ., Tempe, AZ (United States)
SLAC National Accelerator Lab., Menlo Park, CA (United States)
Moscow Inst. of Physics and Technology, Dolgoprudny (Russia); Inst. of Complex Systems, Juelich (Germany); Univ. Grenoble Alpes-CEA-CNRS, Grenoble (France); Juelich Center for Structural Biology, Juelich (Germany); RWTH Aachen Univ., Aachen (Germany)
Univ. of Southern California, Los Angeles, CA (United States). Center for Energy Nanoscience and Technology
Moscow Inst. of Physics and Technology, Dolgoprudny (Russia); Inst. of Complex Systems, Juelich (Germany); Juelich Center for Structural Biology, Juelich (Germany)
Moscow Inst. of Physics and Technology, Dolgoprudny (Russia); Univ. of Southern California, Los Angeles, CA (United States)

The G protein–coupled cysteinyl leukotriene receptor CysLT₁R mediates inflammatory processes and plays a major role in numerous disorders, including asthma, allergic rhinitis, cardiovascular disease, and cancer. Selective CysLT₁R antagonists are widely prescribed as antiasthmatic drugs; however, these drugs demonstrate low effectiveness in some patients and exhibit a variety of side effects. To gain deeper understanding into the functional mechanisms of CysLTRs, we determined the crystal structures of CysLT₁R bound to two chemically distinct antagonists, zafirlukast and pranlukast. The structures reveal unique ligand-binding modes and signaling mechanisms, including lateral ligand access to the orthosteric pocket between transmembrane helices TM4 and TM5, an atypical pattern of microswitches, and a distinct four-residue–coordinated sodium site. These results provide important insights and structural templates for rational discovery of safer and more effective drugs.

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Research Organization:: SLAC National Accelerator Laboratory (SLAC), Menlo Park, CA (United States)

Sponsoring Organization:: USDOE

Grant/Contract Number:: AC02-76SF00515

OSTI ID:: 1577320

Journal Information:: Science Advances, Journal Name: Science Advances Journal Issue: 10 Vol. 5; ISSN 2375-2548

Publisher:: AAASCopyright Statement

Country of Publication:: United States

Language:: English

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Allosteric sodium in class A GPCR signaling Vsevolod, Katritch,; Vadim, Cherezov,; C., Stevens, Raymond The University of North Carolina at Chapel Hill University Libraries https://doi.org/10.17615/5vt2-kp93	text	January 2014
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Accurate determination of segmented X-ray detector geometry Yefanov, Oleksandr; Mariani, Valerio; Gati, Cornelius Deutsches Elektronen-Synchrotron, DESY, Hamburg https://doi.org/10.3204/pubdb-2015-04830	text	January 2015
Evaluation of Cysteinyl Leukotriene Signaling as a Therapeutic Target for Colorectal Cancer Burke, Lorraine; Butler, Clare T.; Murphy, Adrian Frontiers in Cell and Developmental Biology, Vol. 4 https://doi.org/10.3389/fcell.2016.00103	journal	September 2016

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Data set describing the in vitro biological activity of JMV2009, a novel silylated neurotensin(8–13) analog Besserer-Offroy, Élie; Tétreault, Pascal; Brouillette, Rebecca L. Data in Brief, Vol. 31 https://doi.org/10.1016/j.dib.2020.105884	journal	August 2020
Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors Gusach, Anastasiia; Luginina, Aleksandra; Marin, Egor Nature Communications, Vol. 10, Issue 1 https://doi.org/10.1038/s41467-019-13348-2	journal	December 2019
Structure-Based Virtual Screening for Ligands of G Protein–Coupled Receptors: What Can Molecular Docking Do for You? Ballante, Flavio; Kooistra, Albert J.; Kampen, Stefanie Pharmacological Reviews, Vol. 73, Issue 4 https://doi.org/10.1124/pharmrev.120.000246	journal	October 2021
Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors Gusach, Anastasiia; Luginina, Aleksandra; Marin, Egor Nature Communications, Vol. 10, Issue 1 https://doi.org/10.1038/s41467-019-13348-2	journal	December 2019
Structural insights into melatonin receptors Stauch, Benjamin; Johansson, Linda C.; Cherezov, Vadim The FEBS Journal, Vol. 287, Issue 8 https://doi.org/10.1111/febs.15128	journal	November 2019
Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors Gusach, Anastasiia; Luginina, Aleksandra; Marin, Egor RWTH Aachen University https://doi.org/10.18154/rwth-2020-00731	text	January 2019
Raman Scattering: From Structural Biology to Medical Applications Vlasov, Alexey V.; Maliar, Nina L.; Bazhenov, Sergey V. RWTH Aachen University https://doi.org/10.18154/rwth-2020-03626	text	January 2020
Raman Scattering: From Structural Biology to Medical Applications Vlasov, Alexey V.; Maliar, Nina L.; Bazhenov, Sergey V. Crystals, Vol. 10, Issue 1 https://doi.org/10.3390/cryst10010038	journal	January 2020

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