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Structure, function and pharmacology of human itch GPCRs by Can Cao; Hye Jin Kang; Isha Singh; He Chen; Chengwei Zhang; Wenlei Ye; Byron W. Hayes; Jing Liu; Ryan H. Gumpper; Brian J. Bender; Samuel T. Slocum; Brian E. Krumm; Katherine Lansu; John D. McCorvy; Wesley K. Kroeze; Justin G. English; Jeffrey F. DiBerto; Reid H. J. Olsen; Xi-Ping Huang; Shicheng Zhang; Yongfeng Liu; Kuglae Kim; Joel Karpiak; Lily Y. Jan; Soman N. Abraham; Jian Jin; Brian K. Shoichet; Jonathan F. Fay; Bryan L. Roth is a Physics and Astronomy article available to read on EtoBox.

What is Structure, function and pharmacology of human itch GPCRs about?

The MRGPRX family of receptors (MRGPRX1-4) is a family of mas-related G-protein-coupled receptors that have evolved relatively recently 1 . Of these, MRGPRX2 and MRGPRX4 are key physiological and pathological mediators of itch and related mast cell-mediated hypersensitivity reactions [2][3][4][5] . MRGPRX2 couples to both G i and G q in mast cells 6 . Here we describe agonist-stabilized structures of MRGPRX2 coupled to G i1 and G q in ternary complexes with the endogenous peptide cortistatin-14 and with a synthetic agonist probe, respectively, and the development of potent antagonist probes for MRGPRX2. We also describe a specific MRGPRX4 agonist and the structure of this agonist in a complex with MRGPRX4 and G q . Together, these findings should accelerate the structure-guided discovery of therapeutic agents for pain, itch and mast cell-mediated hypersensitivity. The sensation of itch (pruritis) can be triggered by many environmental insults, including insect bites, parasites, skin diseases such as eczema, liver and kidney diseases, and hypersensitivity reactions to commonly prescribed medications 7 . Itch has both neuronal 7 and non-neuronal components, with histamine release fro

Who reads Structure, function and pharmacology of human itch GPCRs?

Author

Can Cao; Hye Jin Kang; Isha Singh; He Chen; Chengwei Zhang; Wenlei Ye; Byron W. Hayes; Jing Liu; Ryan H. Gumpper; Brian J. Bender; Samuel T. Slocum; Brian E. Krumm; Katherine Lansu; John D. McCorvy; Wesley K. Kroeze; Justin G. English; Jeffrey F. DiBerto; Reid H. J. Olsen; Xi-Ping Huang; Shicheng Zhang; Yongfeng Liu; Kuglae Kim; Joel Karpiak; Lily Y. Jan; Soman N. Abraham; Jian Jin; Brian K. Shoichet; Jonathan F. Fay; Bryan L. Roth

Publisher

Springer Science and Business Media LLC

Published

2021

Language

EN

Field

Physics and Astronomy (Physical Sciences)