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Molecular Basis for Hormone Recognition and Activation of Corticotropin-Releasing Factor Receptors.

Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE
Mol Cell 77 669-680.e4 (2020)
Cited: 40 times
EuropePMC logo PMID: 32004470

Abstract

Corticotropin-releasing factor (CRF) and the three related peptides urocortins 1-3 (UCN1-UCN3) are endocrine hormones that control the stress responses by activating CRF1R and CRF2R, two members of class B G-protein-coupled receptors (GPCRs). Here, we present two cryoelectron microscopy (cryo-EM) structures of UCN1-bound CRF1R and CRF2R with the stimulatory G protein. In both structures, UCN1 adopts a single straight helix with its N terminus dipped into the receptor transmembrane bundle. Although the peptide-binding residues in CRF1R and CRF2R are different from other members of class B GPCRs, the residues involved in receptor activation and G protein coupling are conserved. In addition, both structures reveal bound cholesterol molecules to the receptor transmembrane helices. Our structures define the basis of ligand-binding specificity in the CRF receptor-hormone system, establish a common mechanism of class B GPCR activation and G protein coupling, and provide a paradigm for studying membrane protein-lipid interactions for class B GPCRs.

Reviews - 6pb1 mentioned but not cited (2)

  1. G protein-coupled receptors: structure- and function-based drug discovery. Yang D, Zhou Q, Labroska V, Qin S, Darbalaei S, Wu Y, Yuliantie E, Xie L, Tao H, Cheng J, Liu Q, Zhao S, Shui W, Jiang Y, Wang MW. Signal Transduct Target Ther 6 7 (2021)
  2. G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders. Wong TS, Li G, Li S, Gao W, Chen G, Gan S, Zhang M, Li H, Wu S, Du Y. Signal Transduct Target Ther 8 177 (2023)

Articles - 6pb1 mentioned but not cited (5)

  1. The quest for high-resolution G protein-coupled receptor-G protein structures. Grisshammer R. Proc Natl Acad Sci U S A 117 6971-6973 (2020)
  2. The Novel Application of Geometric Morphometrics with Principal Component Analysis to Existing G Protein-Coupled Receptor (GPCR) Structures. Wiseman DN, Samra N, Román Lara MM, Penrice SC, Goddard AD. Pharmaceuticals (Basel) 14 953 (2021)
  3. New Insights into the Structure and Function of Class B1 GPCRs. Cary BP, Zhang X, Cao J, Johnson RM, Piper SJ, Gerrard EJ, Wootten D, Sexton PM. Endocr Rev 44 492-517 (2023)
  4. Structure insights into selective coupling of G protein subtypes by a class B G protein-coupled receptor. Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE. Nat Commun 13 6670 (2022)
  5. Therapeutic and prognostic potential of GPCRs in prostate cancer from multi-omics landscape. Li S, Chen J, Chen X, Yu J, Guo Y, Li M, Pu X. Front Pharmacol 13 997664 (2022)


Reviews citing this publication (6)

  1. Capturing Peptide-GPCR Interactions and Their Dynamics. Kaiser A, Coin I. Molecules 25 E4724 (2020)
  2. By what molecular mechanisms do social determinants impact cardiometabolic risk? Baumer Y, Pita MA, Baez AS, Ortiz-Whittingham LR, Cintron MA, Rose RR, Gray VC, Osei Baah F, Powell-Wiley TM. Clin Sci (Lond) 137 469-494 (2023)
  3. Mechanisms of adhesion G protein-coupled receptor activation. Vizurraga A, Adhikari R, Yeung J, Yu M, Tall GG. J Biol Chem 295 14065-14083 (2020)
  4. Targeting VIP and PACAP Receptor Signaling: New Insights into Designing Drugs for the PACAP Subfamily of Receptors. Lu J, Piper SJ, Zhao P, Miller LJ, Wootten D, Sexton PM. Int J Mol Sci 23 8069 (2022)
  5. Structural insights into emergent signaling modes of G protein-coupled receptors. Sutkeviciute I, Vilardaga JP. J Biol Chem 295 11626-11642 (2020)
  6. Structure, function and drug discovery of GPCR signaling. Cheng L, Xia F, Li Z, Shen C, Yang Z, Hou H, Sun S, Feng Y, Yong X, Tian X, Qin H, Yan W, Shao Z. Mol Biomed 4 46 (2023)

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  2. Cryo-EM structures of inactive and active GABAB receptor. Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y. Cell Res 30 564-573 (2020)
  3. Structural insights into hormone recognition by the human glucose-dependent insulinotropic polypeptide receptor. Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW. Elife 10 e68719 (2021)
  4. Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy. Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y. Nat Commun 11 4121 (2020)
  5. Molecular recognition of two endogenous hormones by the human parathyroid hormone receptor-1. Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE. Acta Pharmacol Sin 44 1227-1237 (2023)
  6. Structural determinants of cholesterol recognition in helical integral membrane proteins. Marlow B, Kuenze G, Li B, Sanders CR, Meiler J. Biophys J 120 1592-1604 (2021)
  7. Structural mechanism of calcium-mediated hormone recognition and Gβ interaction by the human melanocortin-1 receptor. Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE. Cell Res 31 1061-1071 (2021)
  8. A unique hormonal recognition feature of the human glucagon-like peptide-2 receptor. Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW. Cell Res 30 1098-1108 (2020)
  9. Conserved class B GPCR activation by a biased intracellular agonist. Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE. Nature 621 635-641 (2023)
  10. Corticotropin-releasing factor is involved in acute stress-induced analgesia and antipruritus. Wang XD, Bai HM, Li XL, Zhang LF, Li F, Bai Y, Wu ZY, Liu SQ, Li H. Brain Behav 12 e2783 (2022)
  11. Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation. Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D. Nat Commun 13 92 (2022)
  12. Molecular insights into differentiated ligand recognition of the human parathyroid hormone receptor 2. Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW. Proc Natl Acad Sci U S A 118 e2101279118 (2021)
  13. Structure and dynamics of the active Gs-coupled human secretin receptor. Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ. Nat Commun 11 4137 (2020)
  14. A combined activation mechanism for the glucagon receptor. Mattedi G, Acosta-Gutiérrez S, Clark T, Gervasio FL. Proc Natl Acad Sci U S A 117 15414-15422 (2020)
  15. A distinctive ligand recognition mechanism by the human vasoactive intestinal polypeptide receptor 2. Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW. Nat Commun 13 2272 (2022)
  16. Altered signaling at the PTH receptor via modified agonist contacts with the extracellular domain provides a path to prolonged agonism in vivo. Liu S, Yu Z, Daley EJ, Bingman CA, Bruchs AT, Gardella TJ, Gellman SH. Proc Natl Acad Sci U S A 119 e2212736119 (2022)
  17. Computational Design of Potent and Selective d-Peptide Agonists of the Glucagon-like Peptide-2 Receptor. Valiente PA, Nim S, Kim J, Kim PM. J Med Chem 66 10342-10353 (2023)
  18. Conformational Dynamics of the Activated GLP-1 Receptor-Gs Complex Revealed by Cross-Linking Mass Spectrometry and Integrative Structure Modeling. Yuan S, Xia L, Wang C, Wu F, Zhang B, Pan C, Fan Z, Lei X, Stevens RC, Sali A, Sun L, Shui W. ACS Cent Sci 9 992-1007 (2023)
  19. Cryo-electron microscopy structure of the glucagon receptor with a dual-agonist peptide. Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM. J Biol Chem 295 9313-9325 (2020)
  20. Erasing m6A-dependent transcription signature of stress-sensitive genes triggers antidepressant actions. Wu PF, Han QQ, Chen FF, Shen TT, Li YH, Cao Y, Chen JG, Wang F. Neurobiol Stress 15 100390 (2021)
  21. Exploring Ligand Binding to Calcitonin Gene-Related Peptide Receptors. Deganutti G, Atanasio S, Rujan RM, Sexton PM, Wootten D, Reynolds CA. Front Mol Biosci 8 720561 (2021)
  22. Molecular Mechanisms of PTH/PTHrP Class B GPCR Signaling and Pharmacological Implications. Vilardaga JP, Clark LJ, White AD, Sutkeviciute I, Lee JY, Bahar I. Endocr Rev 44 474-491 (2023)
  23. New Insights Into the Evolution of Corticotropin-Releasing Hormone Family With a Special Focus on Teleosts. Maugars G, Mauvois X, Martin P, Aroua S, Rousseau K, Dufour S. Front Endocrinol (Lausanne) 13 937218 (2022)
  24. Structural genomics of the human dopamine receptor system. Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE. Cell Res (2023)
  25. Structure-based drug discovery of a corticotropin-releasing hormone receptor 1 antagonist using an X-ray free-electron laser. Kim H, Lim T, Ha GE, Lee JY, Kim JW, Chang N, Kim SH, Kim KH, Lee J, Cho Y, Kim BW, Abrahamsson A, Kim SH, Kim HJ, Park S, Lee SJ, Park J, Cheong E, Kim BM, Cho HS. Exp Mol Med 55 2039-2050 (2023)
  26. The Glycosphingolipid GM3 Modulates Conformational Dynamics of the Glucagon Receptor. Ansell TB, Song W, Sansom MSP. Biophys J 119 300-313 (2020)
  27. mRNA expression of CRF family members in urothelial bladder cancer. Mavridis C, Venihaki M, Dermitzaki E, Deiktakis M, Liapakis G, Mamoulakis C. Oncol Lett 27 13 (2024)


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