Sandbox Reserved 1095

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This Sandbox is Reserved from 25/11/2019, through 30/9/2020 for use in the course "Structural Biology" taught by Bruno Kieffer at the University of Strasbourg, ESBS. This reservation includes Sandbox Reserved 1091 through Sandbox Reserved 1115.
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Human Angiotensin Receptor in complex with olmesartan (4ZUD)

Angiotensin receptors of type 1 belong to the G protein coupled receptor (GPCR) family. These transmembrane proteins interact with angiotensin II, their ligand, and play a crucial role in the renin-angiotensin-aldosterone system. AT1 receptors are predominantly expressed in cardiovascular tissues including heart, endothelium, kidney, vascular smooth muscle cells as well as lungs, brain and adrenal cortex. [1] They are therefore important for the cardiovascular physiology.

Human angiotensin receptor

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References

  1. 1.0 1.1 1.2 Thomas WG, Mendelsohn FA. Angiotensin receptors: form and function and distribution. Int J Biochem Cell Biol. 2003 Jun;35(6):774-9. doi:, 10.1016/s1357-2725(02)00263-7. PMID:12676163 doi:http://dx.doi.org/10.1016/s1357-2725(02)00263-7
  2. Kawai T, Forrester SJ, O'Brien S, Baggett A, Rizzo V, Eguchi S. AT1 receptor signaling pathways in the cardiovascular system. Pharmacol Res. 2017 Nov;125(Pt A):4-13. doi: 10.1016/j.phrs.2017.05.008. Epub, 2017 May 17. PMID:28527699 doi:http://dx.doi.org/10.1016/j.phrs.2017.05.008
  3. Goodfriend TL. Angiotensin receptors: history and mysteries. Am J Hypertens. 2000 Apr;13(4 Pt 1):442-9. doi: 10.1016/s0895-7061(99)00212-5. PMID:10821350 doi:http://dx.doi.org/10.1016/s0895-7061(99)00212-5
  4. Bumpus FM, Catt KJ, Chiu AT, DeGasparo M, Goodfriend T, Husain A, Peach MJ, Taylor DG Jr, Timmermans PB. Nomenclature for angiotensin receptors. A report of the Nomenclature Committee of the Council for High Blood Pressure Research. Hypertension. 1991 May;17(5):720-1. doi: 10.1161/01.hyp.17.5.720. PMID:2022414 doi:http://dx.doi.org/10.1161/01.hyp.17.5.720
  5. Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC. Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor. J Biol Chem. 2015 Sep 29. pii: jbc.M115.689000. PMID:26420482 doi:http://dx.doi.org/10.1074/jbc.M115.689000
  6. Zhang H, Unal H, Gati C, Han GW, Liu W, Zatsepin NA, James D, Wang D, Nelson G, Weierstall U, Sawaya MR, Xu Q, Messerschmidt M, Williams GJ, Boutet S, Yefanov OM, White TA, Wang C, Ishchenko A, Tirupula KC, Desnoyer R, Coe J, Conrad CE, Fromme P, Stevens RC, Katritch V, Karnik SS, Cherezov V. Structure of the Angiotensin receptor revealed by serial femtosecond crystallography. Cell. 2015 May 7;161(4):833-44. doi: 10.1016/j.cell.2015.04.011. Epub 2015 Apr, 23. PMID:25913193 doi:http://dx.doi.org/10.1016/j.cell.2015.04.011
  7. Protein Database (PDBsum): 4zud. European Bioinformatics (EBI); 2013.
  8. Fillion D, Cabana J, Guillemette G, Leduc R, Lavigne P, Escher E. Structure of the human angiotensin II type 1 (AT1) receptor bound to angiotensin II from multiple chemoselective photoprobe contacts reveals a unique peptide binding mode. J Biol Chem. 2013 Mar 22;288(12):8187-97. doi: 10.1074/jbc.M112.442053. Epub 2013, Feb 5. PMID:23386604 doi:http://dx.doi.org/10.1074/jbc.M112.442053
  9. 9.0 9.1 Singh KD, Unal H, Desnoyer R, Karnik SS. Mechanism of Hormone Peptide Activation of a GPCR: Angiotensin II Activated State of AT1R Initiated by van der Waals Attraction. J Chem Inf Model. 2019 Jan 28;59(1):373-385. doi: 10.1021/acs.jcim.8b00583. Epub , 2019 Jan 16. PMID:30608150 doi:http://dx.doi.org/10.1021/acs.jcim.8b00583
  10. 10.0 10.1 Takezako T, Unal H, Karnik SS, Node K. Current topics in angiotensin II type 1 receptor research: Focus on inverse agonism, receptor dimerization and biased agonism. Pharmacol Res. 2017 Sep;123:40-50. doi: 10.1016/j.phrs.2017.06.013. Epub 2017 Jun, 23. PMID:28648738 doi:http://dx.doi.org/10.1016/j.phrs.2017.06.013
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