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Pharmacological Characterization and Investigation of N-Terminal Loop Amino Acids of Adrenomedullin 2 That Are Important for Receptor Activation.

Musa H, Hendrikse ER, Brimble MA, Garelja ML, Watkins HA, Harris PWR, Hay DL.

Biochemistry. 2019 Aug 13;58(32):3468-3474. doi: 10.1021/acs.biochem.9b00571. Epub 2019 Jul 29.


New Insights into the Regulation of CGRP-Family Receptors.

Gingell JJ, Hendrikse ER, Hay DL.

Trends Pharmacol Sci. 2019 Jan;40(1):71-83. doi: 10.1016/ Epub 2018 Dec 4. Review.


Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.

Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM.

Nature. 2018 Sep;561(7724):492-497. doi: 10.1038/s41586-018-0535-y. Epub 2018 Sep 12.


Amyloidogenicity, Cytotoxicity, and Receptor Activity of Bovine Amylin: Implications for Xenobiotic Transplantation and the Design of Nontoxic Amylin Variants.

Akter R, Bower RL, Abedini A, Schmidt AM, Hay DL, Raleigh DP.

ACS Chem Biol. 2018 Sep 21;13(9):2747-2757. doi: 10.1021/acschembio.8b00690. Epub 2018 Aug 22.


Photoaffinity Cross-Linking and Unnatural Amino Acid Mutagenesis Reveal Insights into Calcitonin Gene-Related Peptide Binding to the Calcitonin Receptor-like Receptor/Receptor Activity-Modifying Protein 1 (CLR/RAMP1) Complex.

Simms J, Uddin R, Sakmar TP, Gingell JJ, Garelja ML, Hay DL, Brimble MA, Harris PW, Reynolds CA, Poyner DR.

Biochemistry. 2018 Aug 14;57(32):4915-4922. doi: 10.1021/acs.biochem.8b00502. Epub 2018 Jul 25.


Solid-Phase Thiol-Ene Lipidation of Peptides for the Synthesis of a Potent CGRP Receptor Antagonist.

Williams ET, Harris PWR, Jamaluddin MA, Loomes KM, Hay DL, Brimble MA.

Angew Chem Int Ed Engl. 2018 Sep 3;57(36):11640-11643. doi: 10.1002/anie.201805208. Epub 2018 Aug 6.


CGRP Receptor Biology: Is There More Than One Receptor?

Hay DL.

Handb Exp Pharmacol. 2019;255:13-22. doi: 10.1007/164_2018_131.


Molecular studies of CGRP and the CGRP family of peptides in the central nervous system.

Hendrikse ER, Bower RL, Hay DL, Walker CS.

Cephalalgia. 2019 Mar;39(3):403-419. doi: 10.1177/0333102418765787. Epub 2018 Mar 22.


Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy.

Dal Maso E, Zhu Y, Pham V, Reynolds CA, Deganutti G, Hick CA, Yang D, Christopoulos A, Hay DL, Wang MW, Sexton PM, Furness SGB, Wootten D.

Biochem Pharmacol. 2018 Apr;150:214-244. doi: 10.1016/j.bcp.2018.02.005. Epub 2018 Feb 16.


Receptor Activity Modifying Proteins Have Limited Effects on the Class B G Protein-Coupled Receptor Calcitonin Receptor-Like Receptor Stalk.

Garelja ML, Walker CA, Siow A, Yang SH, Harris PWR, Brimble MA, Watkins HA, Gingell JJ, Hay DL.

Biochemistry. 2018 Feb 27;57(8):1410-1422. doi: 10.1021/acs.biochem.7b01180. Epub 2018 Feb 7.


Probing the Mechanism of Receptor Activity-Modifying Protein Modulation of GPCR Ligand Selectivity through Rational Design of Potent Adrenomedullin and Calcitonin Gene-Related Peptide Antagonists.

Booe JM, Warner ML, Roehrkasse AM, Hay DL, Pioszak AA.

Mol Pharmacol. 2018 Apr;93(4):355-367. doi: 10.1124/mol.117.110916. Epub 2018 Jan 23.


Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25.

Hay DL, Garelja ML, Poyner DR, Walker CS.

Br J Pharmacol. 2018 Jan;175(1):3-17. doi: 10.1111/bph.14075. Epub 2017 Nov 28. Review.


Receptor activity-modifying protein dependent and independent activation mechanisms in the coupling of calcitonin gene-related peptide and adrenomedullin receptors to Gs.

Woolley MJ, Reynolds CA, Simms J, Walker CS, Mobarec JC, Garelja ML, Conner AC, Poyner DR, Hay DL.

Biochem Pharmacol. 2017 Oct 15;142:96-110. doi: 10.1016/j.bcp.2017.07.005. Epub 2017 Jul 11.


N-Glycosylation of Asparagine 130 in the Extracellular Domain of the Human Calcitonin Receptor Significantly Increases Peptide Hormone Affinity.

Lee SM, Booe JM, Gingell JJ, Sjoelund V, Hay DL, Pioszak AA.

Biochemistry. 2017 Jul 5;56(26):3380-3393. doi: 10.1021/acs.biochem.7b00256. Epub 2017 Jun 26.



Hay DL.

Headache. 2017 May;57 Suppl 2:89-96. doi: 10.1111/head.13077. Review.


CGRP and its receptors.

Hay DL, Walker CS.

Headache. 2017 Apr;57(4):625-636. doi: 10.1111/head.13064. Epub 2017 Feb 24.


CGRP receptor antagonist activity of olcegepant depends on the signalling pathway measured.

Walker CS, Raddant AC, Woolley MJ, Russo AF, Hay DL.

Cephalalgia. 2018 Mar;38(3):437-451. doi: 10.1177/0333102417691762. Epub 2017 Feb 6.


Erratum: An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology.

Gingell JJ, Simms J, Barwell J, Poyner DR, Watkins HA, Pioszak AA, Sexton PM, Hay DL.

Cell Discov. 2016 Jun 21;2:16020. doi: 10.1038/celldisc.2016.20. eCollection 2016.


An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology.

J Gingell J, Simms J, Barwell J, Poyner DR, Watkins HA, Pioszak AA, Sexton PM, Hay DL.

Cell Discov. 2016 May 17;2:16012. doi: 10.1038/celldisc.2016.12. eCollection 2016. Erratum in: Cell Discov. 2016;2:16020.


Synthesis and amylin receptor activity of glycomimetics of pramlintide using click chemistry.

Yule LR, Bower RL, Kaur H, Kowalczyk R, Hay DL, Brimble MA.

Org Biomol Chem. 2016 Jun 21;14(23):5238-45. doi: 10.1039/c6ob00850j. Epub 2016 May 3.


Reply to comment on: A second trigeminal CGRP receptor: function and expression of the AMY1 receptor.

Walker CS, Hay DL.

Ann Clin Transl Neurol. 2016 Feb 25;3(4):309-10. doi: 10.1002/acn3.294. eCollection 2016 Apr. No abstract available.


Receptor activity-modifying proteins; multifunctional G protein-coupled receptor accessory proteins.

Hay DL, Walker CS, Gingell JJ, Ladds G, Reynolds CA, Poyner DR.

Biochem Soc Trans. 2016 Apr 15;44(2):568-73. doi: 10.1042/BST20150237. Review.


Amylin structure-function relationships and receptor pharmacology: implications for amylin mimetic drug development.

Bower RL, Hay DL.

Br J Pharmacol. 2016 Jun;173(12):1883-98. doi: 10.1111/bph.13496. Epub 2016 May 18. Review.


Receptor Activity-modifying Proteins 2 and 3 Generate Adrenomedullin Receptor Subtypes with Distinct Molecular Properties.

Watkins HA, Chakravarthy M, Abhayawardana RS, Gingell JJ, Garelja M, Pardamwar M, McElhinney JM, Lathbridge A, Constantine A, Harris PW, Yuen TY, Brimble MA, Barwell J, Poyner DR, Woolley MJ, Conner AC, Pioszak AA, Reynolds CA, Hay DL.

J Biol Chem. 2016 May 27;291(22):11657-75. doi: 10.1074/jbc.M115.688218. Epub 2016 Mar 24.


Mapping the calcitonin receptor in human brain stem.

Bower RL, Eftekhari S, Waldvogel HJ, Faull RL, Tajti J, Edvinsson L, Hay DL, Walker CS.

Am J Physiol Regul Integr Comp Physiol. 2016 May 1;310(9):R788-93. doi: 10.1152/ajpregu.00539.2015. Epub 2016 Feb 24.


Glicentin-related pancreatic polypeptide inhibits glucose-stimulated insulin secretion from the isolated pancreas of adult male rats.

Whiting L, Stewart KW, Hay DL, Harris PW, Choong YS, Phillips AR, Brimble MA, Cooper GJ.

Physiol Rep. 2015 Dec;3(12). pii: e12638. doi: 10.14814/phy2.12638.


Receptor Activity-Modifying Proteins (RAMPs): New Insights and Roles.

Hay DL, Pioszak AA.

Annu Rev Pharmacol Toxicol. 2016;56:469-87. doi: 10.1146/annurev-pharmtox-010715-103120. Epub 2015 Oct 23. Review.


Anxiogenic and Stressor Effects of the Hypothalamic Neuropeptide RFRP-3 Are Overcome by the NPFFR Antagonist GJ14.

Kim JS, Brownjohn PW, Dyer BS, Beltramo M, Walker CS, Hay DL, Painter GF, Tyndall JD, Anderson GM.

Endocrinology. 2015 Nov;156(11):4152-62. doi: 10.1210/en.2015-1532. Epub 2015 Aug 10.


A second trigeminal CGRP receptor: function and expression of the AMY1 receptor.

Walker CS, Eftekhari S, Bower RL, Wilderman A, Insel PA, Edvinsson L, Waldvogel HJ, Jamaluddin MA, Russo AF, Hay DL.

Ann Clin Transl Neurol. 2015 Jun;2(6):595-608. doi: 10.1002/acn3.197. Epub 2015 Apr 1.


Amylin: Pharmacology, Physiology, and Clinical Potential.

Hay DL, Chen S, Lutz TA, Parkes DG, Roth JD.

Pharmacol Rev. 2015 Jul;67(3):564-600. doi: 10.1124/pr.115.010629. Review.


Structural Basis for Receptor Activity-Modifying Protein-Dependent Selective Peptide Recognition by a G Protein-Coupled Receptor.

Booe JM, Walker CS, Barwell J, Kuteyi G, Simms J, Jamaluddin MA, Warner ML, Bill RM, Harris PW, Brimble MA, Poyner DR, Hay DL, Pioszak AA.

Mol Cell. 2015 Jun 18;58(6):1040-52. doi: 10.1016/j.molcel.2015.04.018. Epub 2015 May 14.


Convergent chemoenzymatic synthesis of a library of glycosylated analogues of pramlintide: structure-activity relationships for amylin receptor agonism.

Kowalczyk R, Brimble MA, Tomabechi Y, Fairbanks AJ, Fletcher M, Hay DL.

Org Biomol Chem. 2014 Nov 7;12(41):8142-51. doi: 10.1039/c4ob01208a. Epub 2014 Jul 17.


α-Calcitonin gene related peptide (α-CGRP) mediated lipid mobilization in 3T3-L1 adipocytes.

Walker CS, Hay DL, Fitzpatrick SM, Cooper GJ, Loomes KM.

Peptides. 2014 Aug;58:14-9. doi: 10.1016/j.peptides.2014.05.011. Epub 2014 Jun 2.


The Concise Guide to PHARMACOLOGY 2013/14: overview.

Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ; CGTP Collaborators, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, Arita M, Arthofer E, Barker EL, Barratt C, Barnes NM, Bathgate R, Beart PM, Belelli D, Bennett AJ, Birdsall NJ, Boison D, Bonner TI, Brailsford L, Bröer S, Brown P, Calo G, Carter WG, Catterall WA, Chan SL, Chao MV, Chiang N, Christopoulos A, Chun JJ, Cidlowski J, Clapham DE, Cockcroft S, Connor MA, Cox HM, Cuthbert A, Dautzenberg FM, Davenport AP, Dawson PA, Dent G, Dijksterhuis JP, Dollery CT, Dolphin AC, Donowitz M, Dubocovich ML, Eiden L, Eidne K, Evans BA, Fabbro D, Fahlke C, Farndale R, Fitzgerald GA, Fong TM, Fowler CJ, Fry JR, Funk CD, Futerman AH, Ganapathy V, Gaisnier B, Gershengorn MA, Goldin A, Goldman ID, Gundlach AL, Hagenbuch B, Hales TG, Hammond JR, Hamon M, Hancox JC, Hauger RL, Hay DL, Hobbs AJ, Hollenberg MD, Holliday ND, Hoyer D, Hynes NA, Inui KI, Ishii S, Jacobson KA, Jarvis GE, Jarvis MF, Jensen R, Jones CE, Jones RL, Kaibuchi K, Kanai Y, Kennedy C, Kerr ID, Khan AA, Klienz MJ, Kukkonen JP, Lapoint JY, Leurs R, Lingueglia E, Lippiat J, Lolait SJ, Lummis SC, Lynch JW, MacEwan D, Maguire JJ, Marshall IL, May JM, McArdle CA, McGrath JC, Michel MC, Millar NS, Miller LJ, Mitolo V, Monk PN, Moore PK, Moorhouse AJ, Mouillac B, Murphy PM, Neubig RR, Neumaier J, Niesler B, Obaidat A, Offermanns S, Ohlstein E, Panaro MA, Parsons S, Pwrtwee RG, Petersen J, Pin JP, Poyner DR, Prigent S, Prossnitz ER, Pyne NJ, Pyne S, Quigley JG, Ramachandran R, Richelson EL, Roberts RE, Roskoski R, Ross RA, Roth M, Rudnick G, Ryan RM, Said SI, Schild L, Sanger GJ, Scholich K, Schousboe A, Schulte G, Schulz S, Serhan CN, Sexton PM, Sibley DR, Siegel JM, Singh G, Sitsapesan R, Smart TG, Smith DM, Soga T, Stahl A, Stewart G, Stoddart LA, Summers RJ, Thorens B, Thwaites DT, Toll L, Traynor JR, Usdin TB, Vandenberg RJ, Villalon C, Vore M, Waldman SA, Ward DT, Willars GB, Wonnacott SJ, Wright E, Ye RD, Yonezawa A, Zimmermann M.

Br J Pharmacol. 2013 Dec;170(8):1449-58. doi: 10.1111/bph.12444.


Receptor activity-modifying protein-dependent effects of mutations in the calcitonin receptor-like receptor: implications for adrenomedullin and calcitonin gene-related peptide pharmacology.

Watkins HA, Walker CS, Ly KN, Bailey RJ, Barwell J, Poyner DR, Hay DL.

Br J Pharmacol. 2014 Feb;171(3):772-88. doi: 10.1111/bph.12508.


Activity of pramlintide, rat and human amylin but not Aβ1-42 at human amylin receptors.

Gingell JJ, Burns ER, Hay DL.

Endocrinology. 2014 Jan;155(1):21-6. doi: 10.1210/en.2013-1658. Epub 2013 Dec 20.


Structure-activity relationships of the N-terminus of calcitonin gene-related peptide: key roles of alanine-5 and threonine-6 in receptor activation.

Hay DL, Harris PW, Kowalczyk R, Brimble MA, Rathbone DL, Barwell J, Conner AC, Poyner DR.

Br J Pharmacol. 2014 Jan;171(2):415-26. doi: 10.1111/bph.12464.


The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach.

Woolley MJ, Watkins HA, Taddese B, Karakullukcu ZG, Barwell J, Smith KJ, Hay DL, Poyner DR, Reynolds CA, Conner AC.

J R Soc Interface. 2013 Sep 18;10(88):20130589. doi: 10.1098/rsif.2013.0589. Print 2013 Nov 6.


Functions of third extracellular loop and helix 8 of Family B GPCRs complexed with RAMPs and characteristics of their receptor trafficking.

Kuwasako K, Hay DL, Nagata S, Murakami M, Kitamura K, Kato J.

Curr Protein Pept Sci. 2013 Aug;14(5):416-28. Review.


CGRP in the trigeminovascular system: a role for CGRP, adrenomedullin and amylin receptors?

Walker CS, Hay DL.

Br J Pharmacol. 2013 Dec;170(7):1293-307. doi: 10.1111/bph.12129. Review.


Identification of key residues involved in adrenomedullin binding to the AM1 receptor.

Watkins HA, Au M, Bobby R, Archbold JK, Abdul-Manan N, Moore JM, Middleditch MJ, Williams GM, Brimble MA, Dingley AJ, Hay DL.

Br J Pharmacol. 2013 May;169(1):143-55. doi: 10.1111/bph.12118.


Similarity between class A and class B G-protein-coupled receptors exemplified through calcitonin gene-related peptide receptor modelling and mutagenesis studies.

Vohra S, Taddese B, Conner AC, Poyner DR, Hay DL, Barwell J, Reeves PJ, Upton GJ, Reynolds CA.

J R Soc Interface. 2012 Dec 12;10(79):20120846. doi: 10.1098/rsif.2012.0846. Print 2013 Feb.


Identification of a pathway by which glucose regulates β-catenin signalling via the cAMP/protein kinase A pathway in β-cell models.

Cognard E, Dargaville CG, Hay DL, Shepherd PR.

Biochem J. 2013 Feb 1;449(3):803-11. doi: 10.1042/BJ20121454.


Structure-activity relationships for α-calcitonin gene-related peptide.

Watkins HA, Rathbone DL, Barwell J, Hay DL, Poyner DR.

Br J Pharmacol. 2013 Dec;170(7):1308-22. doi: 10.1111/bph.12072. Review.


Receptor activity-modifying protein-dependent impairment of calcitonin receptor splice variant Δ(1-47)hCT((a)) function.

Qi T, Dong M, Watkins HA, Wootten D, Miller LJ, Hay DL.

Br J Pharmacol. 2013 Feb;168(3):644-57. doi: 10.1111/j.1476-5381.2012.02197.x.


The structure of secretin family GPCR peptide ligands: implications for receptor pharmacology and drug development.

Watkins HA, Au M, Hay DL.

Drug Discov Today. 2012 Sep;17(17-18):1006-14. doi: 10.1016/j.drudis.2012.05.005. Epub 2012 May 11. Review. Erratum in: Drug Discov Today. 2013 Mar;18(5-6):312-3.


The role of glutamic acid 73 in adrenomedullin interactions with rodent AM2 receptors.

Halim A, Hay DL.

Peptides. 2012 Jul;36(1):137-41. doi: 10.1016/j.peptides.2012.04.011. Epub 2012 Apr 21.


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