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Colokinetic effect of an insulin-like peptide 5-related agonist of the RXFP4 receptor.

Diwakarla S, Bathgate RAD, Zhang X, Hossain MA, Furness JB.

Neurogastroenterol Motil. 2020 Jan 27:e13796. doi: 10.1111/nmo.13796. [Epub ahead of print]


Targeted viral vector transduction of relaxin-3 neurons in the rat nucleus incertus using a novel cell-type specific promoter.

Wykes AD, Ma S, Bathgate RAD, Gundlach AL.

IBRO Rep. 2019 Dec 13;8:1-10. doi: 10.1016/j.ibror.2019.11.006. eCollection 2020 Jun.


Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.

Praveen P, Bathgate RAD, Hossain MA.

Sci Rep. 2019 Nov 28;9(1):17828. doi: 10.1038/s41598-019-53707-z.


Coatings Releasing the Relaxin Peptide Analogue B7-33 Reduce Fibrotic Encapsulation.

Welch NG, Mukherjee S, Hossain MA, Praveen P, Werkmeister JA, Wade JD, Bathgate RAD, Winkler DA, Thissen H.

ACS Appl Mater Interfaces. 2019 Dec 11;11(49):45511-45519. doi: 10.1021/acsami.9b17859. Epub 2019 Dec 2.


AT1R-AT2R-RXFP1 Functional Crosstalk in Myofibroblasts: Impact on the Therapeutic Targeting of Renal and Cardiac Fibrosis.

Chow BSM, Kocan M, Shen M, Wang Y, Han L, Chew JY, Wang C, Bosnyak S, Mirabito-Colafella KM, Barsha G, Wigg B, Johnstone EKM, Hossain MA, Pfleger KDG, Denton KM, Widdop RE, Summers RJ, Bathgate RAD, Hewitson TD, Samuel CS.

J Am Soc Nephrol. 2019 Nov;30(11):2191-2207. doi: 10.1681/ASN.2019060597. Epub 2019 Sep 11.


Using the novel HiBiT tag to label cell surface relaxin receptors for BRET proximity analysis.

Hoare BL, Kocan M, Bruell S, Scott DJ, Bathgate RAD.

Pharmacol Res Perspect. 2019 Jul 30;7(4):e00513. doi: 10.1002/prp2.513. eCollection 2019 Aug.


Familial bilateral cryptorchidism is caused by recessive variants in RXFP2.

Ayers K, Kumar R, Robevska G, Bruell S, Bell K, Malik MA, Bathgate RA, Sinclair A.

J Med Genet. 2019 Nov;56(11):727-733. doi: 10.1136/jmedgenet-2019-106203. Epub 2019 Jun 5.


An apically located hybrid guanylate cyclase-ATPase is critical for the initiation of Ca2+ signaling and motility in Toxoplasma gondii.

Yang L, Uboldi AD, Seizova S, Wilde ML, Coffey MJ, Katris NJ, Yamaryo-Botté Y, Kocan M, Bathgate RAD, Stewart RJ, McConville MJ, Thompson PE, Botté CY, Tonkin CJ.

J Biol Chem. 2019 May 31;294(22):8959-8972. doi: 10.1074/jbc.RA118.005491. Epub 2019 Apr 16.


Expression and Purification of a Functional E. coli 13CH3-Methionine-Labeled Thermostable Neurotensin Receptor 1 Variant for Solution NMR Studies.

Bumbak F, Bathgate RAD, Scott DJ, Gooley PR.

Methods Mol Biol. 2019;1947:31-55. doi: 10.1007/978-1-4939-9121-1_3.


Chronic activation of the relaxin-3 receptor on GABA neurons in rat ventral hippocampus promotes anxiety and social avoidance.

Rytova V, Ganella DE, Hawkes D, Bathgate RAD, Ma S, Gundlach AL.

Hippocampus. 2019 Oct;29(10):905-920. doi: 10.1002/hipo.23089. Epub 2019 Mar 19.


Diazepam is not a direct allosteric modulator of α1-adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase-4.

Williams LM, He X, Vaid TM, Abdul-Ridha A, Whitehead AR, Gooley PR, Bathgate RAD, Williams SJ, Scott DJ.

Pharmacol Res Perspect. 2018 Dec 26;7(1):e00455. doi: 10.1002/prp2.455. eCollection 2019 Feb.


Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis.

Hoare BL, Bruell S, Sethi A, Gooley PR, Lew MJ, Hossain MA, Inoue A, Scott DJ, Bathgate RAD.

iScience. 2019 Jan 25;11:93-113. doi: 10.1016/j.isci.2018.12.004. Epub 2018 Dec 10.


Understanding relaxin signalling at the cellular level.

Valkovic AL, Bathgate RA, Samuel CS, Kocan M.

Mol Cell Endocrinol. 2019 May 1;487:24-33. doi: 10.1016/j.mce.2018.12.017. Epub 2018 Dec 25. Review.


Real-time examination of cAMP activity at relaxin family peptide receptors using a BRET-based biosensor.

Valkovic AL, Leckey MB, Whitehead AR, Hossain MA, Inoue A, Kocan M, Bathgate RAD.

Pharmacol Res Perspect. 2018 Sep 24;6(5):e00432. doi: 10.1002/prp2.432. eCollection 2018 Oct.


Binding conformation and determinants of a single-chain peptide antagonist at the relaxin-3 receptor RXFP3.

Haugaard-Kedström LM, Lee HS, Jones MV, Song A, Rathod V, Hossain MA, Bathgate RAD, Rosengren KJ.

J Biol Chem. 2018 Oct 12;293(41):15765-15776. doi: 10.1074/jbc.RA118.002611. Epub 2018 Aug 21.


Distinct but overlapping binding sites of agonist and antagonist at the relaxin family peptide 3 (RXFP3) receptor.

Wong LLL, Scott DJ, Hossain MA, Kaas Q, Rosengren KJ, Bathgate RAD.

J Biol Chem. 2018 Oct 12;293(41):15777-15789. doi: 10.1074/jbc.RA118.002645. Epub 2018 Aug 21.


Gram scale preparation of clozapine N-oxide (CNO), a synthetic small molecule actuator for muscarinic acetylcholine DREADDs.

van der Peet PL, Gunawan C, Abdul-Ridha A, Ma S, Scott DJ, Gundlach AL, Bathgate RAD, White JM, Williams SJ.

MethodsX. 2018 Mar 23;5:257-267. doi: 10.1016/j.mex.2018.03.003. eCollection 2018.


Optimization and 13CH3 methionine labeling of a signaling competent neurotensin receptor 1 variant for NMR studies.

Bumbak F, Keen AC, Gunn NJ, Gooley PR, Bathgate RAD, Scott DJ.

Biochim Biophys Acta Biomembr. 2018 Jun;1860(6):1372-1383. doi: 10.1016/j.bbamem.2018.03.020. Epub 2018 Mar 26.


Determinants of Ligand Subtype-Selectivity at α1A-Adrenoceptor Revealed Using Saturation Transfer Difference (STD) NMR.

Yong KJ, Vaid TM, Shilling PJ, Wu FJ, Williams LM, Deluigi M, Plückthun A, Bathgate RAD, Gooley PR, Scott DJ.

ACS Chem Biol. 2018 Apr 20;13(4):1090-1102. doi: 10.1021/acschembio.8b00191. Epub 2018 Mar 22.


INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells.

Ang SY, Evans BA, Poole DP, Bron R, DiCello JJ, Bathgate RAD, Kocan M, Hutchinson DS, Summers RJ.

J Mol Endocrinol. 2018 Apr;60(3):213-224. doi: 10.1530/JME-17-0152.


The relaxin receptor as a therapeutic target - perspectives from evolution and drug targeting.

Bathgate RAD, Kocan M, Scott DJ, Hossain MA, Good SV, Yegorov S, Bogerd J, Gooley PR.

Pharmacol Ther. 2018 Jul;187:114-132. doi: 10.1016/j.pharmthera.2018.02.008. Epub 2018 Feb 17. Review.


A Novel Ultra-Stable, Monomeric Green Fluorescent Protein For Direct Volumetric Imaging of Whole Organs Using CLARITY.

Scott DJ, Gunn NJ, Yong KJ, Wimmer VC, Veldhuis NA, Challis LM, Haidar M, Petrou S, Bathgate RAD, Griffin MDW.

Sci Rep. 2018 Jan 12;8(1):667. doi: 10.1038/s41598-017-18045-y.


Challenges in the design of insulin and relaxin/insulin-like peptide mimetics.

Hossain MA, Bathgate RAD.

Bioorg Med Chem. 2018 Jun 1;26(10):2827-2841. doi: 10.1016/j.bmc.2017.09.030. Epub 2017 Sep 27. Review.


Distinct activation modes of the Relaxin Family Peptide Receptor 2 in response to insulin-like peptide 3 and relaxin.

Bruell S, Sethi A, Smith N, Scott DJ, Hossain MA, Wu QP, Guo ZY, Petrie EJ, Gooley PR, Bathgate RAD.

Sci Rep. 2017 Jun 12;7(1):3294. doi: 10.1038/s41598-017-03638-4.


ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

Kocan M, Sarwar M, Ang SY, Xiao J, Marugan JJ, Hossain MA, Wang C, Hutchinson DS, Samuel CS, Agoulnik AI, Bathgate RAD, Summers RJ.

Sci Rep. 2017 Jun 7;7(1):2968. doi: 10.1038/s41598-017-02916-5.


B7-33 replicates the vasoprotective functions of human relaxin-2 (serelaxin).

Marshall SA, O'Sullivan K, Ng HH, Bathgate RAD, Parry LJ, Hossain MA, Leo CH.

Eur J Pharmacol. 2017 Jul 15;807:190-197. doi: 10.1016/j.ejphar.2017.05.005. Epub 2017 May 3.


Characterisation of a cell-free synthesised G-protein coupled receptor.

Shilling PJ, Bumbak F, Scott DJ, Bathgate RAD, Gooley PR.

Sci Rep. 2017 Apr 24;7(1):1094. doi: 10.1038/s41598-017-01227-z.


Relaxin-3 inputs target hippocampal interneurons and deletion of hilar relaxin-3 receptors in "floxed-RXFP3" mice impairs spatial memory.

Haidar M, Guèvremont G, Zhang C, Bathgate RAD, Timofeeva E, Smith CM, Gundlach AL.

Hippocampus. 2017 May;27(5):529-546. doi: 10.1002/hipo.22709. Epub 2017 Jan 31.


Relaxin family peptides: structure-activity relationship studies.

Patil NA, Rosengren KJ, Separovic F, Wade JD, Bathgate RAD, Hossain MA.

Br J Pharmacol. 2017 May;174(10):950-961. doi: 10.1111/bph.13684. Epub 2017 Jan 19. Review. Erratum in: Br J Pharmacol. 2017 Dec;174(24):4836.


Promise and Limitations of Relaxin-based Therapies in Chronic Fibrotic Lung Diseases.

Royce SG, Bathgate RA, Samuel CS.

Am J Respir Crit Care Med. 2016 Dec 1;194(11):1434-1435. No abstract available.


The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.

Ang SY, Hutchinson DS, Evans BA, Hossain MA, Patil N, Bathgate RA, Kocan M, Summers RJ.

Naunyn Schmiedebergs Arch Pharmacol. 2017 Jan;390(1):105-111. doi: 10.1007/s00210-016-1321-8. Epub 2016 Nov 26.


Development of a Single-Chain Peptide Agonist of the Relaxin-3 Receptor Using Hydrocarbon Stapling.

Hojo K, Hossain MA, Tailhades J, Shabanpoor F, Wong LL, Ong-Pålsson EE, Kastman HE, Ma S, Gundlach AL, Rosengren KJ, Wade JD, Bathgate RA.

J Med Chem. 2016 Aug 25;59(16):7445-56. doi: 10.1021/acs.jmedchem.6b00265. Epub 2016 Aug 8.


Knockdown of corticotropin-releasing factor 1 receptors in the ventral tegmental area enhances conditioned fear.

Chen NA, Ganella DE, Bathgate RAD, Chen A, Lawrence AJ, Kim JH.

Eur Neuropsychopharmacol. 2016 Sep;26(9):1533-1540. doi: 10.1016/j.euroneuro.2016.06.002. Epub 2016 Jul 7.


Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor.

Ang SY, Hutchinson DS, Patil N, Evans BA, Bathgate RAD, Halls ML, Hossain MA, Summers RJ, Kocan M.

Br J Pharmacol. 2017 May;174(10):1077-1089. doi: 10.1111/bph.13522. Epub 2016 Jul 13. Erratum in: Br J Pharmacol. 2017 Dec;174(24):4836.


A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1.

Hossain MA, Kocan M, Yao ST, Royce SG, Nair VB, Siwek C, Patil NA, Harrison IP, Rosengren KJ, Selemidis S, Summers RJ, Wade JD, Bathgate RAD, Samuel CS.

Chem Sci. 2016 Jun 1;7(6):3805-3819. doi: 10.1039/c5sc04754d. Epub 2016 Feb 26.


Nucleus incertus promotes cortical desynchronization and behavioral arousal.

Ma S, Allocca G, Ong-Pålsson EK, Singleton CE, Hawkes D, McDougall SJ, Williams SJ, Bathgate RA, Gundlach AL.

Brain Struct Funct. 2017 Jan;222(1):515-537. doi: 10.1007/s00429-016-1230-0. Epub 2016 May 20.


The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1.

Sethi A, Bruell S, Patil N, Hossain MA, Scott DJ, Petrie EJ, Bathgate RAD, Gooley PR.

Nat Commun. 2016 Apr 18;7:11344. doi: 10.1038/ncomms11344.


Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.

Patil NA, Hughes RA, Rosengren KJ, Kocan M, Ang SY, Tailhades J, Separovic F, Summers RJ, Grosse J, Wade JD, Bathgate RA, Hossain MA.

J Med Chem. 2016 Mar 10;59(5):2118-25. doi: 10.1021/acs.jmedchem.5b01786. Epub 2016 Feb 12.


The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity.

Patil NA, Bathgate RAD, Kocan M, Ang SY, Tailhades J, Separovic F, Summers R, Grosse J, Hughes RA, Wade JD, Hossain MA.

Amino Acids. 2016 Apr;48(4):987-992. doi: 10.1007/s00726-015-2144-5. Epub 2015 Dec 11.


Native Chemical Ligation to Minimize Aspartimide Formation during Chemical Synthesis of Small LDLa Protein.

Tailhades J, Sethi A, Petrie EJ, Gooley PR, Bathgate RA, Wade JD, Hossain MA.

Chemistry. 2016 Jan 18;22(3):1146-51. doi: 10.1002/chem.201503599. Epub 2015 Nov 27.


Enhanced serelaxin signalling in co-cultures of human primary endothelial and smooth muscle cells.

Sarwar M, Samuel CS, Bathgate RA, Stewart DR, Summers RJ.

Br J Pharmacol. 2016 Feb;173(3):484-96. doi: 10.1111/bph.13371. Epub 2016 Jan 15.


In a Class of Their Own - RXFP1 and RXFP2 are Unique Members of the LGR Family.

Petrie EJ, Lagaida S, Sethi A, Bathgate RA, Gooley PR.

Front Endocrinol (Lausanne). 2015 Sep 7;6:137. doi: 10.3389/fendo.2015.00137. eCollection 2015. Review.


Chemically synthesized dicarba H2 relaxin analogues retain strong RXFP1 receptor activity but show an unexpected loss of in vitro serum stability.

Hossain MA, Haugaard-Kedström LM, Rosengren KJ, Bathgate RA, Wade JD.

Org Biomol Chem. 2015 Nov 28;13(44):10895-903. doi: 10.1039/c5ob01539a. Epub 2015 Sep 14.


Activation of Relaxin Family Receptor 1 from Different Mammalian Species by Relaxin Peptide and Small-Molecule Agonist ML290.

Huang Z, Myhr C, Bathgate RA, Ho BA, Bueno A, Hu X, Xiao J, Southall N, Barnaeva E, Agoulnik IU, Marugan JJ, Ferrer M, Agoulnik AI.

Front Endocrinol (Lausanne). 2015 Aug 17;6:128. doi: 10.3389/fendo.2015.00128. eCollection 2015.


Spatial Learning Requires mGlu5 Signalling in the Dorsal Hippocampus.

Tan SZ, Ganella DE, Dick AL, Duncan JR, Ong-Palsson E, Bathgate RA, Kim JH, Lawrence AJ.

Neurochem Res. 2015 Jun;40(6):1303-10. doi: 10.1007/s11064-015-1595-0. Epub 2015 May 10.


Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3.

Haugaard-Kedström LM, Wong LL, Bathgate RA, Rosengren KJ.

Amino Acids. 2015 Jun;47(6):1267-71. doi: 10.1007/s00726-015-1961-x. Epub 2015 Mar 20.


Relaxin-2 does not ameliorate nephropathy in an experimental model of type-1 diabetes.

Dschietzig TB, Krause-Relle K, Hennequin M, von Websky K, Rahnenführer J, Ruppert J, Grön HJ, Armbruster FP, Bathgate RA, Aschenbach JR, Forssmann WG, Hocher B.

Kidney Blood Press Res. 2015;40(1):77-88.


Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability.

Nair VB, Bathgate RA, Separovic F, Samuel CS, Hossain MA, Wade JD.

Biomed Res Int. 2015;2015:731852. doi: 10.1155/2015/731852. Epub 2015 Jan 22.


Solution structure, aggregation behavior, and flexibility of human relaxin-2.

Haugaard-Kedström LM, Hossain MA, Daly NL, Bathgate RA, Rinderknecht E, Wade JD, Craik DJ, Rosengren KJ.

ACS Chem Biol. 2015 Mar 20;10(3):891-900. doi: 10.1021/cb500918v. Epub 2015 Jan 15.


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