Structure-function relationship of human relaxins.

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

Keiko Hojo, Mohammed Akhter Hossain, Julien Tailhades, Fazel Shabanpoor, Lilian LL Wong, Emma EK Ong-Palsson, Hanna E Kastman, Sherie Ma, Andrew L Gundlach, K Johan Rosengren, John D Wade, Ross AD Bathgate

2016-08-25

Structure-activity studies of the insulin superfamily member, relaxin-3, have shown that its G protein-coupled receptor (RXFP3) bi..

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

Julien Tailhades, Ashish Sethi, Emma J Petrie, Paul R Gooley, Ross A Bathgate, John D Wade, Mohammed A Hossain

2016-01-18

The inhibition of the G protein-coupled receptor, relaxin family peptide receptor 1 (RXFP1), by a small LDLa protein may be a pote..

Synthetic Covalently Linked Dimeric Form of H2 Relaxin Retains Native RXFP1 Activity and Has Improved In Vitro Serum Stability

Vinojini B Nair, Ross AD Bathgate, Frances Separovic, Chrishan S Samuel, Mohammed Akhter Hossain, John D Wade

2015-01-01

Human (H2) relaxin is a two-chain peptide member of the insulin superfamily and possesses potent pleiotropic roles including regul..

Central injection of relaxin-3 receptor (RXFP3) antagonist peptides reduces motivated food seeking and consumption in C57BL/6J mice

Craig M Smith, Berenice E Chua, Cary Zhang, Andrew W Walker, Mouna Haidar, David Hawkes, Fazel Shabanpoor, Mohammad Akhter Hossain, John D Wade, K Johan Rosengren, Andrew L Gundlach

2014-07-15

Behavioural arousal in mammals is regulated by various interacting central monoamine- and peptide-neurotransmitter/receptor system..

Minimum Active Structure of Insulin-like Peptide 5

Alessia Begi, Ross AD Bathgate, Martina Kocan, Nitin Patil, Suode Zhang, Geoffrey W Tregear, John D Wade, Mohammed Akhter Hossain

2013-12-12

Insulin-like peptide 5 (INSL5) is a complex two-chain peptide hormone constrained by three disulfide bonds in a pattern identical ..

C-Terminus of the B-Chain of Relaxin-3 Is Important for Receptor Activity

Fazel Shabanpoor, Ross AD Bathgate, John D Wade, Mohammed Akhter Hossain

2013-12-11

Human relaxin-3 is a neuropeptide that is structurally similar to human insulin with two chains (A and B) connected by three disul..

Chemical synthesis and orexigenic activity of rat/mouse relaxin-3

Mohammed Akhter Hossain, Craig M Smith, Philip J Ryan, Elena Buechler, Ross AD Bathgate, Andrew L Gundlach, John D Wade

2013-06-01

The insulin-like peptide, relaxin-3 was first identified just a decade ago via a genomic database search and is now recognized to ..

Central relaxin-3 receptor (RXFP3) activation decreases anxiety- and depressive-like behaviours in the rat

Philip J Ryan, Elena Buechler, Fazel Shabanpoor, Mohammed Akhter Hossain, John D Wade, Andrew J Lawrence, Andrew L Gundlach

2013-05-01

Relaxin-3 is a recently discovered neuropeptide and the results of earlier anatomical and pharmacological studies suggest it plays..

Sequential Formation of Regioselective Disulfide Bonds in Synthetic Peptides with Multiple Disulfide Bonds

Fazel Shabanpoor, Mohammed Akhter Hossain, Feng Lin, John D Wade

2013-01-01

Numerous methods have been developed for the formation of disulfide bonds in recombinant DNA-derived and chemically synthesized pe..

Synthesis of fluorescent analogs of relaxin family peptides and their preliminary in vitro and in vivo characterization

Linda J Chan, Craig M Smith, Berenice E Chua, Feng Lin, Ross AD Bathgate, Frances Separovic, Andrew L Gundlach, Mohammed Akhter Hossain, John D Wade

2013-01-01

Relaxin, a heterodimeric polypeptide hormone, is a key regulator of collagen metabolism and multiple vascular control pathways in ..

Total chemical synthesis of a heterodimeric interchain bis-lactam-linked Peptide: application to an analogue of human insulin-like Peptide 3.

John Karas, Fazel Shabanpoor, Mohammed Akhter Hossain, James Gardiner, Frances Separovic, John D Wade, Denis B Scanlon

2013-01-01

Nonreducible cystine isosteres represent important peptide design elements in that they can maintain a near-native tertiary confor..

Identification of Key Residues Essential for the Structural Fold and Receptor Selectivity within the A-chain of Human Gene-2 (H2) Relaxin

Linda J Chan, K Johan Rosengren, Sharon L Layfield, Ross AD Bathgate, Frances Separovic, Chrishan S Samuel, Mohammed A Hossain, John D Wade

2012-11-30

Human gene-2 (H2) relaxin is currently in Phase III clinical trials for the treatment of acute heart failure. It is a 53-amino aci..

Human relaxin-2: historical perspectives and role in cancer biology

Vinojini B Nair, Chrishan S Samuel, Frances Separovic, Mohammed Akhter Hossain, John D Wade

2012-09-01

One of the most recognised and studied family of peptide hormones is the insulin superfamily. Within this family is the relaxin su..

Site-specific DOTA/europium-labeling of recombinant human relaxin-3 for receptor-ligand interaction studies

Wei-Jie Zhang, Xiao Luo, Ya-Li Liu, Xiao-Xia Shao, John D Wade, Ross AD Bathgate, Zhan-Yun Guo

2012-08-01

Relaxin-3 (also known as INSL7) is a recently identified neuropeptide belonging to the insulin/relaxin superfamily. It has putativ..

Chimeric relaxin peptides highlight the role of the A-chain in the function of H2 relaxin

Mohammed Akhter Hossain, John D Wade, Ross AD Bathgate

2012-05-01

Human gene-2 (H2) relaxin is a member of the insulin-relaxin peptide superfamily. Because of the potential clinical applications o..

Site-specific conjugation of a lanthanide chelator and its effects on the chemical synthesis and receptor binding affinity of human relaxin-2 hormone

Fazel Shabanpoor, Ross AD Bathgate, Alessia Belgi, Linda J Chan, Vinojini B Nair, John D Wade, Mohammed Akhter Hossain

2012-04-06

Diethylenetriamine pentaacetic acid (DTPA) is a popular chelator agent for enabling the labeling of peptides for their use in stru..

Minimization of Human Relaxin-3 Leading to High-Affinity Analogues with Increased Selectivity for Relaxin-Family Peptide 3 Receptor (RXFP3) over RXFP1

Fazel Shabanpoor, Mohammad Alchter Hossain, Philip J Ryan, Alessia Belgi, Sharon Layfield, Martina Kocan, Suode Zhang, Chrishan S Samuel, Andrew L Gundlach, Ross AD Bathgate, Frances Separovic, John D Wade

2012-02-23

Relaxin-3 is a neuropeptide that is implicated in the regulation of stress responses and memory. The elucidation of its precise ph..

The Minimal Active Structure of Human Relaxin-2

Mohammed Akhter Hossain, K Johan Rosengren, Chrishan S Samuel, Fazel Shabanpoor, Linda J Chan, Ross AD Bathgate, John D Wade

2011-10-28

H2 relaxin is a peptide hormone associated with a number of therapeutically relevant physiological effects, including regulation o..

A simple approach for the preparation of mature human relaxin-3

Xiao Luo, Ya-Li Liu, Sharon Layfield, Xiao-Xia Shao, Ross AD Bathgate, John D Wade, Zhan-Yun Guo

2010-11-01

Relaxin-3 (also known as INSL7) is the most recently identified member of the insulin-like family. It is predominantly expressed i..

Design and recombinant expression of insulin-like peptide 5 precursors and the preparation of mature human INSL5

Xiao Luo, Ross AD Bathgate, Wei-Jie Zhang, Ya-Li Liu, Xiao-Xia Shao, John D Wade, Zhan-Yun Guo

2010-11-01

Insulin-like peptide 5 (INSL5) is a recently identified insulin superfamily member. Although it binds to and activates the G-prote..

Solid Phase Synthesis of an Analogue of Insulin, A0:R glargine, That Exhibits Decreased Mitogenic Activity

Seon-Yeong Kwak, Briony E Forbes, Yoon-Sik Lee, Alessia Belgi, John D Wade, Mohammed Akhter Hossain

2010-09-01

Numerous analogues of insulin have been prepared over the past three decades for use in diabetic therapy. However, only two long-a..

The chemically synthesized human relaxin-2 analog, B-R13/17K H2, is an RXFP1 antagonist

Mohammed Akhter Hossain, Chrishan S Samuel, Claudia Binder, Tim D Hewitson, Geoffrey W Tregear, John D Wade, Ross AD Bathgate

2010-07-01

Relaxin is a pleiotropic hormone which exerts its biological functions through its G-protein coupled receptor, RXFP1. While relaxi..

Structure of human insulin-like peptide 5 and characterization of conserved hydrogen bonds and electrostatic interactions within the relaxin framework

Linda M Haugaard-Jonsson, Mohammed Akhter Hossain, Norelle L Daly, David J Craik, John D Wade, K Johan Rosengren

2009-05-01

INSL5 (insulin-like peptide 5) is a two-chain peptide hormone related to insulin and relaxin. It was recently discovered through s..

Solid phase synthesis and structural analysis of novel A-chain dicarba analogs of human relaxin-3 (INSL7) that exhibit full biological activity

Mohammed Akhter Hossain, K Johan Rosengren, Suode Zhang, Ross AD Bathgate, Geoffrey W Tregear, Bianca J van Lierop, Andrea J Robinson, John D Wade

2009-01-01

Replacement of disulfide bonds with non-reducible isosteres can be a useful means of increasing the in vivo stability of a protein..

Structure and Activity in the Relaxin Family of Peptides

Geoffrey W Tregear, Ross AD Bathgate, Mohammed Akhter Hossain, Feng Lin, Suode Zhang, Fazel Shabanpoor, Daniel J Scott, Sherie Ma, Andrew L Gundlach, Chrishan S Samuel, John D Wade

2009-01-01

The availability of improved peptide synthesis procedures, convenient and sensitive assays for receptor binding and activation, to..

The Structural and Functional Role of the B-chain C-terminal Arginine in the Relaxin-3 Peptide Antagonist, R3(B Delta 23-27)R/I5

Mohammed Akhter Hossain, Ross AD Bathgate, K Johan Rosengren, Fazel Shabanpoor, Suode Zhang, Feng Lin, Geoffrey W Tregear, John D Wade

2009-01-01

Relaxin-3, a member of the insulin superfamily, is involved in regulating stress and feeding behavior. It is highly expressed in t..