Structure-Function Relationship of Human Relaxins.

Development of a single-chain peptide agonist of the relaxin-3 receptor using hydrocarbon stapling

K Hojo, MA Hossain, J Tailhades, F Shabanpoor, LLL Wong, EEK Ong-Pålsson, HE Kastman, S Ma, AL Gundlach, KJ Rosengren, JD Wade, RAD 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

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

2016-01-18

© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.The inhibition of the G protein-coupled receptor, relaxin family peptide recepto..

Synthetic covalently linked dimeric form of h2 relaxin retains native RXFP1 activity and has improved in vitro serum stability

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

2015-01-22

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

CM Smith, BE Chua, C Zhang, AW Walker, M Haidar, D Hawkes, F Shabanpoor, MA Hossain, JD Wade, KJ Rosengren, AL Gundlach

2014-07-15

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

Relaxin and its role in fibrotic diseases

LJ Chan, CS Samuel, F Separovic, MA Hossain, JD Wade

2014-01-01

Relaxin is a member of the insulin family of peptides. It is produced in the corpus luteum and/or placenta during pregnancy in mam..

Minimum active structure of insulin-like peptide 5

A Belgi, RAD Bathgate, M Kocan, N Patil, S Zhang, GW Tregear, JD Wade, MA 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

F Shabanpoor, RAD Bathgate, JD Wade, MA 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..

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

LJ Chan, CM Smith, BE Chua, F Lin, RAD Bathgate, F Separovic, AL Gundlach, MA Hossain, JD Wade

2013-12-06

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

J Karas, F Shabanpoor, MA Hossain, J Gardiner, F Separovic, JD Wade, DB Scanlon

2013-12-06

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

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

MA Hossain, CM Smith, PJ Ryan, E Büchler, RAD Bathgate, AL Gundlach, JD 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

PJ Ryan, E Büchler, F Shabanpoor, MA Hossain, JD Wade, AJ Lawrence, AL 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

F Shabanpoor, MA Hossain, F Lin, JD Wade

2013-01-01

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

Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin

LJ Chan, KJ Rosengren, SL Layfield, RAD Bathgate, F Separovic, CS Samuel, MA Hossain, JD 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

VB Nair, CS Samuel, F Separovic, MA Hossain, JD 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

WJ Zhang, X Luo, YL Liu, XX Shao, JD Wade, RAD Bathgate, ZY 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

MA Hossain, JD Wade, RAD 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

F Shabanpoor, RAD Bathgate, A Belgi, LJ Chan, VB Nair, JD Wade, MA 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

F Shabanpoor, M Akhter Hossain, PJ Ryan, A Belgi, S Layfield, M Kocan, S Zhang, CS Samuel, AL Gundlach, RAD Bathgate, F Separovic, JD 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

MA Hossain, KJ Rosengren, CS Samuel, F Shabanpoor, LJ Chan, RAD Bathgate, JD Wade

2011-10-28

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

Structure and function relationship of murine insulin-like peptide 5 (INSL5): Free C-terminus is essential for RXFP4 receptor binding and activation

A Belgi, MA Hossain, F Shabanpoor, L Chan, S Zhang, RAD Bathgate, GW Tregear, JD Wade

2011-10-04

Insulin-like peptide 5 (INSL5) is a member of insulin/relaxin superfamily of peptides. It has recently been identified as the cogn..

H3 relaxin demonstrates antifibrotic properties via the RXFP1 receptor

MA Hossain, B Chow Suet Man, C Zhao, Q Xu, XJ Du, JD Wade, CS Samuel

2011-03-01

Human gene 3 (H3) relaxin is the most recently discovered member of the relaxin peptide family and can potentially bind all of the..

The relaxin peptide family - structure, function and clinical applications

LJ Chan, MA Hossain, CS Samuel, F Separovic, JD Wade

2011-03-01

The relaxin peptide family in humans consists of seven members, relaxin-1, -2 and -3 and insulin-like (INSL) peptides 3, 4, 5 and ..

The roles of the A- and B-chains of human relaxin-2 and -3 on their biological activity

MA Hossain, JD Wade

2010-12-01

Two members of the human insulin/relaxin superfamily, relaxins-2 and 3 (H2 and H3 respectively), are separated by nearly 75 years ..

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

X Luo, YL Liu, S Layfield, XX Shao, RAD Bathgate, JD Wade, ZY 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

X Luo, RAD Bathgate, WJ Zhang, YL Liu, XX Shao, JD Wade, ZY 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

SY Kwak, BE Forbes, YS Lee, A Belgi, JD Wade, MA 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

MA Hossain, CS Samuel, C Binder, TD Hewitson, GW Tregear, JD Wade, RAD 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

LM Haugaard-Jönsson, MA Hossain, NL Daly, DJ Craik, JD Wade, KJ 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

MA Hossain, KJ Rosengren, S Zhang, RAD Bathgate, GW Tregear, BJ Van Lierop, AJ Robinson, JD Wade

2009-04-15

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

GW Tregear, RAD Bathgate, MA Hossain, F Lin, S Zhang, F Shabanpoor, DJ Scott, S Ma, AL Gundlach, CS Samuel, JD 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(BΔ23-27)R/I5

MA Hossain, RAD Bathgate, KJ Rosengren, F Shabanpoor, S Zhang, F Lin, GW Tregear, JD 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..