Novel approaches leading towards peptide GPCR de-orphanisation

Research output: Contribution to journal › Review › Research › peer-review

Standard

Novel approaches leading towards peptide GPCR de-orphanisation. / Hauser, Alexander S.; Gloriam, David E.; Bräuner-Osborne, Hans; Foster, Simon R.

In: British Journal of Pharmacology, Vol. 177, No. 5, 01.03.2020, p. 961-968.

Research output: Contribution to journal › Review › Research › peer-review

Harvard

Hauser, AS, Gloriam, DE, Bräuner-Osborne, H & Foster, SR 2020, 'Novel approaches leading towards peptide GPCR de-orphanisation', British Journal of Pharmacology, vol. 177, no. 5, pp. 961-968. https://doi.org/10.1111/bph.14950

APA

Hauser, A. S., Gloriam, D. E., Bräuner-Osborne, H., & Foster, S. R. (2020). Novel approaches leading towards peptide GPCR de-orphanisation. British Journal of Pharmacology, 177(5), 961-968. https://doi.org/10.1111/bph.14950

Vancouver

Hauser AS, Gloriam DE, Bräuner-Osborne H, Foster SR. Novel approaches leading towards peptide GPCR de-orphanisation. British Journal of Pharmacology. 2020 Mar 1;177(5):961-968. https://doi.org/10.1111/bph.14950

Author

Hauser, Alexander S. ; Gloriam, David E. ; Bräuner-Osborne, Hans ; Foster, Simon R. / Novel approaches leading towards peptide GPCR de-orphanisation. In: British Journal of Pharmacology. 2020 ; Vol. 177, No. 5. pp. 961-968.

Bibtex

@article{89399d2629ed4e2fa71ad26e8c3aaa85,
title = "Novel approaches leading towards peptide GPCR de-orphanisation",
abstract = "The discovery of novel ligands for orphan GPCRs has profoundly affected our understanding of human biology, opening new opportunities for research, and ultimately for therapeutic development. Accordingly, much effort has been directed towards the remaining orphan receptors, yet the rate of GPCR de-orphanisation has slowed in recent years. Here, we briefly review contemporary methodologies of de-orphanisation and then highlight our recent integrated computational and experimental approach for discovery of novel peptide ligands for orphan GPCRs. We identified putative endogenous peptide ligands and found peptide receptor sequence and structural characteristics present in selected orphan receptors. With comprehensive pharmacological screening using three complementary assays, we discovered novel pairings of 17 peptides with five different orphan GPCRs and revealed potential additional ligands for nine peptide GPCRs. These promising findings lay the foundation for future studies on these peptides and receptors to characterise their roles in human physiology and disease.",
author = "Hauser, {Alexander S.} and Gloriam, {David E.} and Hans Br{\"a}uner-Osborne and Foster, {Simon R.}",
year = "2020",
month = mar,
day = "1",
doi = "10.1111/bph.14950",
language = "English",
volume = "177",
pages = "961--968",
journal = "British Journal of Pharmacology",
issn = "0007-1188",
publisher = "Wiley",
number = "5",

}

RIS

TY - JOUR

T1 - Novel approaches leading towards peptide GPCR de-orphanisation

AU - Hauser, Alexander S.

AU - Gloriam, David E.

AU - Bräuner-Osborne, Hans

AU - Foster, Simon R.

PY - 2020/3/1

Y1 - 2020/3/1

N2 - The discovery of novel ligands for orphan GPCRs has profoundly affected our understanding of human biology, opening new opportunities for research, and ultimately for therapeutic development. Accordingly, much effort has been directed towards the remaining orphan receptors, yet the rate of GPCR de-orphanisation has slowed in recent years. Here, we briefly review contemporary methodologies of de-orphanisation and then highlight our recent integrated computational and experimental approach for discovery of novel peptide ligands for orphan GPCRs. We identified putative endogenous peptide ligands and found peptide receptor sequence and structural characteristics present in selected orphan receptors. With comprehensive pharmacological screening using three complementary assays, we discovered novel pairings of 17 peptides with five different orphan GPCRs and revealed potential additional ligands for nine peptide GPCRs. These promising findings lay the foundation for future studies on these peptides and receptors to characterise their roles in human physiology and disease.

AB - The discovery of novel ligands for orphan GPCRs has profoundly affected our understanding of human biology, opening new opportunities for research, and ultimately for therapeutic development. Accordingly, much effort has been directed towards the remaining orphan receptors, yet the rate of GPCR de-orphanisation has slowed in recent years. Here, we briefly review contemporary methodologies of de-orphanisation and then highlight our recent integrated computational and experimental approach for discovery of novel peptide ligands for orphan GPCRs. We identified putative endogenous peptide ligands and found peptide receptor sequence and structural characteristics present in selected orphan receptors. With comprehensive pharmacological screening using three complementary assays, we discovered novel pairings of 17 peptides with five different orphan GPCRs and revealed potential additional ligands for nine peptide GPCRs. These promising findings lay the foundation for future studies on these peptides and receptors to characterise their roles in human physiology and disease.

U2 - 10.1111/bph.14950

DO - 10.1111/bph.14950

M3 - Review

C2 - 31863461

AN - SCOPUS:85078903732

VL - 177

SP - 961

EP - 968

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

SN - 0007-1188

IS - 5

ER -

ID: 239156704