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Class-B GPCR activation : is ligand helix-capping the key ?
- Source :
- Trends Biochems Sci, Trends Biochems Sci, 2008, 33, pp.314-9, Trends in Biochemical Sciences, Trends in Biochemical Sciences, 2008, 33 (7), pp.314-319. ⟨10.1016/j.tibs.2008.05.001⟩, Trends in Biochemical Sciences, Elsevier, 2008, 33 (7), pp.314-319. ⟨10.1016/j.tibs.2008.05.001⟩
- Publication Year :
- 2008
- Publisher :
- HAL CCSD, 2008.
-
Abstract
- The class B family of G-protein-coupled receptors (GPCRs) regulates essential physiological functions such as exocrine and endocrine secretions, feeding behaviour, metabolism, growth, and neuro- and immuno-modulations. These receptors are activated by endogenous peptide hormones including secretin, glucagon, vasoactive intestinal peptide, corticotropin-releasing factor and parathyroid hormone. We have identified a common structural motif that is encoded in all class B GPCR-ligand N-terminal sequences. We propose that this local structure, a helix N-capping motif, is formed upon receptor binding and constitutes a key element underlying class B GPCR activation. The folded backbone conformation imposed by the capping structure could serve as a template for a rational design of drugs targeting class B GPCRs in several diseases.
- Subjects :
- [ SDV.BBM.BP ] Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biophysics
Vasoactive intestinal peptide
Molecular Sequence Data
Biology
Ligands
Biochemistry
Models, Biological
Protein Structure, Secondary
Secretin
Receptors, G-Protein-Coupled
03 medical and health sciences
[ SDV.BBM.BC ] Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biomolecules [q-bio.BM]
Animals
Humans
Amino Acid Sequence
[SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biochemistry [q-bio.BM]
Structural motif
Receptor
Molecular Biology
030304 developmental biology
G protein-coupled receptor
0303 health sciences
[SDV.BBM.BS]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Structural Biology [q-bio.BM]
030302 biochemistry & molecular biology
Rational design
Ligand (biochemistry)
3. Good health
Protein Structure, Tertiary
[SDV.BBM.BP]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biophysics
Alpha helix
hormones, hormone substitutes, and hormone antagonists
Protein Binding
[ SDV.BBM.BS ] Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biomolecules [q-bio.BM]
Subjects
Details
- Language :
- English
- ISSN :
- 09680004
- Database :
- OpenAIRE
- Journal :
- Trends Biochems Sci, Trends Biochems Sci, 2008, 33, pp.314-9, Trends in Biochemical Sciences, Trends in Biochemical Sciences, 2008, 33 (7), pp.314-319. ⟨10.1016/j.tibs.2008.05.001⟩, Trends in Biochemical Sciences, Elsevier, 2008, 33 (7), pp.314-319. ⟨10.1016/j.tibs.2008.05.001⟩
- Accession number :
- edsair.doi.dedup.....1b6f604275fb0ad1e033b8a47044783f