Mechanism of N-terminal modulation of activity at the melanocortin-4 receptor GPCR.

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المؤلفون: Ersoy, Baran A; Pardo, Leonardo; Zhang, Sumei; Thompson, Darren A; Millhauser, Glenn; Govaerts, Cédric; Vaisse, Christian
المصدر:
Nature Chemical Biology, 8 (8
نوع التسجيلة:
Electronic Resource
الدخول الالكتروني :
http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/146280
http://worldcat.org/search?q=on:EQY+http://difusion-oai.ulb.ac.be/oai/request+DCG_ENTIRE_REPOSITORY+CNTCOLL

معلومة اضافية
- Publisher Information:
  2012-08
- نبذة مختصرة :
  Most of our understanding of G protein-coupled receptor (GPCR) activation has been focused on the direct interaction between diffusible ligands and their seven-transmembrane domains. However, a number of these receptors depend on their extracellular N-terminal domain for ligand recognition and activation. To dissect the molecular interactions underlying both modes of activation at a single receptor, we used the unique properties of the melanocortin-4 receptor (MC4R), a GPCR that shows constitutive activity maintained by its N-terminal domain and is physiologically activated by the peptide α-melanocyte stimulating hormone (αMSH). We find that activation by the N-terminal domain and αMSH relies on different key residues in the transmembrane region. We also demonstrate that agouti-related protein, a physiological antagonist of MC4R, acts as an inverse agonist by inhibiting N terminus-mediated activation, leading to the speculation that a number of constitutively active orphan GPCRs could have physiological inverse agonists as sole regulators.
  Journal Article
  Research Support, N.I.H. Extramural
  Research Support, Non-U.S. Gov't
  SCOPUS: ar.j
  info:eu-repo/semantics/published
- الموضوع:
  Sciences biomédicales; Médecine pathologie humaine; Ingénierie biomédicale; Sciences bio-médicales et agricoles; Agouti-Related Protein -- metabolism; Cell Membrane; Gene Expression Regulation -- physiology; HEK293 Cells; Humans; Models, Molecular; Plasmids; Protein Conformation; Protein Structure, Tertiary; Receptor, Melanocortin, Type 4 -- agonists -- genetics -- metabolism; alpha-MSH -- genetics -- metabolism; info:eu-repo/semantics/article; info:ulb-repo/semantics/articlePeerReview; info:ulb-repo/semantics/openurl/article
- Availability:
  Open access content. Open access content
  1 full-text file(s): info:eu-repo/semantics/restrictedAccess
- Note:
  1 full-text file(s): application/pdf
  English
- Other Numbers:
  EQY oai:dipot.ulb.ac.be:2013/146280
  uri/info:doi/10.1038/nchembio.1008
  uri/info:pii/nchembio.1008
  uri/info:pmid/22729149
  uri/info:scp/84864290272
  uri/info:pmcid/PMC3657613
  https://dipot.ulb.ac.be/dspace/bitstream/2013/146280/4/PMC3657613.pdf
  855620812
- Contributing Source:
  UNIVERSITE LIBRE DE BRUXELLES
  From OAIster®, provided by the OCLC Cooperative.
- الرقم المعرف:
  edsoai.ocn855620812

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Mechanism of N-terminal modulation of activity at the melanocortin-4 receptor GPCR.

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