The Resource Constitutive activity in orphan G protein coupled receptors, by Adam Lee Martin

Constitutive activity in orphan G protein coupled receptors, by Adam Lee Martin

Label
Constitutive activity in orphan G protein coupled receptors
Title
Constitutive activity in orphan G protein coupled receptors
Statement of responsibility
by Adam Lee Martin
Creator
Author
Subject
Language
eng
Summary
"The goal of this research was to use a distal signaling pathway analysis to evaluate the extent of agonist independent constitutive signaling among orphan class-A G protein coupled receptors (GPCRs). These receptors translate extracellular signals via conformational change into intracellular activation of different G proteins and subsequent second messenger synthesis. These small molecules regulate cellular biochemistry, eventually leading to nuclear signaling that results in changes in gene expression. Some GPCRs are capable of signaling in the absence of an activating ligand, a phenomenon called constitutive activity that is inhibited via an "inverse-agonist". The use of cAMP dependent Luciferase expression is used to compare the canonical signaling of all five wild-type Muscarinic Acetylcholine receptors and their constitutively active (CA) mutant counterparts. All five members, both wild-type and CA, signaled via cAMP dependent pathways, although only the CA mutants do so in the absence of an agonist. This technique is then applied to 40 different orphan GPCRs for which an agonist is unknown/not-present. This resulted in 75% (30 out of 40) scoring as constitutively active, grouped into five different categories based on their response. The largest and most significant group of 17 orphans inhibited cAMP dependent expression, both basal and forskolin stimulated, by more than 40%, indicating activation of Gi. In total, novel findings of constitutive activity were found in 23 of the 40 Orphan receptors with results otherwise in agreement with literature in most cases. Orphan receptors that were closely related based on amino acid homology tended to have similar effects on gene expression. These results suggest that identification of inverse agonists may be a fruitful approach for categorizing these orphan receptors and targeting them for pharmacological intervention."--Abstract, page iii
Member of
Cataloging source
UMR
http://library.link/vocab/creatorDate
1978-
http://library.link/vocab/creatorName
Martin, Adam Lee
Degree
Ph. D.
Dissertation year
2015.
Granting institution
Missouri University of Science and Technology
Illustrations
illustrations
Index
no index present
Literary form
non fiction
Nature of contents
  • dictionaries
  • bibliography
  • theses
http://library.link/vocab/subjectName
  • G proteins
  • Cell receptors
  • Cellular signal transduction
  • Receptors, G-Protein-Coupled
Label
Constitutive activity in orphan G protein coupled receptors, by Adam Lee Martin
Instantiates
Publication
Note
Vita
Bibliography note
Includes bibliographic references (pages 64-79)
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier.
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent.
Control code
913399740
Extent
1 online resource (xii, 80 pages)
Form of item
online
Governing access note
These materials are protected under copyright by the original author
Media category
computer
Media MARC source
rdamedia.
Media type code
  • c
Other physical details
illustrations (some colored).
Specific material designation
remote
System control number
(OCoLC)913399740
Label
Constitutive activity in orphan G protein coupled receptors, by Adam Lee Martin
Publication
Note
Vita
Bibliography note
Includes bibliographic references (pages 64-79)
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier.
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent.
Control code
913399740
Extent
1 online resource (xii, 80 pages)
Form of item
online
Governing access note
These materials are protected under copyright by the original author
Media category
computer
Media MARC source
rdamedia.
Media type code
  • c
Other physical details
illustrations (some colored).
Specific material designation
remote
System control number
(OCoLC)913399740

Library Locations

  • Curtis Laws Wilson LibraryBorrow it
    400 West 14th Street, Rolla, MO, 65409, US
    37.955220 -91.772210
  • Missouri University of Science & Technology Library DepositoryBorrow it
    2908 Lemone Blvd, Columbia, MO, 65201, US
    38.919360 -92.291620
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