2006
DOI: 10.2174/138920306778017981
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Structure-Activity Relationship Studies: Methods and Ligand Design for G-Protein Coupled Peptide Receptors

Abstract: The exchange of information between cells represents an important regulatory mechanism for cellular activities. Such regulation processes mainly occur by hydrophilic compounds, unable to penetrate the cell membrane. Accordingly such signals have to be transmitted into the cell that is performed by transmembrane receptors. The widespread group of G-protein coupled receptors plays a decisive role in extracellular signal recognition and transition into cellular response. The importance of this interaction is evid… Show more

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Cited by 7 publications
(3 citation statements)
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References 105 publications
(137 reference statements)
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“…The coupling of GPCRs with G-proteins leads to GDP release and Guanosine TriPhosphate (GTP) binding to the G α subunit. Subsequently, the GTP binding induces conformational alterations on G α subunit, promoting the release of G-proteins from GPCR and the dissociation of heterotrimeric G-proteins into G α and G βγ subunits [25]. The G α (G α s , G α i/o , G αq , G α12/13 ) and G βγ subunits amplify and propagate their cell transduction signals through the modulation of various downstream effectors [26], including Adenylyl Cyclase (AC; EC 4.6.1.1) and PhosphoLipase C (PLC; EC 3.1.4.3), that, in turn, regulate the production of second messengers, such as Ca 2+ , cyclic Adenosine MonoPhosphate (cAMP), cyclic Guanosine MonoPhosphate (cGMP), DiAcylGlycerol (DAG), and Inositol-1,4,5-triPhosphate (IP 3 ), the modulation of ion channels, and the activation of kinases cascades, triggering a wide array of cellular responses of physiological importance [27, 28] (Fig.…”
Section: G-protein-coupled Receptors As Thera-peutic Targets For Parkmentioning
confidence: 99%
“…The coupling of GPCRs with G-proteins leads to GDP release and Guanosine TriPhosphate (GTP) binding to the G α subunit. Subsequently, the GTP binding induces conformational alterations on G α subunit, promoting the release of G-proteins from GPCR and the dissociation of heterotrimeric G-proteins into G α and G βγ subunits [25]. The G α (G α s , G α i/o , G αq , G α12/13 ) and G βγ subunits amplify and propagate their cell transduction signals through the modulation of various downstream effectors [26], including Adenylyl Cyclase (AC; EC 4.6.1.1) and PhosphoLipase C (PLC; EC 3.1.4.3), that, in turn, regulate the production of second messengers, such as Ca 2+ , cyclic Adenosine MonoPhosphate (cAMP), cyclic Guanosine MonoPhosphate (cGMP), DiAcylGlycerol (DAG), and Inositol-1,4,5-triPhosphate (IP 3 ), the modulation of ion channels, and the activation of kinases cascades, triggering a wide array of cellular responses of physiological importance [27, 28] (Fig.…”
Section: G-protein-coupled Receptors As Thera-peutic Targets For Parkmentioning
confidence: 99%
“…The coupling of GPCRs with Gproteins leads to GDP release and Guanosine TriPhosphate (GTP) binding to the G α subunit. Subsequently, the GTP binding induces conformational alterations on G α subunit, promoting the release of G-proteins from GPCR and the dissociation of heterotrimeric G-proteins into G α and G βγ subunits [25]. The G α (G αs , G αi/o , G αq , G α12/13 ) and G βγ subunits amplify and propagate their cell transduction signals through the modulation of various downstream effectors [26], including Adenylyl Cyclase (AC; EC 4.6.1.1) and PhosphoLipase C (PLC; EC 3.1.4.3), that, in turn, regulate the production of second messengers, such as Ca 2+ , cyclic Adenosine MonoPhosphate (cAMP), cyclic Guanosine MonoPhosphate (cGMP), DiAcylGlycerol (DAG), and Inositol-1,4,5-triPhosphate (IP 3 ), the modulation of ion channels, and the activation of kinases cascades, triggering a wide array of cellular responses of physiological importance [27,28] (Fig.…”
Section: G-protein-coupled Receptors As Therapeutic Targets For Parkimentioning
confidence: 99%
“…Plasma membrane receptors that bind hydrophilic hormones can be classified by the molecular mechanisms involved in their associated signal‐transduction mechanism (Table 3) (54). Some plasma membrane receptor proteins not only bind a specific hormone, but also serve as effectors within the cell.…”
Section: Mechanisms Of Hormone Actionmentioning
confidence: 99%