Sandbox Reserved 1165: Difference between revisions
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[[Image:Screen Shot 2016-03-29 at 3.24.43 PM.png|(|):|400 px|center|thumb|'''Figure 5: Salt Bridge'''. The non-covalent interactions between residues Glu 406, Arg 173, and Arg 346 form a [https://en.wikipedia.org/wiki/Denticity tridentate] salt bridge. The Glu 406 acts as the central residue in the tridentate salt bridge; Arg 173 and Arg 436 both | [[Image:Screen Shot 2016-03-29 at 3.24.43 PM.png|(|):|400 px|center|thumb|'''Figure 5: Salt Bridge'''. The non-covalent interactions between residues Glu 406, Arg 173, and Arg 346 form a [https://en.wikipedia.org/wiki/Denticity tridentate] salt bridge. The Glu 406 acts as the central residue in the tridentate salt bridge; Arg 173 and Arg 436 both [https://en.wikipedia.org/wiki/Chelation chelating] with Glu 406. The salt bridge is located on the intracellular side of the transmembrane helices.]] | ||
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=Clinical Relevancy= | =Clinical Relevancy= | ||
Of the fifteen human class B GPCRs, eight have been confirmed as potential [https://en.wikipedia.org/wiki/Biological_target drug target]. <ref name="Drug">PMID: 24628305</ref> However, overall family B GPCRS have been difficult drug targets. This difficulty is partially related to the inherent flexibility in the class B GCGR 7TM. The flexibility comes from the ability of GCGR to be a receptor many ligands. The ECD and it's role in interactions on the extracellular side of receptors may provide evidence to how class B receptors adjust the conformational spectra for various ligands. Researchers hope to show how these conformations can be utilized in potential treatments of a wide array [https://en.wikipedia.org/wiki/List_of_mental_disorders disorders]. <ref name="Drug">PMID: 24628305</ref> | Of the fifteen human class B GPCRs, eight have been confirmed as potential [https://en.wikipedia.org/wiki/Biological_target drug target]. <ref name="Drug">PMID: 24628305</ref> However, overall family B GPCRS have been difficult drug targets. This difficulty is partially related to the inherent flexibility in the class B GCGR 7TM. The flexibility comes from the ability of GCGR to be a receptor many ligands. The ECD and it's role in interactions on the extracellular side of receptors may provide evidence to how class B receptors adjust the conformational spectra for various ligands. Researchers hope to show how these conformations can be utilized in potential treatments of a wide array [https://en.wikipedia.org/wiki/List_of_mental_disorders disorders]. <ref name="Drug">PMID: 24628305</ref> | ||
=Potential Inhibitors= | =Potential Inhibitors for GCGR= | ||
There are potential class B GCGR [https://en.wikipedia.org/wiki/Enzyme_inhibitor inhibitors] that have clinic relevancy. These inhibitors to class B GCGRs have primarily focused on [https://en.wikipedia.org/wiki/Allosteric_regulation allosteric inhibitors] with high specificity and the ability to treat diseases including: [https://en.wikipedia.org/wiki/Stress-related_disorders stress disorders], managing [http://www.webmd.com/diabetes/guide/diabetes-hyperglycemia hyperglycemia], and also alternative mechanisms for treating [https://en.wikipedia.org/wiki/Migraine migraines]. <ref name="Inhibitors">PMID: 24189067</ref> Inhibitors include [https://en.wikipedia.org/wiki/Monoclonal_antibody monoclonal antibodies] which inhibit glucagon receptors through an allosteric mechanism. <ref name="Last">PMID: 19305799</ref> Further research still to be done on | There are potential class B GCGR [https://en.wikipedia.org/wiki/Enzyme_inhibitor inhibitors] that have clinic relevancy. These inhibitors to class B GCGRs have primarily focused on [https://en.wikipedia.org/wiki/Allosteric_regulation allosteric inhibitors] with high specificity and the ability to treat diseases including: [https://en.wikipedia.org/wiki/Stress-related_disorders stress disorders], managing [http://www.webmd.com/diabetes/guide/diabetes-hyperglycemia hyperglycemia], and also alternative mechanisms for treating [https://en.wikipedia.org/wiki/Migraine migraines]. <ref name="Inhibitors">PMID: 24189067</ref> Inhibitors include [https://en.wikipedia.org/wiki/Monoclonal_antibody monoclonal antibodies] which inhibit glucagon receptors through an allosteric mechanism. <ref name="Last">PMID: 19305799</ref> Further research still to be done on | ||
==Research== | ==Research== | ||
