GPR40: Difference between revisions
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=== Other Potential Inhibitors === | === Other Potential Inhibitors === | ||
TAK-875 had the most promising outlooks of any current known agonists of hGPR40, but clinical trials were discontinued. Some other agonists tested in clinical trials include AMG-837 and AM-1638. When coadministered, AMG-837 and AM-1638 enhanced glucose tolerance, but they were found to be toxic in the human trials. Some other agonsits are currently being examined as well. One compound, LY 2881835 (Eli Lilly & Company, Indianapolis, IN), has undergone clinical trials, but the results are unknown. In addition to the above-mentioned compound, other orally bioavailable GPR40-specific agonists are currently in preclinical or clinical development. As of 2015, TUG-770 and CNX-011-67 (Connexios Life Sciences, Karnataka, India) were in preclinical trials and JTT-851 (Japan Tobacco, Toyko, Japan), and P11187 (Piramal, Mumbai, India) were in clinical trails.<ref name="Mancini">PMID: 25604916</ref> | TAK-875 had the most promising outlooks of any current known agonists of hGPR40, but clinical trials were discontinued. Some other agonists tested in clinical trials include AMG-837 and AM-1638. When coadministered, AMG-837 and AM-1638 enhanced glucose tolerance, but they were found to be toxic in the human trials. Some other agonsits are currently being examined as well. One compound, LY 2881835 (Eli Lilly & Company, Indianapolis, IN), has undergone clinical trials, but the results are unknown. In addition to the above-mentioned compound, other orally bioavailable GPR40-specific agonists are currently in preclinical or clinical development. As of 2015, TUG-770 and CNX-011-67 (Connexios Life Sciences, Karnataka, India) were in preclinical trials and JTT-851 (Japan Tobacco, Toyko, Japan), and P11187 (Piramal, Mumbai, India) were in clinical trails.<ref name="Mancini">PMID: 25604916</ref> | ||
== 3D Structures of GPR40 == | |||
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | |||
[[4phu]], [[5kw2]] – hGPR40/lysozyme + agonist – human <br /> | |||
[[5tzy]], [[5tzr]] – hGPR40/lysozyme (mutant) + partial agonist <br /> | |||
== References == | == References == | ||
<references/> | <references/> | ||
[[Category:Topic Page]] | |||
==Proteopedia Resources== | ==Proteopedia Resources== | ||
[http://proteopedia.org/wiki/index.php/Category:Gpr40 Category:GPR40] | [http://proteopedia.org/wiki/index.php/Category:Gpr40 Category:GPR40] | ||
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[http://proteopedia.org/wiki/index.php/User:R._Jeremy_Johnson/CH462:Biochemistry_II_Butler_University Butler University Proteopedia Pages] | [http://proteopedia.org/wiki/index.php/User:R._Jeremy_Johnson/CH462:Biochemistry_II_Butler_University Butler University Proteopedia Pages] | ||
See also: | |||
*[[Receptor]] | |||
*[[Transmembrane (cell surface) receptors]] | |||
*[[G protein-coupled receptors]] | |||
</StructureSection> | </StructureSection> | ||
==Student Contributors== | ==Student Contributors== | ||
