Sandbox Reserved 1170: Difference between revisions

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=== TAK-875 ===

[[Image:Tak-875.png |300 px|right|thumb|Figure 4. Structure of TAK-875. The carboxylate moiety (upper right) inserts into hGPR40. The Sulfonate group (upper left) remains on the outside of the protein once bound.]] One example of an hGPR40 agonist is <scene name='72/721541/Tak875/2'>TAK-875</scene>. The carboxylate moiety of the agonist enters through the auxiliary loop of hGPR40, ~~interrupts~~ the charge network, and binds with Arg 183, Arg 258, Tyr 91, and Tyr 240.<ref name="Srivastava"/> TAK-875 has shown efficacy in increasing insulin secretion and lowering blood glucose in rodent models of type 2 diabetes.<ref name="Burant"/> This drug was studied in stage III clinical trials. It significantly reduced [http://www.diabetes.co.uk/what-is-hba1c.html HbA1c] and fasting plasma glucose levels in Japanese patients with type 2 diabetes that was not controlled by diet and exercise. However, clinical trials were stopped shortly after this study because TAK-875 was suspected of causing liver damage.<ref name="Kaku">PMID:25787200</ref>

[[Image:Tak-875.png |300 px|right|thumb|Figure 4. Structure of TAK-875. The carboxylate moiety (upper right) inserts into hGPR40. The Sulfonate group (upper left) remains on the outside of the protein once bound.]] One example of an hGPR40 agonist is <scene name='72/721541/Tak875/2'>TAK-875</scene>. The carboxylate moiety of the agonist enters through the auxiliary loop of hGPR40, disrupts the hydrogen bonding of the charge network, and binds with Arg 183, Arg 258, Tyr 91, and Tyr 240.<ref name="Srivastava"/> TAK-875 has shown efficacy in increasing insulin secretion and lowering blood glucose in rodent models of type 2 diabetes.<ref name="Burant"/> This drug was studied in stage III clinical trials. It significantly reduced [http://www.diabetes.co.uk/what-is-hba1c.html HbA1c] and fasting plasma glucose levels in Japanese patients with type 2 diabetes that was not controlled by diet and exercise. However, clinical trials were stopped shortly after this study because TAK-875 was suspected of causing liver damage.<ref name="Kaku">PMID:25787200</ref>

Sandbox Reserved 1170: Difference between revisions

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Revision as of 13:15, 12 April 2016 view source Whitney Hart (talk \| contribs) 186 edits No edit summary ← Older edit		Revision as of 13:16, 12 April 2016 view source Whitney Hart (talk \| contribs) 186 edits No edit summary Newer edit →
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	=== TAK-875 ===		=== TAK-875 ===
	[[Image:Tak-875.png \|300 px\|right\|thumb\|Figure 4. Structure of TAK-875. The carboxylate moiety (upper right) inserts into hGPR40. The Sulfonate group (upper left) remains on the outside of the protein once bound.]] One example of an hGPR40 agonist is <scene name='72/721541/Tak875/2'>TAK-875</scene>. The carboxylate moiety of the agonist enters through the auxiliary loop of hGPR40, ~~interrupts~~ the charge network, and binds with Arg 183, Arg 258, Tyr 91, and Tyr 240.<ref name="Srivastava"/> TAK-875 has shown efficacy in increasing insulin secretion and lowering blood glucose in rodent models of type 2 diabetes.<ref name="Burant"/> This drug was studied in stage III clinical trials. It significantly reduced [http://www.diabetes.co.uk/what-is-hba1c.html HbA1c] and fasting plasma glucose levels in Japanese patients with type 2 diabetes that was not controlled by diet and exercise. However, clinical trials were stopped shortly after this study because TAK-875 was suspected of causing liver damage.<ref name="Kaku">PMID:25787200</ref>		[[Image:Tak-875.png \|300 px\|right\|thumb\|Figure 4. Structure of TAK-875. The carboxylate moiety (upper right) inserts into hGPR40. The Sulfonate group (upper left) remains on the outside of the protein once bound.]] One example of an hGPR40 agonist is <scene name='72/721541/Tak875/2'>TAK-875</scene>. The carboxylate moiety of the agonist enters through the auxiliary loop of hGPR40, disrupts the hydrogen bonding of the charge network, and binds with Arg 183, Arg 258, Tyr 91, and Tyr 240.<ref name="Srivastava"/> TAK-875 has shown efficacy in increasing insulin secretion and lowering blood glucose in rodent models of type 2 diabetes.<ref name="Burant"/> This drug was studied in stage III clinical trials. It significantly reduced [http://www.diabetes.co.uk/what-is-hba1c.html HbA1c] and fasting plasma glucose levels in Japanese patients with type 2 diabetes that was not controlled by diet and exercise. However, clinical trials were stopped shortly after this study because TAK-875 was suspected of causing liver damage.<ref name="Kaku">PMID:25787200</ref>