The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470)-Reference-Cited by-同舟云学术

The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470)

Published:2016-11-11 Issue:24 Volume:59 Page:10891-10916
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Hamdouchi Chafiq¹,Kahl Steven D.¹,Patel Lewis Anjana¹,Cardona Guemalli R.¹,Zink Richard W.¹,Chen Keyue¹,Eessalu Thomas E.¹,Ficorilli James V.¹,Marcelo Marialuisa C.¹,Otto Keith A.¹,Wilbur Kelly L.¹,Lineswala Jayana P.¹,Piper Jared L.¹,Coffey D. Scott¹,Sweetana Stephanie A.¹,Haas Joseph V.¹,Brooks Dawn A.¹,Pratt Edward J.²,Belin Ruth M.¹,Deeg Mark A.¹,Ma Xiaosu¹,Cannady Ellen A.¹,Johnson Jason T.¹,Yumibe Nathan P.¹,Chen Qi¹,Maiti Pranab³,Montrose-Rafizadeh Chahrzad¹,Chen Yanyun¹,Reifel Miller Anne¹

Affiliation:

1. Lilly Research Laboratories, A division of Eli Lilly and Company, Lilly Corporate Center, DC: 0540, Indianapolis, Indiana 46285, United States

2. Eli Lilly and Company, 237994 Singapore

3. Jubilant Biosys Research Center, 560 022 Bangalore, India

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

http://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.6b00892

Reference54 articles.

1. Global Report on Diabetes;World Health Organization:Geneva, 2016; http://apps.who.int/iris/bitstream/10665/204871/1/9789241565257_eng.pdf(accessed May 26, 2016).

2. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules

3. Oleic acid interacts with GPR40 to induce Ca2+signaling in rat islet β-cells: mediation by PLC and L-type Ca2+channel and link to insulin release

4. Overexpression of GPR40 in Pancreatic β-Cells Augments Glucose-Stimulated Insulin Secretion and Improves Glucose Tolerance in Normal and Diabetic Mice

5. Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from β-cells through activation of GPR40

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