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Expert Opinion on Therapeutic Patents Volume 17, 2007 - Issue 11
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Review

Antisense and small-molecule modulation of diacylglycerol acyltransferase

Brian K Hubbard Novartis Institutes for BioMedical Research, Inc., 100 Technology Square, Cambridge, MA 02139, USA +1 617 871 7523; +1 617 871 7043; [email protected]
,
Istvan Enyedy Novartis Institutes for BioMedical Research, Inc., 100 Technology Square, Cambridge, MA 02139, USA +1 617 871 7523; +1 617 871 7043; [email protected]
,
Thomas A Gilmore Novartis Institutes for BioMedical Research, Inc., 100 Technology Square, Cambridge, MA 02139, USA +1 617 871 7523; +1 617 871 7043; [email protected]
&
Michael H Serrano-Wu Novartis Institutes for BioMedical Research, Inc., 100 Technology Square, Cambridge, MA 02139, USA +1 617 871 7523; +1 617 871 7043; [email protected]
Pages 1331-1339 | Published online: 09 Nov 2007

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Vishal P. Zambre, Shamali M. Khamkar, Dnyaneshwar D. Gavhane, Sagar C. Khedkar, Monali R. Chavan, Madhuri M. Pandey, Sonali B. Sanap, Rajesh B. Patil & Sanjay D. Sawant. (2020) Patent landscape for discovery of promising acyltransferase DGAT and MGAT inhibitors. Expert Opinion on Therapeutic Patents 30:11, pages 873-896.
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Andrew J King, Andrew S Judd & Andrew J Souers. (2010) Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents. Expert Opinion on Therapeutic Patents 20:1, pages 19-29.
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Articles from other publishers (13)

Jianwei Yan, Gaihong Wang, Xiangyu Dang, Binbin Guo, Wuhong Chen, Ting Wang, Limin Zeng, Heyao Wang & Youhong Hu. (2017) Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety. Bioorganic & Medicinal Chemistry 25:17, pages 4701-4714.
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Katsumasa Nakajima, Ricardo Chatelain, Kevin B. Clairmont, Renee Commerford, Gary M. Coppola, Thomas Daniels, Cornelia J. Forster, Thomas A. Gilmore, Yongjin Gong, Monish Jain, Aaron Kanter, Youngshin Kwak, Jingzhou Li, Charles D. Meyers, Alan D. Neubert, Paul Szklennik, Vivienne Tedesco, James Thompson, David Truong, Qing Yang, Brian K. Hubbard & Michael H. Serrano-Wu. (2017) Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. Journal of Medicinal Chemistry 60:11, pages 4657-4664.
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Katsumasa Nakajima, Myriam April, Jason T. Brewer, Thomas Daniels, Cornelia J. Forster, Thomas A. Gilmore, Monish Jain, Aaron Kanter, Youngshin Kwak, Jingzhou Li, Les McQuire, Michael H. Serrano-Wu, Ryan Streeper, Paul Szklennik, James Thompson & Bing Wang. (2016) Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors. Bioorganic & Medicinal Chemistry Letters 26:4, pages 1245-1248.
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Jian-Peng Yin, Min Gu, Ying Li & Fa-Jun Nan. (2014) Total Synthesis of Aphadilactones A–D. The Journal of Organic Chemistry 79:13, pages 6294-6301.
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Brian M. Fox, Kazuyuki Sugimoto, Kiyosei Iio, Atsuhito Yoshida, Jian (Ken) Zhang, Kexue Li, Xiaolin Hao, Marc Labelle, Marie-Louise Smith, Steven M. Rubenstein, Guosen Ye, Dustin McMinn, Simon Jackson, Rebekah Choi, Bei Shan, Ji Ma, Shichang Miao, Takuya Matsui, Nobuya Ogawa, Masahiro Suzuki, Akio Kobayashi, Hidekazu Ozeki, Chihiro Okuma, Yukihito Ishii, Daisuke Tomimoto, Noboru Furakawa, Masahiro Tanaka, Mutsuyoshi Matsushita, Mitsuru Takahashi, Takashi Inaba, Shoichi Sagawa & Frank Kayser. (2014) Discovery of 6-Phenylpyrimido[4,5- b ][1,4]oxazines as Potent and Selective Acyl CoA:Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors with in Vivo Efficacy in Rodents . Journal of Medicinal Chemistry 57:8, pages 3464-3483.
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Alleyn T. Plowright, Peter Barton, Stuart Bennett, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Robert D. M. Davies, Anne Ertan, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Per H. Svensson, Andrew V. Turnbull & Michael J. Waring. (2013) Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1. MedChemComm 4:1, pages 151-158.
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Kyeong Lee, Ja-Il Goo, Hwa Young Jung, Minkyoung Kim, Shanthaveerappa K. Boovanahalli, Hye Ran Park, Mun-Ock Kim, Dong-Hyun Kim, Hyun Sun Lee & Yongseok Choi. (2012) Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors. Bioorganic & Medicinal Chemistry Letters 22:24, pages 7456-7460.
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William McCoull, Matthew S. Addie, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Suzanne S. Bowker, Scott Boyd, Stephen Chapman, Robert D.M. Davies, Craig S. Donald, Clive P. Green, Chloe Jenner, Paul D. Kemmitt, Andrew G. Leach, Graeme C. Moody, Pablo Morentin Gutierrez, Nicholas J. Newcombe, Thorsten Nowak, Martin J. Packer, Alleyn T. Plowright, John Revill, Paul Schofield, Chris Sheldon, Steve Stokes, Andrew V. Turnbull, Steven J.Y. Wang, David P. Whalley & J. Matthew Wood. (2012) Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorganic & Medicinal Chemistry Letters 22:12, pages 3873-3878.
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Michael H. Serrano-Wu, Gary M. Coppola, Yongjin Gong, Alan D. Neubert, Ricardo Chatelain, Kevin B. Clairmont, Renee Commerford, Theresa Cosker, Thomas Daniels, Ying Hou, Monish Jain, Marlene Juedes, Lisha Li, Tara Mullarkey, Erik Rocheford, Moo Je Sung, Andrew Tyler, Qing Yang, Taeyoung Yoon & Brian K. Hubbard. (2012) Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides. ACS Medicinal Chemistry Letters 3:5, pages 411-415.
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Matthew M. RavnSeble H. WagawKenneth M. EngstromJianzhang MeiBrian KoteckiAndrew J. SouersPhilip R. KymAndrew S. JuddGang Zhao. (2010) Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor. Organic Process Research & Development 14:2, pages 417-424.
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Paulo J. Magalhães, Daniel O. Carvalho, José M. Cruz, Luís F. Guido & Aquiles A. Barros. (2009) Fundamentals and Health Benefits of Xanthohumol, a Natural Product Derived from Hops and Beer. Natural Product Communications 4:5, pages 1934578X0900400.
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Alan M. Birch, Susan Birtles, Linda K. Buckett, Paul D. Kemmitt, Graham J. Smith, Tim J. D. Smith, Andrew V. Turnbull & Steven J. Y. Wang. (2009) Discovery of a Potent, Selective, and Orally Efficacious Pyrimidinooxazinyl Bicyclooctaneacetic Acid Diacylglycerol Acyltransferase-1 Inhibitor. Journal of Medicinal Chemistry 52:6, pages 1558-1568.
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Victor A. Zammit, Linda K. Buckett, Andrew V. Turnbull, Haja Wure & Andrew Proven. (2008) Diacylglycerol acyltransferases: Potential roles as pharmacological targets. Pharmacology & Therapeutics 118:3, pages 295-302.
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