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Expert Opinion on Therapeutic Patents Volume 23, 2013 - Issue 12
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The therapeutic potential of GPR120: a patent review

Somnath HalderDepartment of Medicinal Chemistry, Piramal Enterprises Ltd, 1, Nirlon Complex, Off Western Exp. Highway, Near NSE Complex, Goregaon East, Mumbai, Maharashtra 400 063, India+91 22 30818078; [email protected]
, PhD,
Sanjay KumarDepartment of Medicinal Chemistry, Piramal Enterprises Ltd, 1, Nirlon Complex, Off Western Exp. Highway, Near NSE Complex, Goregaon East, Mumbai, Maharashtra 400 063, India
, PhD &
Rajiv SharmaDepartment of Medicinal Chemistry, Piramal Enterprises Ltd, 1, Nirlon Complex, Off Western Exp. Highway, Near NSE Complex, Goregaon East, Mumbai, Maharashtra 400 063, India
, PhD
Pages 1581-1590 | Published online: 06 Oct 2013

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David Rychtrmoc, Pavla Staňková, Otto Kučera & Zuzana Červinková. (2022) Comparison of two anti-diabetic monoestolides regarding effects on intact murine liver tissue. Archives of Physiology and Biochemistry 128:4, pages 985-992.
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Xuqing Zhang & Mark J. Macielag. (2020) GPR120 agonists for the treatment of diabetes: a patent review (2014 present). Expert Opinion on Therapeutic Patents 30:10, pages 729-742.
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Yuichi Hattori, Kuniaki Ishii, Kazuhiko Yanai & Masao Endoh. (2022) The large part German medicine has played in the development of experimental pharmacology in Japan. Naunyn-Schmiedeberg's Archives of Pharmacology 396:1, pages 35-42.
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Saeed Al Mahri, Shuja Shafi Malik, Maria Al Ibrahim, Esraa Haji, Ghida Dairi & Sameer Mohammad. (2022) Free Fatty Acid Receptors (FFARs) in Adipose: Physiological Role and Therapeutic Outlook. Cells 11:4, pages 750.
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Angelo Maria Patti, Rosaria Vincenza Giglio, Nikolaos Papanas, Dragos Serban, Anca Pantea Stoian, Kalliopi Pafili, Khalid Al Rasadi, Kanya Rajagopalan, Ali A. Rizvi, Marcello Ciaccio & Manfredi Rizzo. (2022) Experimental and Emerging Free Fatty Acid Receptor Agonists for the Treatment of Type 2 Diabetes. Medicina 58:1, pages 109.
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Brian D. Hudson. 2022. Allosteric Modulation of G Protein-Coupled Receptors. Allosteric Modulation of G Protein-Coupled Receptors 97 116 .
Manuel Grundmann, Eckhard Bender, Jens Schamberger & Frank Eitner. (2021) Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators. International Journal of Molecular Sciences 22:4, pages 1763.
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Tiechao Jiang, Dongli Jiang, Dong You, Lirong Zhang, Long Liu & Qini Zhao. (2020) Agonism of GPR120 prevents ox-LDL-induced attachment of monocytes to endothelial cells. Chemico-Biological Interactions 316, pages 108916.
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Meijuan Zhang & ShengFeng Qiu. (2019) Activation of GPR120 promotes the metastasis of breast cancer through the PI3K/Akt/NF-κB signaling pathway. Anti-Cancer Drugs 30:3, pages 260-270.
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Dong-Soon Im. (2018) FFA4 (GPR120) as a fatty acid sensor involved in appetite control, insulin sensitivity and inflammation regulation. Molecular Aspects of Medicine 64, pages 92-108.
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Runisha Moodaley, David M Smith, Iain R Tough, Marcus Schindler & Helen M Cox. (2017) Agonism of free fatty acid receptors 1 and 4 generates peptide YY-mediated inhibitory responses in mouse colon. British Journal of Pharmacology 174:23, pages 4508-4522.
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Steven M. Sparks, Christopher Aquino, Pierette Banker, Jon L. Collins, David Cowan, Caroline Diaz, Steven T. Dock, Donald L. Hertzog, Xi Liang, Erin D. Swiger, Josephine Yuen, Grace Chen, Channa Jayawickreme, David Moncol, Christopher Nystrom, Vincent Rash, Thomas Rimele, Shane Roller & Sean Ross. (2017) Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist. Bioorganic & Medicinal Chemistry Letters 27:5, pages 1278-1283.
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Jie Zhao, Honggang Wang, Peiliang Shi, Wenbo Wang & Ye Sun. (2016) GPR120, a potential therapeutic target for experimental colitis in IL-10 deficient mice. Oncotarget 8:5, pages 8397-8405.
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Graeme Milligan, Bharat Shimpukade, Trond Ulven & Brian D. Hudson. (2016) Complex Pharmacology of Free Fatty Acid Receptors. Chemical Reviews 117:1, pages 67-110.
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Matthew Lombardo, Kate Bender, Clare London, Michael A. Plotkin, Melissa Kirkland, Joel Mane, Michele Pachanski, Wayne Geissler, John Cummings, Bahanu Habulihaz, Taro E. Akiyama, Jerry Di Salvo, Maria Madeira, Joanna Pols, Mary Ann Powles, Michael F. Finley, Eric Johnson, Thomas Roussel, Victor N. Uebele, Alejandro Crespo, Dennis Leung, Candice Alleyne, Dorina Trusca, Ying Lei, Andrew D. Howard, Feroze Ujjainwalla, James R. Tata & Christopher J. Sinz. (2016) Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects. Bioorganic & Medicinal Chemistry Letters 26:23, pages 5724-5728.
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M T M van Jaarsveld, J M Houthuijzen & E E Voest. (2015) Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer. Oncogene 35:31, pages 4021-4035.
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Dong-Soon Im. (2016) Functions of omega-3 fatty acids and FFA4 (GPR120) in macrophages. European Journal of Pharmacology 785, pages 36-43.
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Nader H. Moniri. (2016) Free-fatty acid receptor-4 (GPR120): Cellular and molecular function and its role in metabolic disorders. Biochemical Pharmacology 110-111, pages 1-15.
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Ai-Jun Li, Qing Wang, Thu T. Dinh, Steve M. Simasko & Sue Ritter. (2016) Mercaptoacetate blocks fatty acid-induced GLP-1 secretion in male rats by directly antagonizing GPR40 fatty acid receptors. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 310:8, pages R724-R732.
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Jency Thomas & Manohar L. Garg. 2016. Molecular Nutrition and Diabetes. Molecular Nutrition and Diabetes 291 299 .
Steffen V. F. Hansen & Trond Ulven. 2017. Free Fatty Acid Receptors. Free Fatty Acid Receptors 33 56 .
Rosa Formicola, Paolo Pevarello, Christina Kuhn, Chiara Liberati, Francesco Piscitelli & Mariangela Sodano. (2015) FFA4/GPR120 agonists: a survey of the recent patent literature. Pharmaceutical Patent Analyst 4:6, pages 443-451.
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Ang Li, Yue Li & Lupei Du. (2015) Biological characteristics and agonists of GPR120 (FFAR4) receptor: the present status of research. Future Medicinal Chemistry 7:11, pages 1457-1468.
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G Milligan, E Alvarez-Curto, K R Watterson, T Ulven & B D Hudson. (2015) Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. British Journal of Pharmacology 172:13, pages 3254-3265.
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Akira Hirasawa. (2015) Free Fatty Acid Receptor Family: A New Therapeutic Target for Metabolic Diseases消化管脂肪酸センサーの創薬展開. YAKUGAKU ZASSHI 135:6, pages 769-777.
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Akira Hirasawa, Masato Takeuchi, Ryouhei Shirai, Zao Chen, Shota Ishii & Keiko Iida. (2015) Free fatty acid receptors as therapeutic targets for metabolic disorders. Folia Pharmacologica Japonica 146:6, pages 296-301.
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Shuhei Ishii, Miku Hirane, Sayumi Kato, Nobuyuki Fukushima & Toshifumi Tsujiuchi. (2015) Opposite effects of GPR120 and GPR40 on cell motile activity induced by ethionine in liver epithelial cells. Biochemical and Biophysical Research Communications 456:1, pages 135-138.
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Akira Hirasawa, Masato Takeuchi, Takafumi Hara, Ayako Hirata, Soshi Tanabe & Naoya Umeda. 2015. Bioactive Lipid Mediators. Bioactive Lipid Mediators 139 154 .
Jennifer L. Pluznick. (2014) Extra sensory perception. Current Opinion in Nephrology and Hypertension 23:5, pages 507-512.
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Kenneth R. Watterson, Brian D. Hudson, Trond Ulven & Graeme Milligan. (2014) Treatment of Type 2 Diabetes by Free Fatty Acid Receptor Agonists. Frontiers in Endocrinology 5.
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Robin M. Tucker, Richard D. Mattes & Cordelia A. Running. (2014) Mechanisms and effects of “fat taste” in humans. BioFactors 40:3, pages 313-326.
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