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1. Full Text A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice
by Oh, Da Young and Walenta, Evelyn and Akiyama, Taro E and Lagakos, William S and Lackey, Denise and Lackey, Denise and Pessentheiner, Ariane R and Sasik, Roman and Hah, Nasun and Chi, Tyler J and Cox, Jason M and Powels, Mary Ann and Di Salvo, Jerry and Sinz, Christopher and Sinz, Christopher and Watkins, Steven M and Armando, Aaron M and Chung, Heekyung and Evans, Ronald M and Quehenberger, Oswald and McNelis, Joanne and Bogner-Strauss, Juliane G and Olefsky, Jerrold M
Nature Medicine, ISSN 1078-8956, 2014, Volume 20, Issue 8, pp. 942 - 947
It is well known that the omega-3 fatty acids (omega-3-FAs; also known as n-3 fatty acids) can exert potent anti-inflammatory effects(1-4). Commonly consumed... 
MEDICINE, RESEARCH & EXPERIMENTAL | CELLS | POTENT | GPR120 | BIOCHEMISTRY & MOLECULAR BIOLOGY | DISEASE | POLYUNSATURATED FATTY-ACIDS | SECRETION | GPR40 | RECEPTORS | CELL BIOLOGY | Nitric Oxide Synthase Type II - biosynthesis | Receptors, G-Protein-Coupled - metabolism | Diabetes Mellitus, Type 2 - genetics | Molecular Sequence Data | Arginase - biosynthesis | Male | Hyperinsulinism - drug therapy | Receptors, G-Protein-Coupled - agonists | Obesity - genetics | T-Lymphocytes, Regulatory - immunology | Insulin Resistance - physiology | Base Sequence | Macrophages - immunology | Fatty Acids, Omega-3 - metabolism | Mice, Inbred C57BL | Inflammation | B-Lymphocytes, Regulatory - immunology | Fatty Liver - drug therapy | Mice, Knockout | Docosahexaenoic Acids - pharmacology | Animals | Mice, Obese | Mice | Receptors, G-Protein-Coupled - genetics | Diabetes Mellitus, Type 2 - drug therapy | Physiological aspects | Insulin resistance | Triglycerides | B cells | Health aspects | Omega-3 fatty acids | Obesity | Fatty acids | Rodents | Inflammatory diseases | Chronic illnesses
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2. Full Text (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide:  A Selective α-Amino Amide Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
by Edmondson, Scott D and Mastracchio, Anthony and Mathvink, Robert J and He, Jiafang and Harper, Bart and Park, You-Jung and Beconi, Maria and Di Salvo, Jerry and Eiermann, George J and He, Huaibing and Leiting, Barbara and Leone, Joseph F and Levorse, Dorothy A and Lyons, Kathryn and Patel, Reshma A and Patel, Sangita B and Petrov, Aleksandr and Scapin, Giovanna and Shang, Jackie and Roy, Ranabir Sinha and Smith, Aaron and Wu, Joseph K and Xu, Shiyao and Zhu, Bing and Thornberry, Nancy A and Weber, Ann E
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2006, Volume 49, Issue 12, pp. 3614 - 3627
A series of β-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type... 
Dipeptidyl Peptidase 4 - metabolism | Phenylalanine - analogs & derivatives | Phenylalanine - pharmacology | Stereoisomerism | Triazoles - chemistry | Humans | Microsomes, Liver - metabolism | Biological Availability | Crystallography, X-Ray | Male | Muscle, Skeletal - metabolism | Structure-Activity Relationship | Protease Inhibitors - pharmacology | Microsomes, Liver - drug effects | Phenylalanine - chemistry | Muscle Proteins - antagonists & inhibitors | Triazoles - chemical synthesis | NAV1.5 Voltage-Gated Sodium Channel | Cell Line | Rabbits | Glucose Tolerance Test | Administration, Oral | Mice, Inbred C57BL | Sodium Channels | Models, Molecular | Protease Inhibitors - chemistry | Hypoglycemic Agents - chemistry | Hypoglycemic Agents - pharmacology | Triazoles - pharmacology | Animals | Calcium Channels, L-Type - drug effects | Hypoglycemic Agents - chemical synthesis | Phenylalanine - chemical synthesis | Mice, Obese | Mice | Protease Inhibitors - chemical synthesis | Diabetes Mellitus, Type 2 - drug therapy | In Vitro Techniques
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3. Full Text Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40
by Lu, Jun and Byrne, Noel and Wang, John and Bricogne, Gerard and Brown, Frank K and Chobanian, Harry R and Colletti, Steven L and Di Salvo, Jerry and Thomas-Fowlkes, Brande and Guo, Yan and Hall, Dawn L and Hadix, Jennifer and Hastings, Nicholas B and Hermes, Jeffrey D and Ho, Thu and Howard, Andrew D and Josien, Hubert and Kornienko, Maria and Lumb, Kevin J and Miller, Michael W and Patel, Sangita B and Pio, Barbara and Plummer, Christopher W and Sherborne, Bradley S and Sheth, Payal and Souza, Sarah and Tummala, Srivanya and Vonrhein, Clemens and Webb, Maria and Allen, Samantha J and Johnston, Jennifer M and Weinglass, Adam B and Sharma, Sujata and Soisson, Stephen M and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Nature Structural and Molecular Biology, ISSN 1545-9993, 07/2017, Volume 24, Issue 7, pp. 570 - 577
Clinical studies indicate that partial agonists of the G-protein-coupled, free fatty acid receptor 1 GPR40 enhance glucose-dependent insulin secretion and... 
ANTAGONIST | RECOGNITION | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | SEROTONIN RECEPTORS | VALIDATION | IDENTIFICATION | CELL BIOLOGY | BIOPHYSICS | PROTEIN-COUPLED RECEPTOR | INTRACELLULAR LOOP | FUNCTIONAL SELECTIVITY | BINDING-SITES | Allosteric Regulation | Humans | Models, Molecular | Protein Binding | Crystallography, X-Ray | Protein Conformation | Receptors, G-Protein-Coupled - agonists | Binding Sites | Receptors, G-Protein-Coupled - chemistry | Cell receptors | Molecular structure | Properties | Ligands (Biochemistry) | Testing | Secretion | Diabetes mellitus | Lipids | Helices | Glucose | Insulin | Fatty acids | Bundling | Proteins | Allosteric properties | Acids | Ligands | Cooperativity | Binding sites | Activation analysis | Crystal structure | BASIC BIOLOGICAL SCIENCES | 60 APPLIED LIFE SCIENCES
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4. Full Text GPR40 reduces food intake and body weight through GLP-1
by Gorski, Judith N and Pachanski, Michele J and Mane, Joel and Plummer, Christopher W and Souza, Sarah and Thomas-Fowlkes, Brande S and Ogawa, Aimie M and Weinglass, Adam B and Di Salvo, Jerry and Cheewatrakoolpong, Boonlert and Howard, Andrew D and Colletti, Steven L and Trujillo, Maria E
American Journal of Physiology - Endocrinology and Metabolism, ISSN 0193-1849, 2017, Volume 313, Issue 1, pp. E37 - E47
G protein-coupled receptor 40 (GPR40) partial agonists lower glucose through the potentiation of glucose-stimulated insulin secretion, which is believed to... 
Obesity | Glucagon-like peptide-1 | Diet-induced obesity | Diabetes | G protein-coupled receptor 40 | CELLS | PHYSIOLOGY | AMIDE | glucagon-like peptide-1 | INSULIN-SECRETION | TAK-875 | diet-induced obesity | DIPEPTIDYL PEPTIDASE IV | LIRAGLUTIDE | ENDOCRINOLOGY & METABOLISM | diabetes | obesity | AGONIST | Glucagon-Like Peptide 1 - metabolism | Receptors, G-Protein-Coupled - metabolism | Mice, Inbred C57BL | Male | Appetite Regulation - genetics | Body Weight - genetics | Eating - genetics | Mice, Knockout | Animals | Receptors, G-Protein-Coupled - antagonists & inhibitors | Weight Loss - physiology | Mice | Receptors, G-Protein-Coupled - genetics | Glucagon | Physiological aspects | Physiological research | G proteins | Eating (Physiology) | Research
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5. Full Text GPR40 (FFAR1) - Combined Gs and Gq signaling invitro is associated with robust incretin secretagogue action ex vivo and in vivo
by Hauge, Maria and Vestmar, Marie A and Husted, Anna S and Ekberg, Jeppe P and Wright, Michael J and Di Salvo, Jerry and Weinglass, Adam B and Engelstoft, Maja S and Madsen, Andreas N and Lückmann, Michael and Miller, Michael W and Trujillo, Maria E and Frimurer, Thomas M and Holst, Birgitte and Howard, Andrew D and Schwartz, Thue W
Molecular Metabolism, ISSN 2212-8778, 01/2015, Volume 4, Issue 1, pp. 3 - 14
Objectives: GPR40 (FFAR1), a clinically proven anti-diabetes target, is a Gq-coupled receptor for long chain fatty acids (LCFA) stimulating insulin secretion... 
G protein-coupled receptor | Biased signaling | Ago-allosteric agonist | Glucagon like peptide 1 (GLP-1) | Long chain fatty acids (LCFAs)
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6. Full Text GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo
by Hauge, Maria and Vestmar, Marie A and Husted, Anna S and Ekberg, Jeppe P and Wright, Michael J and Di Salvo, Jerry and Weinglass, Adam B and Engelstoft, Maja S and Madsen, Andreas N and Lückmann, Michael and Miller, Michael W and Trujillo, Maria E and Frimurer, Thomas M and Holst, Birgitte and Howard, Andrew D and Schwartz, Thue W
Molecular Metabolism, ISSN 2212-8778, 2014, Volume 4, Issue 1, pp. 3 - 14
Abstract Objectives GPR40 (FFAR1), a clinically proven anti-diabetes target, is a Gq-coupled receptor for long chain fatty acids (LCFA) stimulating insulin... 
Endocrinology & Metabolism | G protein-coupled receptor | Biased signaling | Ago-allosteric agonist | Glucagon like peptide 1 (GLP-1) | Long chain fatty acids (LCFAs) | INSULIN-SECRETION | FATTY-ACID STIMULATION | TAK-875 | DISCOVERY | POTENT | INTERNATIONAL UNION | BIASED AGONISM | PROTEIN-COUPLED RECEPTOR | ENTEROENDOCRINE CELLS | ENDOCRINOLOGY & METABOLISM | ALLOSTERISM
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7. Full Text GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent
by Pachanski, Michele J and Kirkland, Melissa E and Kosinski, Daniel T and Mane, Joel and Cheewatrakoolpong, Boonlert and Xue, Jiyan and Szeto, Daphne and Forrest, Gail and Miller, Corin and Bunzel, Michelle and Plummer, Christopher W and Chobanian, Harry R and Miller, Michael W and Souza, Sarah and Thomas-Fowlkes, Brande S and Ogawa, Aimie M and Weinglass, Adam B and Di Salvo, Jerry and Li, Xiaoyan and Feng, Yue and Tatosian, Daniel A and Howard, Andrew D and Colletti, Steven L and Trujillo, Maria E
PLoS ONE, ISSN 1932-6203, 10/2017, Volume 12, Issue 10, p. e0186033
GPR40 agonists are effective antidiabetic agents believed to lower glucose through direct effects on the beta cell to increase glucose stimulated insulin... 
CELLS | ACTIVATION | RAT PANCREAS | ISLETS | REDUCTION | MULTIDISCIPLINARY SCIENCES | INSULIN-SECRETION | RELEASE | IDENTIFICATION | FATTY-ACID RECEPTOR | GLUCAGON | Cell Line | Glucose Tolerance Test | Cricetulus | Humans | Incretins - metabolism | Rats | Male | Receptors, G-Protein-Coupled - agonists | Insulin - metabolism | Animals | Islets of Langerhans - metabolism | Glucose - metabolism | Glucagon - metabolism | Mice | Insulin Secretion | CHO Cells | Inhibitor drugs | Glucagon | Secretion | Body weight | Diabetes mellitus | Pharmacology | Glucose | Secretions | Insulin | Fatty acids | Beta cells | Rodents | Biomarkers | Diabetes | Pancreas | Binding sites | Pharmaceutical sciences | Metabolic disorders
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8. GPR40 reduces food intake and body weight through GLP-1
by Judith N Gorski and Michele J Pachanski and Joel Mane and Christopher W Plummer and Sarah Souza and Brande S Thomas-Fowlkes and Aimie M Ogawa and Adam B Weinglass and Jerry Di Salvo and Boonlert Cheewatrakoolpong and Andrew D Howard and Steven L Colletti and Maria E Trujillo
American Journal of Physiology, ISSN 0193-1849, 07/2017, Volume 313, Issue 1, p. E37
G protein-coupled receptor 40 (GPR40) partial agonists lower glucose through the potentiation of glucose-stimulated insulin secretion, which is believed to... 
Potentiation | Obesity | CD26 antigen | Peptidase | Peptides | Glucagon | Secretion | Body weight | Weight loss | Body weight loss | Glucose | Insulin | Body weight gain | Weight | Modulators | Proteins | Allosteric properties | Diet | Food intake | Mice | Diabetes | Glucagon-like peptide 1 | Gastric motility
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9. Full Text GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production
by Miller, Corin and Pachanski, Michele J and Kirkland, Melissa E and Kosinski, Daniel T and Mane, Joel and Bunzel, Michelle and Cao, Jin and Souza, Sarah and Thomas-Fowlkes, Brande and Di Salvo, Jerry and Weinglass, Adam B and Li, Xiaoyan and Myers, Robert W and Knagge, Kevin and Carrington, Paul E and Hagmann, William K and Trujillo, Maria E
PLoS ONE, ISSN 1932-6203, 05/2017, Volume 12, Issue 5, p. e0176182
GPR40 (FFA1) is a fatty acid receptor whose activation results in potent glucose lowering and insulinotropic effects in vivo. Several reports illustrate that... 
OBESITY | STIMULATION | GLUCONEOGENESIS | DEPENDENT INSULIN-SECRETION | MULTIDISCIPLINARY SCIENCES | GLYCOGENOLYSIS | PANCREATIC BETA-CELLS | IMPROVES | TAK-875 | TYPE-2 | RECEPTOR 1 AGONIST | Diabetes Mellitus, Experimental - drug therapy | Cricetulus | Rats, Wistar | Receptors, G-Protein-Coupled - metabolism | Humans | Male | Receptors, G-Protein-Coupled - agonists | Thiazolidinediones - chemistry | Insulin - blood | Benzopyrans - chemistry | Liver - drug effects | Time Factors | Fasting - blood | HEK293 Cells | Benzopyrans - pharmacology | Diabetes Mellitus, Experimental - metabolism | Drug Evaluation, Preclinical | Thiazolidinediones - pharmacology | CHO Cells | Tissue Culture Techniques | Liver - metabolism | Rats | Hypoglycemic Agents - chemistry | Hypoglycemic Agents - pharmacology | Mice, Knockout | Blood Glucose - drug effects | Animals | Glucose - metabolism | Receptors, G-Protein-Coupled - genetics | Blood Glucose - metabolism | Type 2 diabetes | Glucose metabolism | Care and treatment | Analysis | Patient outcomes | Dosage and administration | Fatty acids | Health aspects | Insulin | Cell culture | Blasticidin S | Biochemistry | Glucose | Males | Assaying | Temperature effects | Penicillin | Hemoglobin | Inhibition | Pharmaceutical industry | Gluconeogenesis | Obesity | Estrus | Media | Bioavailability | Metabolism | Chemicals | Beta cells | Studies | Dilution | Diet | Biomarkers | Mice | Binding sites | Metabolic disorders | Temperature | Physiological effects | Media (culture) | Nuclear magnetic resonance--NMR | Centrifugation | Medical services | Homeostasis | Clinical trials | Amino acids | Stimulation | Defects | Quinones | Allosteric properties | Farms | Rodents | Fasting | Purification | Secretion | Diabetes mellitus | Pharmacology | Skeletal muscle | Glucose tolerance | Buffers (chemistry) | Musculoskeletal system | Growth media | Reagents | Insulin resistance | In vivo methods and tests | Resonance | Diabetes | Females | Nuclear magnetic resonance | NMR
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10. Full Text GPR120 suppresses adipose tissue lipolysis and synergizes with GPR40 in antidiabetic efficacy
by Satapati, Santhosh and Qian, Ying and Wu, Margaret S and Petrov, Aleksandr and Dai, Ge and Wang, Sheng-Ping and Zhu, Yonghua and Shen, Xiaolan and Muise, Eric S and Chen, Ying and Zycband, Emanuel and Weinglass, Adam and Di Salvo, Jerry and Debenham, John S and Cox, Jason M and Lan, Ping and Shah, Vinit and Previs, Stephen F and Erion, Mark and Kelley, David E and Wang, Liangsu and Howard, Andrew D and Shang, Jin
Journal of Lipid Research, ISSN 0022-2275, 2017, Volume 58, Issue 8, pp. 1561 - 1578
GPR40 and GPR120 are fatty acid sensors that play important roles in glucose and energy homeostasis. GPR40 potentiates glucose-dependent insulin secretion and... 
Insulin resistance | Diabetes | Lipolysis and fatty acid metabolism | Fatty acid | FFAR4 GPR120 | BIOCHEMISTRY & MOLECULAR BIOLOGY | PHASE-III | fatty acid | FATTY-ACID-METABOLISM | RECEPTOR 40 AGONIST | FASIGLIFAM TAK-875 | NICOTINIC-ACID | GLUCOSE-HOMEOSTASIS | INSULIN-RESISTANCE | HUMAN OBESITY | lipolysis and fatty acid metabolism | JAPANESE PATIENTS | insulin resistance | diabetes | Islets of Langerhans - drug effects | Cricetinae | Lipolysis - drug effects | Cricetulus | Receptors, G-Protein-Coupled - metabolism | Insulin Resistance | Rats | Male | Receptors, G-Protein-Coupled - agonists | Gene Expression Regulation - drug effects | Adipose Tissue - metabolism | Animals | Diabetes Mellitus, Experimental - pathology | Islets of Langerhans - physiopathology | Mice | Diabetes Mellitus, Experimental - metabolism | Adipose Tissue - drug effects | CHO Cells | Animal models | Adipose tissue | Secretion | Diabetes mellitus | Homeostasis | Adipocytes | Glucose | Insulin | Lipolysis | Energy balance | Rodents | Islets of Langerhans | Pancreas
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11. Full Text Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder
by Edmondson, Scott D and Zhu, Cheng and Kar, Nam Fung and Di Salvo, Jerry and Nagabukuro, Hiroshi and Sacre-Salem, Beatrice and Dingley, Karen and Berger, Richard and Goble, Stephen D and Morriello, Gregori and Harper, Bart and Moyes, Christopher R and Shen, Dong-Ming and Wang, Liping and Ball, Richard and Fitzmaurice, Aileen and Frenkl, Tara and Gichuru, Loise N and Ha, Sookhee and Hurley, Amanda L and Jochnowitz, Nina and Levorse, Dorothy and Mistry, Shruty and Miller, Randy R and Ormes, James and Salituro, Gino M and Sanfiz, Anthony and Stevenson, Andra S and Villa, Katherine and Zamlynny, Beata and Green, Stuart and Struthers, Mary and Weber, Ann E
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2016, Volume 59, Issue 2, pp. 609 - 623
The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical... 
Cricetulus | Humans | Structure-Activity Relationship | Pyrrolidines - therapeutic use | Urinary Bladder, Overactive - drug therapy | Microsomes, Liver - drug effects | X-Ray Diffraction | Urination - drug effects | Female | Microsomes, Liver - enzymology | Pyrimidinones - toxicity | Receptors, Adrenergic, beta - drug effects | Receptors, Adrenergic, beta - metabolism | CHO Cells | Cricetinae | Pyrrolidines - pharmacokinetics | Pyrimidinones - therapeutic use | Models, Molecular | Rats | Drug Discovery | Rats, Sprague-Dawley | Adrenergic beta-3 Receptor Agonists - toxicity | Lipidoses - chemically induced | Serotonin Plasma Membrane Transport Proteins - metabolism | Adrenergic beta-3 Receptor Agonists - therapeutic use | Animals | Pyrimidinones - pharmacokinetics | Pyrrolidines - toxicity | Adrenergic beta-3 Receptor Agonists - pharmacokinetics | Urinary Bladder - drug effects | Index Medicus
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12. Full Text Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs
by Pio, Barbara and Chobanian, Harry R and Guo, Yan and Josien, Hubert and Hagmann, William K and Miller, Michael and Trujillo, Maria E and Kirkland, Melissa and Kosinski, Daniel and Mane, Joel and Pachanski, Michele and Cheewatrakoolpong, Boonlert and Ashley, Eric and Orr, Robert and Wright, Michael J and Bugianesi, Randal and Souza, Sarah and Zhang, Xiaoping and Di Salvo, Jerry and Weinglass, Adam B and Tschirret-Guth, Richard and Samuel, Koppara and Chen, Qing and Shang, Jackie and Lamca, James and Ehrhart, Juliann and Nargund, Ravi and Howard, Andrew D and Colletti, Steven L
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1842 - 1848
GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by... 
FFA1 | GPCR | Diabetes | GPR40 AgoPAM | Indane | CELLS | CHEMISTRY, MEDICINAL | EFFICACY | SAFETY | ACIDS | CHEMISTRY, ORGANIC | RECEPTOR 40 AGONIST | FASIGLIFAM TAK-875 | DISCOVERY | POTENT | JAPANESE PATIENTS | Pancreatic beta cells | Analysis | Liver | Glucose | G proteins | Fatty acids | Dextrose | Membrane proteins
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13. Full Text Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents
by Adams, Gregory L and Velazquez, Francisco and Jayne, Charles and Shah, Unmesh and Miao, Shouwu and Ashley, Eric R and Madeira, Maria and Akiyama, Taro E and Di Salvo, Jerry and Suzuki, Takao and Wang, Nengxue and Truong, Quang and Gilbert, Eric and Zhou, Dan and Verras, Andreas and Kirkland, Melissa and Pachanski, Michele and Powles, Maryann and Yin, Wu and Ujjainwalla, Feroze and Venkatraman, Srikanth and Edmondson, Scott D
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 01/2017, Volume 8, Issue 1, pp. 96 - 101
GPR120 (FFAR4) is a fatty acid sensing G protein coupled receptor (GPCR) that has been identified as a target for possible treatment of type 2 diabetes. A... 
Type 2 diabetes | FFAR4 | Insulin sensitization | Chromane | GPR120 | RECEPTOR GPR120 | CHEMISTRY, MEDICINAL | HIT | type 2 diabetes | INHIBITION | INSULIN-RESISTANCE | insulin sensitization | chromane | SECRETION | BINDING | LIFE
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14. Full Text Discovery of benzamides as potent human β3 adrenergic receptor agonists
by Zhu, Cheng and Kar, Nam F and Li, Xiaofang and Li, Bing and Costa, Melissa and Dingley, Karen H and Di Salvo, Jerry and Ha, Sookhee N and Hurley, Amanda L and Miller, Randy R and Salituro, Gino M and Struthers, Mary and Weber, Ann E and Hale, Jeffrey J and Edmondson, Scott D
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2016, Volume 26, Issue 1, pp. 55 - 59
The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human β -adrenergic... 
Overactive bladder | Bioisostere | β3 adrenergic receptor agonist | Reverse amide | Pyrrolidine scaffold | adrenergic receptor agonist | Dose-Response Relationship, Drug | Adrenergic beta-3 Receptor Agonists - chemical synthesis | Humans | Benzamides - pharmacology | Molecular Structure | Structure-Activity Relationship | Receptors, Adrenergic, beta-3 - metabolism | Adrenergic beta-3 Receptor Agonists - pharmacology | Benzamides - chemical synthesis | Drug Discovery | Adrenergic beta-3 Receptor Agonists - chemistry | Benzamides - chemistry
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15. Full Text Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects
by Lombardo, Matthew and Bender, Kate and London, Clare and Plotkin, Michael A and Kirkland, Melissa and Mane, Joel and Pachanski, Michele and Geissler, Wayne and Cummings, John and Habulihaz, Bahanu and Akiyama, Taro E and Di Salvo, Jerry and Madeira, Maria and Pols, Joanna and Powles, Mary Ann and Finley, Michael F and Johnson, Eric and Roussel, Thomas and Uebele, Victor N and Crespo, Alejandro and Leung, Dennis and Alleyne, Candice and Trusca, Dorina and Lei, Ying and Howard, Andrew D and Ujjainwalla, Feroze and Tata, James R and Sinz, Christopher J
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 12/2016, Volume 26, Issue 23, pp. 5724 - 5728
The transformation of an aryloxybutanoic acid ultra high-throughput screening (uHTS) hit into a potent and selective series of G-protein coupled receptor 120... 
Type 2 diabetes | FFAR4 | GPR120 | Benzofuran propanoic acid | Ultra high-throughput screening | Aryloxybutanoic acid | POTENT | CHEMISTRY, MEDICINAL | DISEASES | INSULIN-RESISTANCE | CHEMISTRY, ORGANIC | GPR40 | Propionates - pharmacology | Propionates - chemistry | Blood Glucose - analysis | Receptors, G-Protein-Coupled - metabolism | Humans | Benzofurans - pharmacology | Benzofurans - blood | Hypoglycemic Agents - chemistry | Diabetes Mellitus, Type 2 - metabolism | Receptors, G-Protein-Coupled - agonists | Hypoglycemic Agents - pharmacology | Benzofurans - chemistry | Hypoglycemic Agents - blood | Propionates - blood | Diabetes Mellitus, Type 2 - blood | Animals | High-Throughput Screening Assays | Mice | Blood Glucose - metabolism | Diabetes Mellitus, Type 2 - drug therapy | Drug Evaluation, Preclinical | Phenylalanine
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16. Full Text Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder
by Harper, Bart H and Wang, Liping and Zhu, Cheng and Kar, Nam F and Li, Bing and Moyes, Christopher R and Goble, Stephen D and Costa, Melissa and Dingley, Karen and Di Salvo, Jerry and Ha, Sookhee N and Hurley, Amanda and Li, Xiaofang and Miller, Randy R and Nagabukuro, Hiroshi and Salituro, Gino M and Smith, Sean and Struthers, Mary and Hale, Jeffrey J and Edmondson, Scott D and Berger, Richard
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 02/2017, Volume 27, Issue 4, pp. 1094 - 1098
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β -adrenergic receptor for the treatment of overactive bladder... 
Urinary Bladder, Overactive - drug therapy | Adrenergic beta-3 Receptor Agonists - therapeutic use | Humans | Piperazines - chemistry | Piperazines - therapeutic use | Structure-Activity Relationship | Adrenergic beta-3 Receptor Agonists - pharmacology | Piperazines - pharmacology | Adrenergic beta-3 Receptor Agonists - chemistry
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17. Full Text Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder
by Harper, Bart H and Wang, Liping and Zhu, Cheng and Kar, Nam F and Li, Xiaofang and Li, Bing and Moyes, Christopher R and Goble, Stephen D and Costa, Melissa and Dingley, Karen and Di Salvo, Jerry and Ha, Sookhee N and Hurley, Amanda and Miller, Randy R and Nagabukuro, Hiroshi and Salituro, Gino M and Smith, Sean and Struthers, Mary and Hale, Jeffrey J and Edmondson, Scott D and Berger, Richard
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2017, Volume 27, Issue 4, pp. 1094 - 1098
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β -adrenergic receptor for the treatment of overactive bladder... 
Overactive bladder | Norepinephrine transporter | β3-Adrenergic receptor agonist | Reverse amide | Pyrrolidine scaffold | Adrenergic receptor agonist
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