Current status of GPR40/FFAR1 modulators in medicinal chemistry (2016–2019): a patent review

RLA8—A New and Highly Effective Quadruple PPAR-α/γ/δ and GPR40 Agonist to Reverse Nonalcoholic Steatohepatitis and Fibrosis

(2019) Meng Hua Li et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

SCO-267, a GPR40 Full Agonist, Improves Glycemic and Body Weight Control in Rat Models of Diabetes and Obesity

(2019) Hikaru Ueno et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The future of new drugs for diabetes management

(2019) Clifford J. Bailey et al.   DIABETES RESEARCH AND CLINICAL PRACTICE

Discovery of HWL-088: A highly potent FFA1/GPR40 agonist bearing a phenoxyacetic acid scaffold

(2019) Zheng Li et al.   BIOORGANIC CHEMISTRY

Design, synthesis, and biological evaluation of novel dual FFA1 (GPR40)/PPARδ agonists as potential anti-diabetic agents

(2019) Zheng Li et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold

(2019) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold

(2018) Zheng Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of a novel potent GPR40 full agonist

(2018) Sanath K. Meegalla et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists

(2018) Khaled M. Darwish et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel benzo[ b ]thiophene tetrazoles as non-carboxylate GPR40 agonists

(2018) Hui Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and structure−activity relationship studies of GPR40 agonists containing amide linker

(2018) Tingting Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

GPR40-Mediated Gα12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets

(2018) Marie-Laure Rives et al.   MOLECULAR PHARMACOLOGY

Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ

(2018) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents

(2018) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thiazolidinediones and PPAR orchestra as antidiabetic agents: From past to present

(2017) Sabina Yasmin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes

(2017) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges

(2017) Zheng Li et al.   MEDICINAL RESEARCH REVIEWS

SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists

(2017) Dong-Oh Yoon et al.   ACS Medicinal Chemistry Letters

Design and Synthesis of Novel, Selective GPR40 AgoPAMs

(2017) Christopher W. Plummer et al.   ACS Medicinal Chemistry Letters

Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes

(2016) Zheng Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Complex Pharmacology of Free Fatty Acid Receptors

(2016) Graeme Milligan et al.   CHEMICAL REVIEWS

Long-term safety and efficacy of fasiglifam (TAK-875), a G-protein-coupled receptor 40 agonist, as monotherapy and combination therapy in Japanese patients with type 2 diabetes: a 52-week open-label phase III study

(2016) K. Kaku et al.   DIABETES OBESITY & METABOLISM

Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole

(2016) Lingyun Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists

(2016) Khaled M. Darwish et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development

(2016) Zheng Li et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Yhhu4488, a novel GPR40 agonist, promotes GLP-1 secretion and exerts anti-diabetic effect in rodent models

(2015) Dan-yang Guo et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Activation of Extracellular Signal-Regulated Protein Kinases 1 and 2 (ERK1/2) by Free Fatty Acid Receptor 1 (FFAR1/GPR40) Protects from Palmitate-Induced Beta Cell Death, but Plays no Role in Insulin Secretion

(2015) Madhura Panse et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Safety of antidiabetes medications: An update

(2015) CJ Bailey   CLINICAL PHARMACOLOGY & THERAPEUTICS

G Protein-coupled Receptor 40 (GPR40) and Peroxisome Proliferator-activated Receptor γ (PPARγ)

(2015) Shuibang Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

(2015) Maria Hauge et al.   Molecular Metabolism

Homology modeling and explicit membrane molecular dynamics simulation to delineate the mode of binding of thiazolidinediones into FFAR1 and the mechanism of receptor activation

(2014) Mohamed A. Helal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potentiation of insulin secretion and improvement of glucose intolerance by combining a novel G protein-coupled receptor 40 agonist DS-1558 with glucagon-like peptide-1 receptor agonists

(2014) Ryutaro Nakashima et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice

(2014) Da Young Oh et al.   NATURE MEDICINE

The G-Protein-Coupled Long-Chain Fatty Acid Receptor GPR40 and Glucose Metabolism

(2014) Tsutomu Tomita et al.   Frontiers in Endocrinology

Treatment of Type 2 Diabetes by Free Fatty Acid Receptor Agonists

(2014) Kenneth R. Watterson et al.   Frontiers in Endocrinology

Reevaluation of Fatty Acid Receptor 1 as a Drug Target for the Stimulation of Insulin Secretion in Humans

(2013) R. Wagner et al.   DIABETES

Lack of GPR40/FFAR1does not induce diabetes even under insulin resistance condition

(2013) K. Matsuda-Nagasumi et al.   DIABETES OBESITY & METABOLISM

The importance of synthetic drugs for type 2 diabetes drug discovery

(2013) Maliheh Safavi et al.   Expert Opinion on Drug Discovery

Novel GPR40 agonist AS2575959 exhibits glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion

(2013) Hirotsugu Tanaka et al.   LIFE SCIENCES

Regulation of energy metabolism by long-chain fatty acids

(2013) Manabu T. Nakamura et al.   PROGRESS IN LIPID RESEARCH

A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents

(2012) Jian Luo et al.   PLoS One

Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist

(2012) Sean P. Brown et al.   ACS Medicinal Chemistry Letters

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist

(2010) Nobuyuki Negoro et al.   ACS Medicinal Chemistry Letters

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

(2009) K. Nagasumi et al.   DIABETES

Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes

(2009) Sandip B Bharate et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Lack of FFAR1/GPR40 Does Not Protect Mice From High-Fat Diet-Induced Metabolic Disease

(2008) H. Lan et al.   DIABETES

International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1, -2, and -3: Pharmacology and Pathophysiological Functions

(2008) L. A. Stoddart et al.   PHARMACOLOGICAL REVIEWS