Genomes and Genes
B B Zhang
Affiliation: Merck Research Laboratories
- Insulin- and mitogen-activated protein kinase-mediated phosphorylation and activation of peroxisome proliferator-activated receptor gammaB Zhang
Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
J Biol Chem 271:31771-4. 1996..2) PPARgamma is phosphorylated in vivo by insulin stimulation or activation of the MAP kinase pathway. 3) MAP kinase is an important mediator of cross-talk between insulin signal transduction pathways and PPARgamma function...
- Small molecule insulin receptor activators potentiate insulin action in insulin-resistant cellsM Li
University of California at San Francisco, Mount Zion Medical Center, San Francisco, California 94143-1616, USA
Diabetes 50:2323-8. 2001..In summary, these two classes of IR activators selectively increased IR function in a variety of insulin-resistant cell lines...
- Discovery of a small molecule insulin mimetic with antidiabetic activity in miceB Zhang
Department of Molecular Endocrinology, Merck Research Laboratories, R80W250, Post Office Box 2000, Rahway, NJ 07065, USA
Science 284:974-7. 1999..These results demonstrate the feasibility of discovering novel insulin receptor activators that may lead to new therapies for diabetes...
- New approaches in the treatment of type 2 diabetesB B Zhang
Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, NJ 07065, USA
Curr Opin Chem Biol 4:461-7. 2000....
- AMPK: an emerging drug target for diabetes and the metabolic syndromeBei B Zhang
Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ 07065, USA
Cell Metab 9:407-16. 2009..Activation of AMPK by pharmacological agents presents a unique challenge, given the complexity of the biology, but holds a considerable potential to reverse the metabolic abnormalities associated with type 2 diabetes...
- Discovery of a small molecule insulin receptor activatorG M Salituro
Department of Natural Product Drug Discovery, Merck Research Laboratories, Rahway, New Jersey 07065, USA
Recent Prog Horm Res 56:107-26. 2001..Thus, DMAQ-B1 represents the first orally active insulin-mimetic agent. Pharmaceutical intervention aimed at augmenting IR function ultimately may prove beneficial as a novel therapeutic option in patients with diabetes...
- Chronic treatment with a glucagon receptor antagonist lowers glucose and moderately raises circulating glucagon and glucagon-like peptide 1 without severe alpha cell hypertrophy in diet-induced obese miceJ Mu
Merck, RY80N A58, 126 East Lincoln Avenue, Rahway, NJ, USA
Diabetologia 54:2381-91. 2011..Antagonism of the glucagon receptor (GCGR) represents a potential approach for treating diabetes. Cpd-A, a potent and selective GCGR antagonist (GRA) was studied in preclinical models to assess its effects on alpha cells...
- Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptorK Liu
Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
J Med Chem 43:3487-94. 2000..Results from additional studies with compound 2h, aimed at evaluating classical quinone-related phenomena, provided sufficient grounds for optimism to allow more extensive toxicologic evaluation...
- AMPK activators--potential therapeutics for metabolic and other diseasesG Zhou
Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ, USA
Acta Physiol (Oxf) 196:175-90. 2009..Activators of AMPK that target selected tissues hold potential as novel therapeutics for diseases in which altered energy metabolism contributes to aetiology...
- Bone loss in the oestrogen-depleted rat is not exacerbated by sitagliptin, either alone or in combination with a thiazolidinedioneT Cusick
Merck Research Laboratories, Merck Sharp and Dohme Corp, Whitehouse Station, NJ, USA
Diabetes Obes Metab 15:954-7. 2013..These findings support prior findings with TZDs and suggest a neutral or beneficial impact of DPP-4 inhibition on bone health. ..
- Glucagon receptor knockout mice are resistant to diet-induced obesity and streptozotocin-mediated beta cell loss and hyperglycaemiaS L Conarello
Laboratory Animal Resources, Merck Research Laboratories, Rahway, NJ, USA
Diabetologia 50:142-50. 2007..The goal of the current research was to further investigate the role of glucagon signalling in metabolic control and glucose homeostasis...
- RNAi-mediated germline knockdown of FABP4 increases body weight but does not improve the deranged nutrient metabolism of diet-induced obese miceR Yang
Department of Metabolic Disorders Diabetes, Merck Research Laboratories, Rahway, NJ 07065, USA
Int J Obes (Lond) 35:217-25. 2011..To investigate the impact of reduced adipocyte fatty acid-binding protein 4 (FABP4) in control of body weight, glucose and lipid homeostasis in diet-induced obese (DIO) mice...
- Modulation of insulin signalling by insulin sensitizersG Jiang
Metabolic Disorders Diabetes, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Biochem Soc Trans 33:358-61. 2005..Taken together, the results suggest that IRS1 inhibitory serine phosphorylation is a key component of insulin resistance and its reversal may be physiologically relevant to insulin sensitization in vivo...
- Insulin action in cultured human skeletal muscle cells during differentiation: assessment of cell surface GLUT4 and GLUT1 contentL Al-Khalili
Department of Surgical Science, Karolinska Institutet, 17177 Stockholm, Sweden
Cell Mol Life Sci 60:991-8. 2003..05) increased glucose uptake and glycogen synthesis. Thus, cultured myotubes are a useful tool to facilitate biological and molecular validation of novel pharmacological agents aimed to improve glucose metabolism in skeletal muscle...