Lambertus Benthem

Beneficial effects of a plant-fish oil, slow carbohydrate diet on cardio-metabolic health exceed the correcting effects of metformin-pioglitazone in diabetic pigs fed a fast-food diet

S.J. Koopmans, Heleen M.M. van Beusekom, F. Josef van der Staay, G.P. Binnendijk et autres

BACKGROUND: Lifestyle influences endocrine, metabolic and cardiovascular homeostasis. This study investigated the impact of diet and oral anti-diabetic medication on cardio-metabolic health in human-sized diabetic pigs. METHODS: After a growing pre-phase from ~30 to ~69 kg during which domestic pigs were fed …

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Effects of a novel potent melanin‐concentrating hormone receptor 1 antagonist, AZD1979, on body weight homeostasis in mice and dogs

Karolina Ploj, Lambertus Benthem, Dorota Kakol‐Palm, Peter Gennemark et autres

BACKGROUND AND PURPOSE: Melanin-concentrating hormone (MCH) is an orexigen, and while rodents express one MCH receptor (MCH1 receptor), humans, non-human primates and dogs express two MCH receptors (MCH1 and MCH2 ). MCH1 receptor antagonists have been developed for the treatment of obesity …

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Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties

Anders Johansson, Christian Löfberg, Madeleine Antonsson, Sverker von Unge et autres

A novel series of melanin concentrating hormone receptor 1 (MCHr1) antagonists were the starting point for a drug discovery program that culminated in the discovery of 103 (AZD1979). The lead optimization program was conducted with a focus on reducing lipophilicity and understanding …

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CCDC 1429511: Experimental Crystal Structure Determination

Anders Johansson, Christian Löfberg, Madeleine Antonsson, Sverker von Unge et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Novel Zn2+ Modulated GPR39 Receptor Agonists Do Not Drive Acute Insulin Secretion in Rodents

Ola Fjellström, Niklas Larsson, Shin-ichiro Yasuda, Takuma Tsuchida et autres

Type 2 diabetes (T2D) occurs when there is insufficient insulin release to control blood glucose, due to insulin resistance and impaired β-cell function. The GPR39 receptor is expressed in metabolic tissues including pancreatic β-cells and has been proposed as a T2D target. …

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Structural and Pharmacological Characterization of Novel Potent and Selective Monoclonal Antibody Antagonists of Glucose-dependent Insulinotropic Polypeptide Receptor

Peter Ravn, Chaithanya Madhurantakam, Susan Kunze, Evelyn Matthews et autres

Glucose-dependent insulinotropic polypeptide (GIP) is an endogenous hormonal factor (incretin) that, upon binding to its receptor (GIPr; a class B G-protein-coupled receptor), stimulates insulin secretion by beta cells in the pancreas. There has been a lack of potent inhibitors of the GIPr …

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Forced and voluntary exercise counteract insulin resistance in rats: The role of coping style

Gretha J. Boersma, R. Paulien Barf, Lambertus Benthem, Gertjan van Dijk et autres

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Personality as a risk factor for adiposity and hyperinsulineamia

G.J. Boersma, Lambertus Benthem, Gertjan van Dijk, A.J.W. Scheurink

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Personality, a key factor in personalized medicine?

Gretha J. Boersma, Lambertus Benthem, André P. van Beek, Gertjan van Dijk et autres

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Individual variation in the (patho)physiology of energy balance

Gretha J. Boersma, Lambertus Benthem, Gertjan van Dijk, A.J.W. Scheurink

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Pharmacological treatment of hyperinsulineamia in rats depends on coping style

Gretha J. Boersma, Lambertus Benthem, Gertjan van Dijk, Thierry Steimer et autres

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Coping style predicts the (in)sensitivity for developing hyperinsulinemia on a high fat diet in rats

Gretha J. Boersma, Lambertus Benthem, Gertjan van Dijk, Thierry Steimer et autres

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