• Receptor guanylyl cyclases play essential roles

  2022-05-31

  

  Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists

• Here we show that lactate

  2022-05-31

  

  Here we show that lactate activates the Gi-coupled receptor GPR81, which is exclusively expressed on adipocytes, and that lactate released from adipocytes in response to glucose and insulin mediates insulin-induced antilipolysis by activation of GPR81. Results Discussion Nutrients and their m

• Afatinib dimaleate Acute in vivo experiments were performed

  2022-05-31

  

  Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding Afatinib dimaleate control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg

• br FXR Agonists Azepinol b indole hEC

  2022-05-31

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• br Material and methods br Results Consistent with our previ

  2022-05-31

  

  Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing glutathione reductase in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the m

• br Disclosure statement br Acknowledgements We thank Dr Rona

  2022-05-31

  

  Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot

• Here we performed TEM and AFM imaging to study

  2022-05-31

  

  Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence

• br Materials and methods br Results br Discussion Neurotrans

  2022-05-31

  

  Materials and methods Results Discussion Neurotransmitter uptake is one of the most important aspects of synaptic transmission, it fact, the existence of a specific uptake system is one of the requisites that any neuroactive substance has to cover to be considered a neurotransmitter. It has

• NP118809 receptor br Introduction Depression is a prevalent

  2022-05-31

  

  Introduction Depression is a prevalent and disabling psychiatric illness that affects millions of individuals worldwide, resulting in enormous personal suffering and public health costs [1]. Traditional antidepressants such as monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake

• The structure and activity of

  2022-05-31

  

  The structure and activity of GLUT1 has been most intensively studied in erythrocytes, in which this transporter makes up 10–20% of membrane protein content. Carruthers has shown that, while GLUT1 can exist and transport glucose as monomers, dimers and tetramers, in erythrocytes GLUT1 exists predomi

• The developed method was used to quantify RBC membrane

  2022-05-31

  

  The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe

• Palifosfamide mg br Introduction As is now well known obesit

  2022-05-31

  

  Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other

• It is important to control hyperglycaemia because

  2022-05-31

  

  It is important to control hyperglycaemia because it can contribute to serious complications. Hyperglycaemia can be managed by maintaining stable blood glucose levels inside the normal range. This can be achieved by various strategies such as diet, medications and exercise (O’Keefe & Bell, 2007). Se

• The relationship between estrogen and the Hedgehog pathway

  2022-05-31

  

  The relationship between estrogen and the Hedgehog pathway as well as the associated mechanism have already been investigated in many tissues, especially in breast cancer (Chang et al., 2012, Katayama et al., 2006, Ramaswamy et al., 2012). Hitherto, even though we have proved that HH-Gli pathway pro

• In order to facilitate the preparation of

  2022-05-31

  

  In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to

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