• Although GABA C receptors were

  2022-07-14

  

  Although, GABA-C receptors were originally described in the spinal cord [16], clues to their physiological function arise mainly from studies in the visual system [5], [26]. In mammals, GABA-C receptors are found abundantly in cone photoreceptors and bipolar cell axon terminals, where they participa

• br Funding Our work in

  2022-07-14

  

  Funding Our work in this field was supported by CNRSLIA528, Agence Nationale de la Recherche 06-Neuro, Agence Nationale de la Recherche MNMP 2009. Introduction GABA and the GI motility The role of GABA in the modulation of GI motility is quite complex and not fully understood, since GABA-i

• While there have been a variety

  2022-07-14

  

  While there have been a variety of recent reviews on the signaling and physiological effects of FFA4, particularly towards its anti-inflammatory effects, the goal of this research update is to present the most recent details on the role of FFA4 in human cancers. The known contributions of FFA4 towar

• br Chronic obstructive pulmonary disease

  2022-07-14

  

  Chronic obstructive pulmonary disease (COPD) is characterized by progressive obstruction of airflow, not fully reversible, which is accompanied by a chronic inflammatory response, induced by deleterious particles or gases, in airways and lung parenchyma. The most important risk factor for COPD is

• Glucose induced nuclear translocation of several

  2022-07-14

  

  Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu

• In regards to animals several studies have reported the pero

  2022-07-14

  

  In regards to animals, several studies have reported the peroxisomal localization of FPS (Krisans et al., 1994, Olivier et al., 2000, Kovacs et al., 2007). Transfections of mammalian cells with the rat short FPS isoform followed by immunodetection localized the enzyme to the peroxisome (Olivier et a

• Introduction Thrombotic disorders including ischemic heart d

  2022-07-14

  

  Introduction Thrombotic disorders including ischemic heart disease, deep venous thrombosis, and ischemic stroke represent one of the most common causes of death in the world [1]. All these conditions relate to states accompanied by a shift of hemostasis balance into a coagulation side because of va

• br Substrate Interactions Outside of the Catalytic Cleft As

  2022-07-13

  

  Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use

• Etoposide VP a semisynthetic podophyllotoxin derivative agen

  2022-07-13

  

  Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology

• br Conflict of interest statement br Acknowledgements RF is

  2022-07-13

  

  Conflict of interest statement Acknowledgements RF is supported by Pancreatic Cancer Research Fund (grant to MF); MF is supported by Prostate Cancer UK (PG12-23 and PG13-029). Background Lysophosphatidylinositol Molecular species and the biosynthesis of phosphatidylinositol, the precu

• Excessive adiposity is also a key

  2022-07-13

  

  Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP

• Strengths The primary feature of GPR agonists

  2022-07-13

  

  Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L Exendin-3 (9-39) amide as well as glucose-dependent insulin secretion and insulin promoter activity enhancem

• Acknowledgments This research was supported by the

  2022-07-13

  

  Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor

• br Introduction In the treatment of patients

  2022-07-13

  

  Introduction In the treatment of patients with AIDS and human immunodeficiency virus type 1 (HIV-1), anti-retroviral therapy (ART), which uses anti-HIV drugs such as protease inhibitors, integrase inhibitors and reverse transferase inhibitors, has made a major contribution. There are still some s

• Based on work from our labs with mGlu NAMs and

  2022-07-13

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

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