• br Materials and methods br Results and discussion br

  2022-04-15

  

  Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t

• Knock out mice of FXR showed enhancing cholesterol

  2022-04-15

  

  Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon

• Recent research has focused on identifying key agonists

  2022-04-15

  

  Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty TNP-ATP triethylammonium salt receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it c

• As a part of our continuing efforts towards discovery

  2022-04-15

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• To meet the requirement of

  2022-04-15

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

• In the FARM motifs of GGPPSs hydrophobic amino

  2022-04-15

  

  In the FARM motifs of GGPPSs, hydrophobic flavopiridol are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase (GG

• br Introduction Thrombosis is one of

  2022-04-15

  

  Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable CM-272 and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–2 per

• Introduction Histamine Imidazolyl ethylamine is an important

  2022-04-15

  

  Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric SB 204070 receptor secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamin

• The CRY protein contains a conserved photolyase homology

  2022-04-15

  

  The CRY1 protein contains a conserved photolyase homology region crucially involved in repression of CLOCK/BMAL1; a C-terminal helix also known as the predicted coiled coil (CC), which interacts with PER2 and FBXL3 in a mutually exclusive manner; and a C-terminal extension also referred to as the “t

• In the course of studies leading to

  2022-04-14

  

  In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of

• In this precancerous condition though cancer develops from t

  2022-04-14

  

  In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio

• insulin receptor br Materials and methods br Results br

  2022-04-14

  

  Materials and methods Results Discussion The compound P7C3 has been reported to activate NAMPT (Wang et al., 2014) and augment NAD+ levels, thereby promoting the survival of mature neurons and postnatal neurogenesis throughout the post-ischemic insulin receptor (Loris et al., 2017). Howeve

• In the pathogenesis of insulin resistance chronic activation

  2022-04-14

  

  In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph

• br Synthetic Antagonists for FFA To date only compounds

  2022-04-14

  

  Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this

• The first described synthetic FFA

  2022-04-14

  

  The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was

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