• Thiola br Membrane transporters as a

  2022-08-15

  

  Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS

• We recently reported the first cyclopropene

  2022-08-15

  

  We recently reported the first cyclopropene-analog of the amino Capecitabine neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28].

• As a part of our continuing efforts

  2022-08-15

  

  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

• br Clinical trials testing GLP mimetics

  2022-08-13

  

  Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino Evans Blue tetrasodium salt incretin growth factor which activates pancreatic islets to en

• br Experimental br Results and discussion

  2022-08-13

  

  Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f

• br Materials and methods br Results br

  2022-08-13

  

  Materials and methods Results Discussion In the absence of vascularization phenomena, endothelial cells (ECs) are among the most quiescent cells of the body [27]. ECs proliferation is significant during embryogenesis, as the vasculature is being formed, while in the adult life takes place o

• One class of microbial derived

  2022-08-13

  

  One class of microbial-derived metabolites that have received significant attention are the short-chain fatty acids (SCFA), which include butyrate, acetate and propionate. The production of SCFA occurs in the colon following microbial fermentation of dietary fibers and SCFA can also be consumed in c

• br Concluding Remarks and Future Perspectives Our understand

  2022-08-12

  

  Concluding Remarks and Future Perspectives Our understanding of substrate targeting mechanisms utilized by kinases has grown tremendously in the past few years, but challenges still remain in relating these mechanisms to the organization of complex signaling networks. Substrate prediction based o

• Pseudo-UTP receptor There are five subfamilies of

  2022-08-12

  

  There are five subfamilies of P-type ATPases (I-V), which transport metal ions or phospholipids across membranes (Palmgren and Nissen, 2011). Although our studies indicate that the P-type ATPase domain is important for function, how it contributes to cGMP production is currently unknown. The P-type

• br GSK The GSK family is highly conserved throughout

  2022-08-12

  

  GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Aminoallyl-dUT

• Decreasing GSK activity has therapeutic benefits in animal

  2022-08-12

  

  Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic microtubule inhibitor injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregul

• Lactate LA the end product of

  2022-08-12

  

  Lactate (LA), the end product of aerobic glycolysis, has been long neglected and seen as a byproduct until recently the findings for its important role in global gene transcription, cancer progression, functional polarisation of immune Tideglusib and the sustenance of stem cells [[7], [8], [9]]. La

• Although it is currently unknown why the longer

  2022-08-12

  

  Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the Methscopolamine receptor splice variant ERbeta2 identified in human and primate, but not other species (Si

• br Materials and methods br Results br Discussion and

  2022-08-12

  

  Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited

• G protein coupled receptor GPCR ligands can be

  2022-08-12

  

  G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not ex

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