• Antioxidant flavonoid Small kinase inhibitors have been deve

  2025-01-26

  

  Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha

• Pyrimidine is the important pharmacology

  2025-01-26

  

  Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the 9184 core as well as t

• Recent studies have indicated that V ATPase activity negativ

  2025-01-26

  

  Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ PBIT have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells' acidit

• Why do glutamate and glycine bind to the receptor in

  2025-01-26

  

  Why do glutamate and glycine bind to the Ac-YVAD-CHO in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lob

• Atherosclerosis is a chronic lipid metabolism

  2025-01-26

  

  Atherosclerosis is a chronic lipid metabolism disorder linked with lipid accumulation within the arterial wall and subsequent formation of foam cells and vascular disease [96], [97]. The level of apelin is decreased in human atherosclerotic coronary arteries [4], and coronary collateral formation in

• Pathological angiogenesis occurs when an imbalance of endoge

  2025-01-24

  

  Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance

• br Introduction The development and plasticity

  2025-01-24

  

  Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo

• The clinical impact of our

  2025-01-24

  

  The clinical impact of our findings is also supported by our earlier report that the level of 12-LOX expression was correlated with the tumor stage and grade [17], [52] and that overall, 38% of patients demonstrated elevated levels of 12-LOX in prostate cancer tissue compared with their matching nor

• br Understanding AD through Transcriptome Analysis Both clas

  2025-01-24

  

  Understanding AD through Transcriptome Analysis Both classical gene discovery and pathway-based analysis of AD GWAS shed light on the range of biological processes that contribute to AD in addition to amyloid pathology. The straightforward interpretation and functional investigation of the associ

• Sphingolipids such as ceramides and glucosylceramides are an

  2025-01-24

  

  Sphingolipids, such as ceramides and glucosylceramides, are an important class of bioactive lipids. The levels of these lipids change as a function of adipose tissue mass and functionality, and are partially driven by cellular availability of palmitoyl-CoA. Aberrant accumulation of ceramide, glucosy

• br Funding This work was supported by Arena Pharmaceuticals

  2025-01-24

  

  Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo

• In addition we performed Western blot analysis of different

  2025-01-24

  

  In addition, we performed Western-blot analysis of different areas of mouse brain with L-690,330 receptor against mAck1 (Ureña et al., 2005). The data obtained showed a high rate of expression in neocortex, hippocampus, cerebellum, and brainstem (Fig. 4). More moderate levels of expression were seen

• It was previously demonstrated that dissociation of

  2025-01-23

  

  It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat

• br Acknowledgements br Introduction Double stranded

  2025-01-23

  

  Acknowledgements Introduction Double-stranded DNA breaks (DSBs) are among the most deleterious DNA lesions that threaten genomic integrity. DSBs are generated not only by exogenous DNA-damaging agents but also by normal cellular processes such as V(D)J recombination, meiosis, and DNA replicati

• br Results br Discussion Context specific and dynamic post t

  2025-01-23

  

  Results Discussion Context-specific and dynamic post-translational protein modifications are well-established regulators of the signaling pathways that protect eukaryotic DNA integrity during the tremendous task of replication. Advancements in speed, resolution, and sensitivity of MS-based tec

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