Showing papers in "Biochemical Pharmacology in 2016"
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TL;DR: This review has thoroughly covered recent advances in the understanding of the functional polarization of brain and peripheral glia and its implications in neuroinflammation and neurological disorders.
198 citations
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TL;DR: An updated view of the structure and function of bromodomains is presented, the development of bRomodomain inhibitors and their potential therapeutic applications are traced, and the current challenges and future directions of this vibrant new field in drug discovery are surveyed.
190 citations
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TL;DR: The therapeutic potential of this family of receptors to treat pathologies where inflammation is a major factor such as type 2 diabetes, whether by the use of novel synthetic molecules or by the modulation of the individual's diet is assessed.
187 citations
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TL;DR: Rationally developed nanoparticle vaccines are one of the most promising candidates for the future of vaccine development, which allows for antigens to be expressed on a particulate delivery system.
179 citations
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TL;DR: Understanding how excess ECM deposition in the adipose tissue deteriorates insulin sensitivity would provide hints to develop a new therapeutic strategy for the treatment of insulin resistance and type 2 diabetes.
154 citations
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TL;DR: This review provides an overview of the positive and negative regulatory role of TRAF2 in different TNFR1 and TNFR2 signaling pathways, and elaborate on some possible strategies to modulate TRAf2 function in the context of therapeutic targeting in autoimmunity and cancer.
139 citations
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TL;DR: Interestingly, phytoalexins, exemplified by quercetin glucuronides and glucosinolate-derived isocyanates, are known insect attractant pigments in plants, and antioxidants, anti-inflammatory and chemopreventive compounds of humans, it is to be anticipated that phytochemicals may provide a rich source in beneficial drugs.
137 citations
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TL;DR: Information is gathered on the currently used experimental animal models of both Type 1 and Type 2 diabetes and their advantages and disadvantages for research purposes and details the factors that should be taken into account in their use.
126 citations
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TL;DR: TAF has a much lower risk of kidney toxicity or bone density changes than TDF, and also offers long-term potential in the pre-exposure prophylaxis (PrEP) of HIV infections.
122 citations
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TL;DR: A deeper knowledge of the mechanisms involved in chondrocyte aging could identify potential targets for the treatment of OA, a prevalent and therapeutic-orphan disease.
117 citations
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TL;DR: Unmet challenges are discussed, including recognition by the receptors of diverse ligands and how biased signals mediate different biological effects, to discuss unmet challenges of neutrophil FPRs.
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TL;DR: The ability of DMF to inhibit NLRP3 inflammasome activation and its potential use in the treatment ofNLRP3-associated diseases was demonstrated and increased glutathione induced by DMF demonstrated its potential antioxidant capacity.
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TL;DR: The emerging field of ADC/IO combination research is reviewed, with a focus on how to optimally combine both modalities as synergistic activities between IO compounds and ADCs may increase the formation of tumor specific immunological memory, ultimately leading to durable responses in a larger fraction of cancer patients.
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TL;DR: New paradigms in CKR signal transduction are explored by considering studies that depict a more intricate architecture governing the consequences of chemokine-CKR interactions, within a rapidly changing landscape in which CKR signaling is influenced by receptor PTMs, chemokin and CKR dimerization, and endogenous non-chemokine ligands.
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TL;DR: In this paper, the IncuCyte ZOOM real-time imaging platform for macrophage phagocytosis based on pHrodo® pathogen bioparticles, which only fluoresce when localized in the acidic environment of the phagolysosome.
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TL;DR: Taken together, the UPR appears to play an important role in GBM tumor progression and is a promising target for developing novel therapeutic interventions.
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TL;DR: The goal of this review is to summarize the body of evidence in regard to FFA4 signal transduction, its mechanisms of regulation, and its functional role in a variety of tissues.
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TL;DR: In this article, the authors applied the pharmacological HDAC 3-selective inhibitor RGFP966, which attenuated pro-inflammatory gene expression in models for inflammatory lung diseases, and a robust decrease of the transcriptional activity of NF-κB p65 was observed.
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TL;DR: Targeting TrxR discloses a novel molecular mechanism underlying the cellular action of ATL, and sheds light in considering the usage of ATL as a potential cancer chemotherapeutic agent.
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TL;DR: mutagenesis and molecular modeling studies of P-gp led to the identification of a pair of phenylalanine-tyrosine structural motifs in the transmembrane region that mediate the inhibition of ATP hydrolysis by certain drugs, with high affinity (IC50's ranging from 10 to 30nM).
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TL;DR: The results here provide a novel combination treatment strategy, especially for patients with 5-FU-resistant tumors expressing low level of BAX, and it is proposed that BAX expression may be a predicted and prognosis marker of5-FU involved chemotherapy.
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TL;DR: It is suggested that resveratrol restored ovarian function through increasing AMH levels, and diminishing ovarian inflammation, predominantly via upregulation of PPAR-γ and SIRT1 expression leading to inhibition of NF-κB provoked inflammatory cytokines.
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TL;DR: It is demonstrated that the pro-inflammatory and cancer-promoting effects of HCD are mediated by the activation of NLRP3 inflammasome, which extended the knowledge on how dietary choices can influence processes involved in chronic inflammatory disorders and colorectal cancer.
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TL;DR: The ability of CORM-401 to release multiple CO, its sensitivity to oxidants which increase CO release, and its vascular and pro-angiogenic properties highlight new advances in the design of CO-releasing molecules that can be tailored for the treatment of inflammatory and oxidative stress-mediated pathologies are examined.
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TL;DR: It is suggested that the PPAR-γ agonist pioglitazone prevents NF-κB activation in cisplatin nephrotoxicity through a reduction in p65 acetylation via the AMPK-SIRT1/p300 pathway.
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TL;DR: The data suggest that CES1 genetic variants and gender are important contributing factors to variability in DABE activation in humans and a personalized DabE treatment approach based on patient-specific CES1 genotypes and sex may have the potential to improve the efficacy and safety of DABe pharmacotherapy.
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TL;DR: Recent advances in targeting transcription factors with small compounds, the challenges that are related to the complex function and regulation of these proteins and also the possible future directions and applications of transcription factor drug targeting are discussed.
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TL;DR: Using human PANC-1 and MIA PaCa-2 cells, it is demonstrated that the bioactive sphingolipid ceramide 1-phosphate (C1P) increases pancreatic cancer cell migration and invasion, and it is suggested that targeting CerK expression/activity and C1P may be relevant factors for controlling pancreaticcancer cell dissemination.
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TL;DR: Marmoset and cynomolgus monkey P450 enzymes showed high sequence homology to their human counterparts and generally had similar substrate recognition functionality to human P 450 enzymes; however, they also possibly contribute to limited specific differences in drug oxidative metabolism partly due to small differences in amino acid residues.
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TL;DR: It is found that DIM dose-dependently inhibited the growth of gastric cancer cells in vitro and in vivo and miR-30e-ATG5 modulating autophagy inhibit the proliferation of gastrics cancer cells.