• br Future perspectives Understanding how peptides are degrad

  2020-09-25

  

  Future perspectives Understanding how peptides are degraded, particularly those which may be therapeutically useful, such as GLP-1, has proved to be invaluable in providing a rationale for the development of a novel class of therapeutic agents. However, while DPP-4 plays an important role in the

• br Introduction Coping with DNA damage is possible

  2020-09-25

  

  Introduction Coping with DNA damage is possible thanks to surveillance mechanisms (checkpoints), that detect the problem and promote its solution [1], [2], and to repair and tolerance pathways that remove the lesions or reduce the damage consequences [3], [4]. Failures in these processes have a h

• Based on our studies presented above atipamezole can

  2020-09-24

  

  Based on our studies presented above, atipamezole can be used as a new in vitro and in vivo tool Garcinol as a pan-CYP inhibitor for CYP mediated metabolism study. It carries many unique characteristics compared to ABT which is currently being widely used for this purpose. These new characteristics

• Alvocidib flavopiridol is a piperidine chromenone http www

  2020-09-24

  

  Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK

• br CDKs as Direct Coactivators

  2020-09-24

  

  CDKs as Direct Coactivators of Proinflammatory Transcription Factors CDKs fuel inflammation by triggering the function of proinflammatory transcription factors such as NF-κB, STAT3, and AP-1. This is achieved at two levels because CDKs can affect gene expression by targeting global transcription

• Using characteristic features of ECM proteins and a computat

  2020-09-24

  

  Using characteristic features of ECM proteins and a computational pipeline combining interrogation of protein and gene databases, we previously defined the matrisome as the ensemble of ECM and ECM-associated proteins [[16], [17], [18]]. In mammals, the matrisome represents 4% of the genome, or appro

• It is now known that

  2020-09-24

  

  It is now known that cholinergic signaling plays a vital role in controlling many peripheral functions including skeletal and smooth muscle contraction, autonomic postganglionic neuron activation, parasympathetic end-organ activation (e.g., salivary, lacrimal and bronchial glands), regulation of car

• The upregulation of PTGS and PTGS in

  2020-09-24

  

  The upregulation of PTGS1 and PTGS2 in late gestation in mares could be linked to the high levels of estrogens produced by the fetoplacental unit. Estrogens are thought to be effective stimulators of prostaglandin production by potentially up regulating PTGS2 expression. Although a recent publicatio

• Our recent QTL mapping study revealed that the adaptor genes

  2020-09-24

  

  Our recent QTL mapping study revealed that the adaptor genes, including the NCK genes and the ABI genes, are located within the genomic regions harboring the most significant QTL (Zhou et al., 2017), suggesting that these genes could be involved in the determination of resistance, and possibly throu

• Another important new result that has expanded

  2020-09-23

  

  Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f

• From an industrial perspective the low turnover numbers and

  2020-09-23

  

  From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo

• Among our patients with anti enolase

  2020-09-23

  

  Among our patients with anti-enolase drusen, those with a relatively short duration from the onset of visual symptoms to the first visit tended to have normal structure of photoreceptors with preserved visual function, despite the presence of drusen-related RPE abnormalities (Cases 1-3 and 8). In co

• br Introduction Epithelial mesenchymal transition EMT is a b

  2020-09-23

  

  Introduction Epithelial-mesenchymal transition (EMT) is a biological process by which epithelial inhibitor of apoptosis proteins lose cell polarity and cell-cell adhesion, and gain mesenchymal features with an increase of migratory and invasive properties [1]. EMT is essential for mesoderm forma

• br Experimental Procedures br Author Contributions br Acknow

  2020-09-23

  

  Experimental Procedures Author Contributions Acknowledgments Research in the Davis laboratory was supported by grants 4R37NS019904, 5R01NS052351, and 1R35NS097224 from NINDS. Research in the Martemyanov laboratory was supported by grants DA036596 and DA026405 from NIDA, and MH105482 from NI

• Our recent discovery M P

  2020-09-22

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

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