• br Identification of the kinase that

  2024-09-27

  

  Identification of the kinase that phosphorylates P450c17 The first Ser/Thr kinase that phosphorylates P450c17 was identified only recently. Of the 518 kinases in the human ‘kinome’ 278 are Ser/Thr kinases (Manning et al., 2002), but microarrays identified only 145 Ser/Thr kinases in human NCI-H29

• br Materials and methods br Results br

  2024-09-27

  

  Materials and methods Results Discussion Author contributions JH purified protein, performed vanadate inhibition experiments, crystallized, collected data, determined and refined the ATX-VO5 structure, analysed all the structures, prepared the displayed items and supervised ALHE; WJK con

• Here we report discovery of highly selective pan

  2024-09-27

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Q-VD(OMe)-OPh bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. T

• A high throughput screening campaign led to the discovery

  2024-09-27

  

  A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity

• Baicalin Another major problem leading to implant failures

  2024-09-27

  

  Another major problem leading to implant failures is post-implant infections, majorly due to bacteria adhesion [13,36,37]. A significant decrease in bacterial counts (~65–90%) has been observed in HA and/or CNT-based composites reinforced with 2.5–10 wt% nano Ag [13,38], thus, drawing the conclusion

• br Materials and methods br Results br

  2024-09-26

  

  Materials and methods Results Discussion Prostate cancer is the most common cancer in men in the United States and the second leading cause of cancer death. Therapeutic interventions include mainly: radical prostatectomy or radiation therapy (RT), with or without androgen deprivation therap

• Overexpression of AR can lead to sorbitol accumulation leadi

  2024-09-26

  

  Overexpression of AR can lead to sorbitol accumulation, leading to diabetic complications (Ransohoff and Cardona, 2010). Therefore, AR is an important enzyme in the growth and development of organisms. With the aim of inhibiting the activity of AR in diabetic patients, screening for inhibitors and i

• mth1 pathway br Regulation of AHR Activity AHR

  2024-09-26

  

  Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex

• In particular we focused our attention on beta adrenergic

  2024-09-26

  

  In particular, we focused our attention on beta2 adrenergic receptors, since their commercial inhibitors are effective in lowering IOP, the primary indication of glaucoma. The hypotensive action of a commercial sequence of beta2 adrenergic receptor siRNA was tested in rabbits. The results confirmed

• br Funding This work was supported by Arena Pharmaceuticals

  2024-09-26

  

  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

• br Materials and methods br Results

  2024-09-26

  

  Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly

• br Funding br Introduction l

  2024-09-26

  

  Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side

• During myeloid cell maturation expression of LO mRNA

  2024-09-26

  

  During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly

• br Methods br Results br Discussion br Acknowledgements

  2024-09-26

  

  Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V

• br Introduction Nausea and vomiting are among the most distr

  2024-09-26

  

  Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co

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