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The compounds were ranked based on
2020-11-06
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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For a physiologically relevant interaction ligand and recept
2020-11-06
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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Plants Cp are widely distributed in
2020-11-06
Plants Cp are widely distributed in the plant kingdom and are believed to act as virulence/defense factors for both hosts and pathogens. Cp are also found in plants, animals and bacteria and are known to be virulence factors involved in bacterial pathogenicity [29]. Further, Cp are involved in pepti
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br Pre clinical combination studies using
2020-11-05
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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Nucleocytoplasmic transport systems play a critical role in
2020-11-05
Nucleocytoplasmic transport systems play a critical role in intracellular localization and regulation of proteins in each cell. This balance is quite important and is typically uncontrolled in cancer cells. Specific localization of tumor suppressor and oncoproteins is quite important because any abn
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br Materials and methods br Results br
2020-11-05
Materials and methods Results Discussion Neointimal VSMC accumulation contributes considerably to vessel occlusion observed in both autologous vein graft degeneration [1], [2] and in-stent restenosis [26], [27]. In this study, the potential for retarding VSMC proliferation and hence amelior
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Brg is a core unit of BAF complex and
2020-11-05
Brg1 is a core unit of BAF complex and is required for the self-renewal and pluripotency of ESCs (Ho and Crabtree, 2010). We confirmed the interaction of DPF2 and BRG1 by immunoprecipitation and showed that these proteins extensively co-localize in the genome. Although both Brg1 and Dpf2 positively
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br Conclusion New series of thiazolo d pyridazine and imidaz
2020-11-05
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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Some mechanistic experiments performed in the early
2020-11-05
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Sennoside C mg from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This ev
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So far few studies have been
2020-11-05
So far few studies have been conducted on the role of chemokines in patients with PTSD and avoidant personality disorders. Ogłodek et al. [10] in her studies found an increase in the level of the chemokine CCL-5 in patients with avoidant personality disorder and general anxiety disorder (GAD) as com
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In the present study real time polymerase chain
2020-11-04
In the present study, real-time polymerase chain reaction also confirmed that gene expressions of RT1 class II, locus Bb (RT1-Bb) was up-regulated and Spi-B transcription factor (Spib) was downregulated at day 3 after the VMH lesions. These two genes work as one of immune responses. RT1-Bb controls
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br Mass spectrometry based technologies Oxysterols tend
2020-11-04
Mass spectrometry-based technologies Oxysterols tend not to be observed in global lipidomic analysis, whether shot-gun based electrospray ionisation – mass spectrometry (ESI-MS) or liquid chromatography (LC)-MS based. This is because of their comparatively low-abundance and poor ionisation charac
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One of the isolated interactors against Mulan Ube E
2020-11-04
One of the isolated interactors against Mulan259–352–Ube2E3 fusion bait was found to be the GABARAP protein, a known member of the Atg8 family that includes LC3 [20]. The Atg8 family-of-proteins are major players in autophagy/mitophagy since they are part of the autophagosome [20], [21], [22]. Our s
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COH inhibited global SUMOylation in cells and blocked the
2020-11-04
COH000 inhibited global SUMOylation in EI1 and blocked the E1 catalyzed attachment of SUMO to the corresponding conjugating enzyme Ubc9, but not the attachment of ubiquitin or NEDD8 to their respective E2s, confirming inhibition and specificity in cellulo. Consistent with previous studies inactivat
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Advances in the total chemical synthesis
2020-11-04
Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functi
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