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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2020-09-24
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase INCB 018424 [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and le
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Our structures also provide new insights
2020-09-24
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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br Conflicts of interest br
2020-09-24
Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest
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T helper Th cells play a central
2020-09-24
T helper (Th) CM-272 mg play a central role in activation of immune system against infectious agents through secretion of lymphokines or cytokines. African trypanosomes target the Th cells and alter their activation, possibly for their own survival and perpetuity (Namangala, 2011). Trypanosoma bruce
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In this report we established mouse
2020-09-24
In this report, we established mouse models suitable for human retinal cell transplantation by introducing phosphodiesterase 6B (Pde6b) mutant allele from retinal degeneration (rd) mouse models into NOG background. Pde6b (rd1) and Pde6b (rd10) mice are well-studied and frequently used animal models
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Enolase as a plasminogen receptor and activator localized on
2020-09-23
Enolase, as a plasminogen receptor and activator localized on the surface of several helminths, can interact with the host fibrinolytic system (Yang et al., 2010, Du et al., 2009, de la Torre-Escudero et al., 2010). The enzyme is also one of excretory/secretory (ES) products in some helminths, such
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To our knowledge this is the first report of an
2020-09-23
To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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In regards to regional variation in metabolic behavior of ad
2020-09-23
In regards to regional variation in metabolic behavior of adipose tissue, subcutaneous adipose tissue transplantation has been shown to reprogram visceral adipose tissue to have subcutaneous-like phenotypic behavior, whereas visceral-to-subcutaneous transplantation does not promote a more detrimenta
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In accordance with its original discovery EBI
2020-09-23
In accordance with its original discovery, EBI2 may play its major role in response to viral infections or in a pathological context such as in autoimmunity. Although we found a significant delay of onset in the Th17 transfer EAE model, active EAE was unchanged in absence of EBI2. At the moment, we
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HCV has evolved mechanisms to evade humoral immune responses
2020-09-23
HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 NHS Biotin of the N-terminus of E2, which is referred to as the hypervariable
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E protein was studied using specific anti E
2020-09-23
E1 protein was studied using specific anti-E1 Cy3 maleimide (non-sulfonated) in wild type cells and in transfected cells overexpressing the enzyme. The results revealed several unusual characteristics, which are unique to this ubiquitin-activating enzyme. The E1 was translated as a full-length prote
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br Experimental Procedures br Author Contributions M B with
2020-09-23
Experimental Procedures Author Contributions M.B., with input and help from T.T.H., conceived the project, designed and performed the experiments, analyzed the data, and wrote the manuscript. B.B.B. and F.D.M. synthesized the wild-type and (nonhydrolyzable, NH) Ub tetramers and contributed Fig
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BR stimulated PA formation via the
2020-09-22
BR-stimulated PA formation via the DGK pathway might have many effects in regulation of cell metabolism. For example, PA originated from DGKs pathway plays important roles in activation of NADPH oxidases, thus turning on ROS signaling [23]. PA is also connected to regulation of respiration processes
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br Conclusion New series of
2020-09-22
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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The discoidin domain receptors DDR
2020-09-22
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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