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Herein we explored by docking studies the effectiveness of r
2020-10-08
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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br Conclusion New series of
2020-10-08
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 DDR mediated lysyl oxidase
2020-10-08
The DDR2-mediated lysyl oxidase induction in osteoblasts reported here is a novel function for this receptor. Various functions have been reported for DDR2. In an in-vitro study, Zhang and colleagues showed that DDR2 activation leads to Runx2 phosphorylation, which regulates osteoblast differentiati
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We show that direct contact with MSCs is necessary and
2020-10-08
We show that direct contact with MSCs is necessary and sufficient to induce DDR2 upregulation in breast cancer cells. DDR2 expression in MSC is required for collagen deposition and leads to increased DDR2 expression and activation in breast cancer cells. This paracrine-autocrine MSC-cancer cell axi
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An important strength of our study is the use
2020-10-08
An important strength of our study is the use of an elastic net regression model to select the variable and construct the model, which performed ideally in terms of both predictive accuracy and sparsity for the high-dimensional datasets [16]. As a result, the apparent predictive effect of multiple c
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The cysteinyl leukotrienes cysLTs LTC LTD
2020-10-08
The cysteinyl leukotrienes (cysLTs) LTC, LTD, and LTE are increased in the airways of asthmatic subjects, with the ability to induce bronchoconstriction, vascular permeability, and mucus secretion., , , , CysLTs are well established as mediators of allergic rhinitis and asthma on the basis of the e
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Our present data show that neuroleptics can affect CYP
2020-10-08
Our present data show that neuroleptics can affect CYP3A via a direct interaction with the enzyme and a significant indirect mechanism (enzyme regulation) produced in vivo. The obtained results revealed interactions of the neuroleptics (added in vitro to control liver microsomes, Model I) with rat C
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Previous studies revealed the expression of the CCR receptor
2020-10-08
Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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Our results implicate a critical role
2020-10-08
Our results implicate a critical role for CXCR-1 in promoting the migration of colonic tumor cells. Expression of this receptor, but not CXCR-2, increased significantly because of the EMT (Fig. 3). Moreover, although Clone A 9-amino Camptothecin receptor express comparable levels of both IL-8 recep
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Prostaglandins PGs are lipid mediators that
2020-10-08
Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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Currently approved anti obesity drugs for
2020-10-08
Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In geldanamycin to this, plant d
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br Results br Discussion This study assesses
2020-10-08
Results Discussion This study assesses impacts of HLA-DPB1 and CMV reactivation on GVHD, relapse, and OS after allo-HSCT. Here we demonstrate that HLA-DPB1 and CMV reactivation both increase aGVHD risk independently. Consistent with reported data, we show that HLA-DPB1 mismatching is associate
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Chemokine receptor expression in MCL is
2020-10-06
Chemokine receptor expression in MCL is shown in Table 1. CXCR4, CXCR5 and CCR6 protein was detected in the majority of patients [10], [72], [102], [118] and CX3CR1 was found to be present in up to 75% of cases depending on the method used to identify the receptor [103]. CCR7 was more highly express
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Resistance to SP is linked to point mutations
2020-10-05
Resistance to SP is linked to point mutations that accumulate at several sites in the dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) Senexin B of P. falciparum (Roper et al., 2003). These mutations have been identified in codons 16, 51, 59, 108, and 164 in the dhfr gene and codo
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br Experimental procedures br Introduction Protein kinases r
2020-10-05
Experimental procedures Introduction Protein kinases represent one of the largest enzyme Meropenem trihydrate in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activit
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