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br Acknowledgments This study was supported
2022-04-09

Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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As a part of our continuing efforts towards discovery of
2022-04-09

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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br Material and methods br Acknowledgements and funding The
2022-04-09

Material and methods Acknowledgements and funding The authors thank Katharina Elsässer for technical support and Emma Esser for careful editing of the manuscript. We also thank Marcus Conrad for providing Liproxstatin-1 and advisory comments and discussion on the manuscript. This work was part
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br Materials and methods br Results br Conclusions
2022-04-09

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of st
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In conclusion we have shown that the brain
2022-04-09

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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The site of paracetamol action remains controversial Some pu
2022-04-09

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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Although epigenetic mechanisms are implicated in
2022-04-09

Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Dual acting HR antagonists While the present
2022-04-09

Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4
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We found statistically significant association between p HER
2022-04-09

We found statistically significant association between p95-HER2 levels and hormone receptor status, Ki-67 AY 9944 dihydrochloride and metastatic regions (p = 0.004, 0.05) and the median OS was 27.66 months versus 24.02 months for p95-HER2 positive and p95-HER2 negative BC patients respectively (p
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br Autophagy and HBV induced HCC Researchers
2022-04-08

Autophagy and HBV-induced HCC Researchers have demonstrated downregulation of autophagy in HBV transgenic liver tumors of mouse models and in human HBV-induced HCC specimens. Kotsafti and his colleagues declared that the expression level of BECN1 mRNA in HCC specimens was considerably lower than
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Curcumin is a major yellow pigment in
2022-04-08

Curcumin is a major yellow pigment in turmeric ground rhizome of Curcuma longa Linn, which is used widely as a spice and coloring agent in several foods such as curry, mustard and potato chips as well as cosmetics and drugs (Okada et al., 2001, Joe et al., 2004). Curcumin represents a class of anti-
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definitely Receptor guanylyl cyclases play essential roles i
2022-04-08

Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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pilocarpine hcl Whereas binding of activated RhoA to the
2022-04-08

Whereas binding of activated RhoA to the PH domains of the RhoGEFs is proposed to mediate positive feedback regulation (Chen et al., 2010b, Medina et al., 2013), the sequestration of p190RhoGEF by activated Rac1 reveals a novel putative physiological role, that is to utilize Rac1 to directly drive r
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GSTP has an antiapoptotic activity that is mediated by
2022-04-08

GSTP1 has an antiapoptotic activity that is mediated by the inhibitory interaction with JNK1. Our data suggest that GSTP1 treatment is associated with a significant down-regulation of caspase expression. This might explain the reduction in infarct-related cardiomyocyte death and saving the cardiomyo
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br Introduction Depressive disorder is a syndrome characteri
2022-04-08

Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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