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ALK fusion positive NSCLC is clinically actionable
2023-09-01
ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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Last decade has provided a
2023-09-01
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider
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br Adiponectin in prostate cancer PC was
2023-09-01
Adiponectin in prostate cancer PC was documented as the leading type of malignancy in males in the US with respect to both the estimated number of cases (22,800) and deaths (27,540) (Siegel et al., 2016). Studies have reported an association between low APN levels and the progression of PC (Micha
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br There are three types of HT
2023-09-01
There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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Derivatives of M that possess
2023-08-31
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Adox australia to maintain 5-HTR antagonist properties as (+)-M100907 was demon
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Herein we disclose novel dihydropyrano c pyrazoles that inhi
2023-08-31
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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br Experimental section br Competing interests br Author s c
2023-08-31
Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig
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In Rainey et al published the results
2023-08-31
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Because ASK signaling in microglia and astrocytes is
2023-08-31
Because ASK1 signaling in microglia and astrocytes is important during EAE, we hypothesized that a combination therapy that targets T cells along with microglia and astrocytes would further ameliorate the severity of EAE. We tested this hypothesis by applying valproic Dihydrodaidzein (VPA)—a short-
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Among steroid saponins ginsenosides are the active component
2023-08-31
Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid
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These PrPIF are detected in untreated brain extracts but are
2023-08-31
These PrPIF are detected in untreated VU590 hydrochloride extracts but are consistently enriched following proteinase K (PK) treatment. The biochemical characterization of pathologic PrP has been carried out in most hereditary PrP cerebral amyloidosis associated with PrP mutations and the biochemic
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Activation of AhR is also known
2023-08-31
Activation of AhR is also known to upregulate the expression of AhRR (AhR repressor), an inhibitor protein of AhR [29]. However, the exact mechanism by which AhRR represses AhR signaling is not well understood. The initial study by Mimura and colleagues suggested that AhRR is capable of directly com
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Plant material and growth conditions Arabidopsis thaliana ec
2023-08-30
Plant material and growth conditions. Arabidopsis thaliana ecotype Columbia was grown on a mixture of soil, vermiculite, and perlite (4:2:1) with a 16h light/8h dark luteolin in a temperature-controlled growth room (22°C), unless indicated otherwise. Molecular cloning and plant transformation. The
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EGFR Inhibitor synthesis Because of its role in
2023-08-30
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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Drug resistance development often involves structurally un
2023-08-30
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 SCF, murine recombinant protein receptor are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream a
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