World Health Organization estimated that 71 million people worldwide were chronically infected with hepatitis C virus(HCV) in 2015,representing approximately 1%of the global *** treatment,chronic HCV infection could l...
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World Health Organization estimated that 71 million people worldwide were chronically infected with hepatitis C virus(HCV) in 2015,representing approximately 1%of the global *** treatment,chronic HCV infection could lead to severe liver damage and life-threatening *** example,the risk of cirrhosis of the liver among patients with
Histone methyltransferases(HMTs,also known as protein methyltransferases) have been increasingly pursued as potential therapeutic *** quality selective small-molecule inhibitors of HMTs will permit biological and ther...
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Histone methyltransferases(HMTs,also known as protein methyltransferases) have been increasingly pursued as potential therapeutic *** quality selective small-molecule inhibitors of HMTs will permit biological and therapeutic hypotheses concerning these enzymes to be tested-in cell-based and/or animal models with high *** laboratory has pursued multiple complementary structure-based
As the largest family of integral membrane proteins,G-protein-coupled receptors(GPCRs)comprise the largest class of therapeutic targets that aimed by approximately 45%of modern medicinal ***,understanding the signal t...
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As the largest family of integral membrane proteins,G-protein-coupled receptors(GPCRs)comprise the largest class of therapeutic targets that aimed by approximately 45%of modern medicinal ***,understanding the signal transduction,as well as the agonist/antagonist mechanism of the GPCRs,is pivotal in drug discovery and new therapeutic
Competitive inhibition of KRAS-PDE5 interaction by small molecules can be used to reduce the plasma membrane localization of KRAS and its oncogenic signaling,which represents a novel strategy for cancer ***,an unprece...
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Competitive inhibition of KRAS-PDE5 interaction by small molecules can be used to reduce the plasma membrane localization of KRAS and its oncogenic signaling,which represents a novel strategy for cancer ***,an unprecedented chiral binding pattern was observed for inhibitors of KRAS-PDES *** screening and X-ray
A new series of substituted piperazine-1-yl-pyrimidine derivatives was designed and synthesized as HIV-1 RT non-nucleoside *** N-substituted aromatic groups were incorporated into the piperazine ring through a simple ...
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A new series of substituted piperazine-1-yl-pyrimidine derivatives was designed and synthesized as HIV-1 RT non-nucleoside *** N-substituted aromatic groups were incorporated into the piperazine ring through a simple and practical synthetic route to investigate their biological activity against wild-type and resistant strains of *** of the target compounds were evaluated as HIV-1 reverse transcriptase inhibitors in MT-4 cell *** biological testing results showed that six of these compounds displayed inhibitory activities against the wild-type strain,among which compound 1 t exhibited the most potent anti-HIV activity with an EC value of 3.36μ*** modeling studies could provide the valuable information for developing new anti-HIV-1 agents.
Nitrile-containing pharmaceuticals emerge as potential leads in clinical development thanks to the unique nitrile *** the halogen or carbonyi bioisostere,this small but robust unit is not metabolized,hence to endow th...
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Nitrile-containing pharmaceuticals emerge as potential leads in clinical development thanks to the unique nitrile *** the halogen or carbonyi bioisostere,this small but robust unit is not metabolized,hence to endow the drug candidates with diverse biological activities. Nucleoside analogues are of considerable importance in searching for novel therapeutics to combat various diseases. In the past years,we have developed various triazole nucleosides bearing aromatic functionalities on the nucleobase. Considering the bioactivity of nitrile,we are recently focusing on the transformation of the exocyclic carboxylamide in triazole heterocycle to the nitrile group with the aim to enrich the molecular diversity of aryltriazole nucleosides(Figure 1).The obtained nitrile-containing aryltriazole nucleosides exhibit potent apoptosis-related anticancer activity(Figure 1),which open a new avenue to discover structurally novel nucleosides to treat cancers and related diseases.
Targets identification of bioactive molecules is of great importance in revealing mechanism of action,explaining potential adverse effects,and mining novel therapeutic *** on different principles,several approaches fo...
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Targets identification of bioactive molecules is of great importance in revealing mechanism of action,explaining potential adverse effects,and mining novel therapeutic *** on different principles,several approaches for target identification have been *** those approaches,activity based protein profiling(ABPP) is the mostly used one which has
AMP-activated protein kinase(AMPK) is a key sensor and regulator of energy balance at the cellular level and has been placed at the center stage in studies of type 2 diabetes mellitus(T2DM),obesity,hyperlipidima and r...
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AMP-activated protein kinase(AMPK) is a key sensor and regulator of energy balance at the cellular level and has been placed at the center stage in studies of type 2 diabetes mellitus(T2DM),obesity,hyperlipidima and related metabolic *** regulates metabolism by activating ATP-generating pathways such as glycolysis and fatty acid ***
Chronic fibroproliferative disease is a major cause of death in the industrialized world,placing a substantial burden on healthcare *** in the liver,long-term liver fibrosis may lead to diseases such as cirrhosis,port...
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Chronic fibroproliferative disease is a major cause of death in the industrialized world,placing a substantial burden on healthcare *** in the liver,long-term liver fibrosis may lead to diseases such as cirrhosis,portal hypertension,and liver necrosis,which seriously affect people's lives
Overexpression and somatic heterozygous mutations of EZH2,the catalytic subunit of polycomb repressive complex 2(PRC2),are associated with several tumor ***2inhibitor,EPZ-6438(tazemetostat),demonstrated clinical effic...
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Overexpression and somatic heterozygous mutations of EZH2,the catalytic subunit of polycomb repressive complex 2(PRC2),are associated with several tumor ***2inhibitor,EPZ-6438(tazemetostat),demonstrated clinical efficacy in patients with acceptable safety profile as ***,another subunit of PRC2 complex,is essential for its
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