Steroidogenic CYP enzymes are important in catalyzing the biosynthesis of various hormones including aldosterone,and therefore are promising drug *** studies reveal that besides its classical functions in regulating t...
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Steroidogenic CYP enzymes are important in catalyzing the biosynthesis of various hormones including aldosterone,and therefore are promising drug *** studies reveal that besides its classical functions in regulating the homeostasis of body fluid and electrolytes,aldosterone also induces ROS and inflammation as well as up-regulates a series of
β-carboline is an important thicyclic indole alkaloid with important antitumor *** this paper,β-carboline compounds with different subsituents was synthesized from tiypsamine,the structures of these compounds were c...
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β-carboline is an important thicyclic indole alkaloid with important antitumor *** this paper,β-carboline compounds with different subsituents was synthesized from tiypsamine,the structures of these compounds were characterized by mass pectrometry,hydrogen spectrometry and carbon ***,the antitumor activity of these compounds was investigated and the structure-activity relationship was discussed.
Therapeutic interventions that target virulence rather than the survival of the bacterial pathogens have received immense attention,as these approaches allow selective disarming the pathogen and preserving the integri...
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Therapeutic interventions that target virulence rather than the survival of the bacterial pathogens have received immense attention,as these approaches allow selective disarming the pathogen and preserving the integrity of the host *** Chinese Medicines(TCMs) have been historically used to treat bacterial ***,the molecules responsible for these anti-infective properties and their potential mechanisms of
Proteolysis-Targeting Chimeras are bifunctional small molecules designed to hijack the powerful cellular degradation machinery for inducing targeted protein degradation and this approach has recently gained momentum a...
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Proteolysis-Targeting Chimeras are bifunctional small molecules designed to hijack the powerful cellular degradation machinery for inducing targeted protein degradation and this approach has recently gained momentum as a new therapeutic strategy for small-molecule drug *** this lecture,I will present our recent research in the design and
Iriomoteolide-13a（1） was isolated from a benthic dinoflagellate Amphidinium sp.（strain KCA09053）. Its complex molecular architecture poses a significant challenge to synthetic *** connection with our on-going rese...
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Iriomoteolide-13a（1） was isolated from a benthic dinoflagellate Amphidinium sp.（strain KCA09053）. Its complex molecular architecture poses a significant challenge to synthetic *** connection with our on-going research program on diverted total synthesis of marine macrolides such as amphidinolide Y and T2, iriomoteolide-1a, and laingolide
Drug discovery,from its traditional area of lead discovery and optimization,has extended toward two directions:upstream for target identification and validation,and downstream for preclinical *** directions are associ...
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Drug discovery,from its traditional area of lead discovery and optimization,has extended toward two directions:upstream for target identification and validation,and downstream for preclinical *** directions are associated with discovering new pathogenic pathways or re-evaluating existing *** biology is a new discipline to fulfill such kind of
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
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