Janus kinases(JAKs) are essential signaling mediators downstream of many pro-inflammatory cytokines,and small-molecule inhibitors of JAKs have gained traction as safe and efficacious options for the treatment of infla...
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Janus kinases(JAKs) are essential signaling mediators downstream of many pro-inflammatory cytokines,and small-molecule inhibitors of JAKs have gained traction as safe and efficacious options for the treatment of inflammation-driven pathologies such as rheumatoid arthritis,psoriasis and inflammatory bowel *** first-in-class JAK3 inhibitor tofacitinib blocks
The nuclear estrogen-related receptorα(ERRα) plays a central role in the regulation of expression of the genes involved in mitochondrial biogenesis and oxidative *** molecular ERRαagonist is considered as novel the...
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The nuclear estrogen-related receptorα(ERRα) plays a central role in the regulation of expression of the genes involved in mitochondrial biogenesis and oxidative *** molecular ERRαagonist is considered as novel therapeutic strategy for metabolic ***,the tiny binding pocket of the ERRαligand binding domain(LBD)makes it"an intractable molecular target".Herein,we report the identification of the arguably
The chemokine receptor,CXCR4,is a seven transmembrane,G-protein coupled receptor whose only endogenous ligand is the protein,CXCL12(also known as SDF-1).These receptors play a crucial role in a variety of important no...
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The chemokine receptor,CXCR4,is a seven transmembrane,G-protein coupled receptor whose only endogenous ligand is the protein,CXCL12(also known as SDF-1).These receptors play a crucial role in a variety of important normal and aberrant physiological processes,including chemotaxis,metastasis,angiogenesis and tumor *** it is highly overexpressed in more than 248 hematopoietic and solid cancers,compounds that can
The 90 kDa heat shock proteins(Hsp90) are responsible for the conformational maturation of more than 300 protein substrates,many of which are involved in signaling cascades that are hijacked during malignant *** a res...
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The 90 kDa heat shock proteins(Hsp90) are responsible for the conformational maturation of more than 300 protein substrates,many of which are involved in signaling cascades that are hijacked during malignant *** a result,Hsp90 has emerged as a promising anti-cancer target In fact,17 small molecules have been evaluated in clinical trials,however 13 have already *** there are several reasons for their failure,the
Prodrug approaches are often used to solve drug delivery *** doing so,the chemistry needed to bioreversibly derivatize the drug molecule is the *** this line,bioreversible derivatization of gasotransmitters such as ni...
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Prodrug approaches are often used to solve drug delivery *** doing so,the chemistry needed to bioreversibly derivatize the drug molecule is the *** this line,bioreversible derivatization of gasotransmitters such as nitric oxide,hydrogen sulfide and carbon monoxide are especially ***,the chemistry used to prepare antibody-drug conjugates also has much room for *** presentation will discuss some unique chemistry developed for the preparation of prodrugs of carbon monoxide and hydrogen sulfide as well as a new approach to prodrug activation through enrichment.
The first-generation JAK inhibitors Tofacitinib and Ruxolitinib are considered as promising therapeutics for the treatment of RA or ***,their side effects such as anemia limited their use possibly due to low selectivi...
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The first-generation JAK inhibitors Tofacitinib and Ruxolitinib are considered as promising therapeutics for the treatment of RA or ***,their side effects such as anemia limited their use possibly due to low selectivity of the drugs（dose-limiting） .Selective inhibition of JAK kinases within the JAK family may lead to maximum efficacy with minimized undesired off-target effects and to understanding the role of individual JAK isoforms in disease. We have discovered a class of novel,quinazoline derivatives as potent and selective JAK *** of SAR studies and profiling will be discussed in details.
4’-Ethvnyl-2-fluoro-2’-deoxy-2’-β-fluoroadenosine(1) was designed and synthesized as a novel HTV reverse *** vitro evaluation demonstrated that nucleoside 1 possesses potent antiviral activity against HIV-1 infect...
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4’-Ethvnyl-2-fluoro-2’-deoxy-2’-β-fluoroadenosine(1) was designed and synthesized as a novel HTV reverse *** vitro evaluation demonstrated that nucleoside 1 possesses potent antiviral activity against HIV-1 infection(ECm = 0.9 nM) and low cytotoxicity(CC>>100μM).
Most lung cancer patients were diagnosed at advanced stage,therefore,local treatment for cure is often *** treatment is the mainstay for advanced stage nonsmall cell lung cancer ***-based chemotherapy has become stand...
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Most lung cancer patients were diagnosed at advanced stage,therefore,local treatment for cure is often *** treatment is the mainstay for advanced stage nonsmall cell lung cancer ***-based chemotherapy has become standard treatment *** new chemotherapy were designed and improved treatment outcome for *** year 2000,small molecules act as targeted therapy has changed the treatment paradigm
A series of novel gossypol Schiff bases were identified much potent(10-100 fold) than the gossypol and its known Schiff base derivatives for the anticancer activity.[1]This is the first example for Gossypol Schiff bas...
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A series of novel gossypol Schiff bases were identified much potent(10-100 fold) than the gossypol and its known Schiff base derivatives for the anticancer activity.[1]This is the first example for Gossypol Schiff bases with the increased activity.[2]The investigation of the Schiff base side chain of gossypol revealed the unique anticancer effect was achieved by the introduced hydrophobic ester *** molecular modeling analysis demonstrated the possible binding mode of these compounds with the Bcl-2,which could explain the good binding affinity of these novel gossypol Schiff bases with the proteins.
Chromones,which universally exist in nature,exhibit various pharmacological activities,such as antitumor,anti-inflammatory,antioxidant,cardioprotective,anti-HIV and antimicrobial *** were also favored due to low mamma...
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Chromones,which universally exist in nature,exhibit various pharmacological activities,such as antitumor,anti-inflammatory,antioxidant,cardioprotective,anti-HIV and antimicrobial *** were also favored due to low mammalian toxicity,which attracted many researchers' interest for structural modification of *** oxide has great potential in inhibiting carcinogenesis and tumor ***,due to its instability and short half-life,it is not really *** predicament inspired us to design and synthesize a series of chromones derivatives bearing nitric oxide *** biological activities of this series of compounds are under evaluation.
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