Search Results - "Xiao, Xiangshu"
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Toward Developing Chemical Modulators of Hsp60 as Potential Therapeutics
Published in Frontiers in molecular biosciences (20-04-2018)“…The 60 kDa heat shock protein (Hsp60) is classically known as a mitochondrial chaperonin protein working together with co-chaperonin 10 kDa heat shock protein…”
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Systemic Inhibition of CREB is Well-tolerated in vivo
Published in Scientific reports (03-10-2016)“…cAMP-response element binding protein (CREB) is a nuclear transcription factor activated by multiple extracellular signals including growth factors and…”
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3
Design, synthesis and biological evaluation of regioisomers of 666-15 as inhibitors of CREB-mediated gene transcription
Published in Bioorganic & medicinal chemistry letters (15-02-2017)“…[Display omitted] cAMP-response element binding protein (CREB) is a nuclear transcription factor that has been implicated in the pathogenesis and maintenance…”
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4
Discovery of a Small-Molecule Inhibitor of the KIX-KID Interaction
Published in Chembiochem : a European journal of chemical biology (23-11-2009)“…Are you too small? The small molecule (MW=297) shown here was discovered to be an inhibitor of the KIX–KID interaction by using a novel Renilla luciferase…”
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5
Design, synthesis and evaluation of antitumor acylated monoaminopyrroloquinazolines
Published in Bioorganic & medicinal chemistry letters (15-07-2017)“…[Display omitted] Pyrroloquinazoline is a privileged chemical scaffold with diverse biological activities. We recently described a series of N-3 acylated…”
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6
CG-SLENP: A Chemical Genetics Strategy To Selectively Label Existing Proteins and Newly Synthesized Proteins
Published in JACS Au (26-08-2024)“…Protein synthesis and subsequent delivery to the target locations in cells are essential for their proper functions. Methods to label and distinguish newly…”
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Phosphorylation of Lamin A/C at serine 22 modulates Nav1.5 function
Published in Physiological reports (01-11-2021)“…Variants in the LMNA gene, which encodes for Lamin A/C, are associated with cardiac conduction disease (CCD). We previously reported that Lamin A/C variants…”
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A clickable photoaffinity probe of betulinic acid identifies tropomyosin as a target
Published in Acta pharmaceutica Sinica. B (01-05-2022)“…Target identification of bioactive compounds is important for understanding their mechanisms of action and provides critical insights into their therapeutic…”
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Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription
Published in Bioorganic & medicinal chemistry letters (01-10-2013)“…2-[(7-Nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide was identified as a potent inhibitor of KIX–KID interaction from screening the NCI diversity…”
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10
An Ab Initio Quantum Mechanics Calculation that Correlates with Ligand Orientation and DNA Cleavage Site Selectivity in Camptothecin−DNA−Topoisomerase I Ternary Cleavage Complexes
Published in Journal of the American Chemical Society (20-07-2005)“…Camptothecin (CPT), a cytotoxic natural alkaloid isolated from Camptotheca acuminata, and its derivatives represent an important class of cancer…”
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Design, Synthesis, and Biological Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Featuring Polyamine Side Chains on the Lactam Nitrogen
Published in Journal of medicinal chemistry (18-12-2003)“…The indenoisoquinolines are a class of noncamptothecin topoisomerase I inhibitors that display significant cytotoxicity in human cancer cell cultures. They…”
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A Lamin-Binding Ligand Inhibits Homologous Recombination Repair of DNA Double-Strand Breaks
Published in ACS central science (26-09-2018)“…Nuclear lamins are type V intermediate filament proteins. Lamins, including LA, LB1, LB2, and LC, are the major protein components forming the nuclear lamina…”
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13
Total Synthesis and Biological Evaluation of 22-Hydroxyacuminatine
Published in Journal of medicinal chemistry (23-02-2006)“…A total synthesis of 22-hydroxyacuminatine, a cytotoxic alkaloid isolated from Camptotheca acuminata, is reported. The key step in the synthesis involves the…”
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On the Binding of Indeno[1,2-c]isoquinolines in the DNA−Topoisomerase I Cleavage Complex
Published in Journal of medicinal chemistry (05-05-2005)“…An ab initio quantum mechanics calculation is reported which predicts the orientation of indenoisoquinoline 4 in the ternary cleavage complex formed from DNA…”
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15
Design, Synthesis, and Biological Evaluation of Cytotoxic 11-Alkenylindenoisoquinoline Topoisomerase I Inhibitors and Indenoisoquinoline−Camptothecin Hybrids
Published in Journal of medicinal chemistry (17-07-2003)“…The indenoisoquinolines are a novel class of topoisomerase I (top1) inhibitors that are cytotoxic in cancer cell cultures and are therefore under development…”
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Novel Type of Prodrug Activation through a Long-Range O,N‑Acyl Transfer: A Case of Water-Soluble CREB Inhibitor
Published in ACS medicinal chemistry letters (09-10-2014)“…CREB (cAMP response element binding protein) has been shown to play an important role in tumor initiation, progression, and metastasis. We discovered that…”
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Effect of E-Ring Modifications in Camptothecin on Topoisomerase I Inhibition: A Quantum Mechanics Treatment
Published in Journal of organic chemistry (11-11-2005)“…Camptothecins (CPTs) are the prototypical class of topoisomerase I (Top1) inhibitors with significant anticancer activities. Structure−activity relationship…”
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18
Rapid identification of improved protein ligands using peptoid microarrays
Published in Bioorganic & medicinal chemistry letters (15-07-2009)“…A rapid array-based protocol is presented by which a modest affinity protein-binding small molecule can be appended to a library of peptoids via click…”
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A general system for evaluating the efficiency of chromophore-assisted light inactivation (CALI) of proteins reveals Ru(II) tris-bipyridyl as an unusually efficient "warhead"
Published in Molecular bioSystems (01-01-2008)“…Chromophore-assisted light inactivation (CALI) of proteins is a potentially powerful tool in biological research for the triggered disruption of protein…”
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Design, synthesis, and biological evaluation of cytotoxic 11-aminoalkenylindenoisoquinoline and 11-diaminoalkenylindenoisoquinoline topoisomerase I inhibitors
Published in Bioorganic & medicinal chemistry (01-10-2004)“…[Display omitted] The cytotoxic indenoisoquinolines are a novel class of noncamptothecin topoisomerase I inhibitors having certain features that compare…”
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