Search Results - "Weller, Caroline"
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Biodegradable poly(amine-co-ester) terpolymers for targeted gene delivery
Published in Nature materials (01-01-2012)“…Many synthetic polycationic vectors for non-viral gene delivery show high efficiency in vitro , but their usually excessive charge density makes them toxic for…”
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Facile Semisynthesis of Ubiquitylated Peptides with the Ligation Auxiliary 2-Aminooxyethanethiol
Published in Methods in molecular biology (Clifton, N.J.) (2020)“…The posttranslational modification of cellular proteins by ubiquitin (Ub), called ubiquitylation, is indispensable for the normal growth and development of…”
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Facile Synthesis of Native and Protease-Resistant Ubiquitylated Peptides
Published in Chembiochem : a European journal of chemical biology (16-06-2014)“…The reversible post‐translational modification of eukaryotic proteins by ubiquitin regulates key cellular processes including protein degradation and gene…”
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Allosteric Activation of Ubiquitin-Specific Proteases by β-Propeller Proteins UAF1 and WDR20
Published in Molecular cell (21-07-2016)“…Ubiquitin-specific proteases (USPs) constitute the largest family of deubiquitinating enzymes, whose catalytic competency is often modulated by their binding…”
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Polymer nanoparticles encapsulating siRNA for treatment of HSV-2 genital infection
Published in Journal of controlled release (20-08-2012)“…Effective, low-cost, and safe treatments for sexually transmitted viral infections are urgently needed. Here, we show for the first time that intravaginal…”
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Chemically Sumoylated Histone H4 Stimulates Intranucleosomal Demethylation by the LSD1–CoREST Complex
Published in ACS chemical biology (15-09-2017)“…Lysine-specific demethylase 1 (LSD1) downregulates eukaryotic gene activity by demethylating mono- and dimethylated Lys4 in histone H3. Elucidating the…”
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A Facile N-Mercaptoethoxyglycinamide (MEGA) Linker Approach to Peptide Thioesterification and Cyclization
Published in Journal of the American Chemical Society (22-03-2017)“…The C-terminal electrophilic activation of peptides by α-thioesterification requires strongly acidic conditions or complex chemical manipulations, which…”
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Aromatic thiol-mediated cleavage of N–O bonds enables chemical ubiquitylation of folded proteins
Published in Nature communications (29-09-2016)“…Access to protein substrates homogenously modified by ubiquitin (Ub) is critical for biophysical and biochemical investigations aimed at deconvoluting the…”
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Chemical strategies to understand the language of ubiquitin signaling
Published in Biopolymers (01-02-2014)“…ABSTRACT Ubiquitin (Ub) is a small 76 amino acid long protein that is highly conserved in all eukaryotes studied to date. In humans, more than 600 ligases are…”
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Selenocysteine as a Latent Bioorthogonal Electrophilic Probe for Deubiquitylating Enzymes
Published in Journal of the American Chemical Society (26-10-2016)“…Deubiquitylating enzymes (DUBs) remove ubiquitin (Ub) from various cellular proteins and render eukaryotic ubiquitylation a dynamic process. The misregulation…”
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All about that Amide Bond: The Sixth Chemical Protein Synthesis (CPS) Meeting
Published in ChemBioChem (23-11-2015)“…Endless potential: The sixth Chemical Protein Synthesis Meeting, held recently in St. Augustine, Florida, showed the potential of peptide and protein chemistry…”
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Sumoylation of the human histone H4 tail inhibits p300-mediated transcription by RNA polymerase II in cellular extracts
Published in eLife (08-11-2021)“…The post-translational modification of histones by the small ubiquitin-like modifier (SUMO) protein has been associated with gene regulation, centromeric…”
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Prevention of K-Ras- and Pten-mediated intravaginal tumors by treatment with camptothecin-loaded PLGA nanoparticles
Published in Drug delivery and translational research (01-10-2011)“…Primary squamous cell carcinoma of the vagina is an uncommon disease that often exhibits few symptoms before reaching an advanced stage. Topical intravaginal…”
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All About That Amide Bond: The 6th Chemical Protein Synthesis (CPS) Meeting
Published in Chembiochem : a European journal of chemical biology (12-10-2015)Get full text
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Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS
Published in Science (American Association for the Advancement of Science) (18-08-2023)“…The discovery of small-molecule inhibitors requires suitable binding pockets on protein surfaces. Proteins that lack this feature are considered undruggable…”
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Surface modified poly(β amino ester)-containing nanoparticles for plasmid DNA delivery
Published in Journal of controlled release (28-11-2012)“…The use of biodegradable polymers provides a potentially safe and effective alternative to viral and liposomal vectors for the delivery of plasmid DNA to cells…”
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Abstract PR10: Tri-complex inhibitors of the oncogenic, GTP-bound form of KRASG12C overcome RTK-mediated escape mechanisms and drive tumor regressions in vivo
Published in Molecular cancer therapeutics (01-12-2019)“…RAS proteins are small GTPases that drive cell proliferation and survival when bound to GTP. Mutant RAS proteins are found in approximately one-third of human…”
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Abstract B080: Mutant-selective KRASG12D(ON) inhibitor suppresses proliferation in vitro and tumor growth in vivo of KrasG12D GEMM-derived PDAC organoids
Published in Cancer research (Chicago, Ill.) (16-01-2024)“…KRAS is the most frequently mutated oncogene in pancreatic ductal adenocarcinoma (PDAC), with KRASG12D driving initiation and progression of ~40% of tumors…”
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Rapid Semisynthesis of Acetylated and Sumoylated Histone Analogs
Published in Methods in enzymology (2016)“…The density and diversity of posttranslational modifications (PTMs) observed in histone proteins typically limit their purification to homogeneity from…”
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Abstract ND03: Discovery of RMC-9805, an oral, covalent tri-complex KRASG12D(ON) inhibitor
Published in Cancer research (Chicago, Ill.) (05-04-2024)“…RASG12D mutant cancers represent a significant unmet medical need with 55,000 new diagnoses annually in the US. The RASG12D mutation increases the abundance of…”
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