Search Results - "Cochran, Andrea G"
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A Subset of Human Bromodomains Recognizes Butyryllysine and Crotonyllysine Histone Peptide Modifications
Published in Structure (London) (06-10-2015)“…Bromodomains are epigenetic readers that are recruited to acetyllysine residues in histone tails. Recent studies have identified non-acetyl acyllysine…”
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BMI1–RING1B is an autoinhibited RING E3 ubiquitin ligase
Published in Nature communications (07-07-2015)“…Polycomb repressive complex 1 (PRC1) is required for ubiquitination of histone H2A lysine 119, an epigenetic mark associated with repression of genes important…”
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3
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
Published in Nature chemical biology (01-07-2016)“…KDM5 histone demethylases promote the survival of drug-tolerant persister (DTP) cells in certain cancers. CPI-455, a chemical probe specific for KDM5, elevates…”
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4
Wnt Antagonists Bind through a Short Peptide to the First β-Propeller Domain of LRP5/6
Published in Structure (London) (12-10-2011)“…The Wnt pathway inhibitors DKK1 and sclerostin (SOST) are important therapeutic targets in diseases involving bone loss or damage. It has been appreciated that…”
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Reconstitution of a Frizzled8·Wnt3a·LRP6 Signaling Complex Reveals Multiple Wnt and Dkk1 Binding Sites on LRP6
Published in The Journal of biological chemistry (19-03-2010)“…Wnt/β-catenin signaling is initiated at the cell surface by association of secreted Wnt with its receptors Frizzled (Fz) and low density lipoprotein…”
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Recognition of UbcH5c and the nucleosome by the Bmi1/Ring1b ubiquitin ligase complex
Published in The EMBO journal (17-08-2011)“…The Polycomb repressive complex 1 (PRC1) mediates gene silencing, in part by monoubiquitination of histone H2A on lysine 119 (uH2A). Bmi1 and Ring1b are…”
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300
Published in Journal of medicinal chemistry (08-12-2016)“…The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation…”
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Non-canonical reader modules of BAZ1A promote recovery from DNA damage
Published in Nature communications (11-10-2017)“…Members of the ISWI family of chromatin remodelers mobilize nucleosomes to control DNA accessibility and, in some cases, are required for recovery from DNA…”
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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance
Published in Bioorganic & medicinal chemistry letters (01-08-2017)“…[Display omitted] Bromodomain-containing protein 9 (BRD9), an epigenetic “reader” of acetylated lysines on post-translationally modified histone proteins, is…”
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Tryptophan Zippers: Stable, Monomeric β-Hairpins
Published in Proceedings of the National Academy of Sciences - PNAS (08-05-2001)“…A structural motif, the tryptophan zipper (trpzip), greatly stabilizes the β-hairpin conformation in short peptides. Peptides (12 or 16 aa in length) with four…”
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Bromodomains: a new target class for drug development
Published in Nature reviews. Drug discovery (01-08-2019)“…Less than a decade ago, it was shown that bromodomains, acetyl lysine ‘reader’ modules found in proteins with varied functions, were highly tractable…”
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GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1
Published in Journal of medicinal chemistry (28-09-2023)“…Bromodomains are acetyl-lysine binding modules that are found in different classes of chromatin-interacting proteins. Among these are large chromatin…”
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The Mitotic Regulator Survivin Binds as a Monomer to Its Functional Interactor Borealin
Published in The Journal of biological chemistry (30-11-2007)“…Survivin is a member of the IAP (inhibitor of apoptosis) protein family, defined in part by the presence of a zinc-binding baculoviral inhibitory repeat (BIR)…”
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14
Short Constrained Peptides That Inhibit HIV-1 Entry
Published in Proceedings of the National Academy of Sciences - PNAS (12-11-2002)“…Peptides corresponding to the C-terminal heptad repeat of HIV-1 gp41 (C-peptides) are potent inhibitors of HIV-1 entry into cells. Their mechanism of…”
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15
Expansion of the ISWI chromatin remodeler family with new active complexes
Published in EMBO reports (01-10-2017)“…ISWI chromatin remodelers mobilize nucleosomes to control DNA accessibility. Complexes isolated to date pair one of six regulatory subunits with one of two…”
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16
Reconstitution of a frizzled8.Wnt3a.LRP6 signaling complex reveals multiple Wnt and Dkk1 binding sites on LRP6
Published in The Journal of biological chemistry (19-03-2010)“…Wnt/beta-catenin signaling is initiated at the cell surface by association of secreted Wnt with its receptors Frizzled (Fz) and low density lipoprotein…”
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Deubiquitinase DUBA is a post-translational brake on interleukin-17 production in T cells
Published in Nature (London) (19-02-2015)“…The deubiquitinase enzyme DUBA is shown to act as a negative regulator of interleukin-17A (IL-17A) in T H 17 cells; DUBA interacts with and stabilizes the…”
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18
Trifluoroacetyl Lysine as a Bromodomain Binding Mimic of Lysine Acetylation
Published in ACS chemical biology (20-05-2022)“…Genetic code expansion has proven invaluable to the elucidation of functions of defined protein modifications through the site-specific incorporation of…”
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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains
Published in Journal of medicinal chemistry (09-06-2016)“…The biological role played by non-BET bromodomains remains poorly understood, and it is therefore imperative to identify potent and highly selective inhibitors…”
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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1
Published in Journal of medicinal chemistry (25-08-2022)“…Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with…”
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