Search Results - "Ficarro, Scott B"
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Substrate processing by the Cdc48 ATPase complex is initiated by ubiquitin unfolding
Published in Science (American Association for the Advancement of Science) (02-08-2019)“…The Cdc48 adenosine triphosphatase (ATPase) (p97 or valosin-containing protein in mammals) and its cofactor Ufd1/Npl4 extract polyubiquitinated proteins from…”
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2
Architecture of autoinhibited and active BRAF–MEK1–14-3-3 complexes
Published in Nature (London) (01-11-2019)“…RAF family kinases are RAS-activated switches that initiate signalling through the MAP kinase cascade to control cellular proliferation, differentiation and…”
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3
Metabolic Signatures Uncover Distinct Targets in Molecular Subsets of Diffuse Large B Cell Lymphoma
Published in Cancer cell (16-10-2012)“…Molecular signatures have identified several subsets of diffuse large B cell lymphoma (DLBCL) and rational targets within the B cell receptor (BCR) signaling…”
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4
LIN28 Regulates Stem Cell Metabolism and Conversion to Primed Pluripotency
Published in Cell stem cell (07-07-2016)“…The RNA-binding proteins LIN28A and LIN28B play critical roles in embryonic development, tumorigenesis, and pluripotency, but their exact functions are poorly…”
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Direct Analysis of Phosphorylation Sites on the Rpb1 C-Terminal Domain of RNA Polymerase II
Published in Molecular cell (21-01-2016)“…Dynamic interactions between RNA polymerase II and various mRNA-processing and chromatin-modifying enzymes are mediated by the changing phosphorylation pattern…”
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6
Translocation of polyubiquitinated protein substrates by the hexameric Cdc48 ATPase
Published in Molecular cell (03-02-2022)“…The hexameric Cdc48 ATPase (p97 or VCP in mammals) cooperates with its cofactor Ufd1/Npl4 to extract polyubiquitinated proteins from membranes or…”
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In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C
Published in Proceedings of the National Academy of Sciences - PNAS (17-06-2014)“…Directly targeting oncogenic V-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog (K-Ras) with small-molecule inhibitors has historically been considered…”
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8
Akt Kinase Activation Mechanisms Revealed Using Protein Semisynthesis
Published in Cell (09-08-2018)“…Akt is a critical protein kinase that drives cancer proliferation, modulates metabolism, and is activated by C-terminal phosphorylation. The current structural…”
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9
Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype
Published in Cell chemical biology (20-06-2019)“…Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and transcription, but its precise role remains elusive. We previously described THZ1, a CDK7…”
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10
BRCA1 binds TERRA RNA and suppresses R-Loop-based telomeric DNA damage
Published in Nature communications (10-06-2021)“…R-loop structures act as modulators of physiological processes such as transcription termination, gene regulation, and DNA repair. However, they can cause…”
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Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor
Published in Angewandte Chemie International Edition (03-01-2014)“…We report the synthesis of a GDP analogue, SML‐8‐73‐1, and a prodrug derivative, SML‐10‐70‐1, which are selective, direct‐acting covalent inhibitors of the…”
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12
Downstream promoter interactions of TFIID TAFs facilitate transcription reinitiation
Published in Genes & development (01-11-2017)“…TFIID binds promoter DNA to recruit RNA polymerase II and other basal factors for transcription. Although the TATA-binding protein (TBP) subunit of TFIID is…”
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In vitro analysis of RNA polymerase II elongation complex dynamics
Published in Genes & development (01-05-2019)“…RNA polymerase II elongation complexes (ECs) were assembled from nuclear extract on immobilized DNA templates and analyzed by quantitative mass spectrometry…”
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14
Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C
Published in Cell chemical biology (17-08-2017)“…Targeted covalent small molecules have shown promise for cancers driven by KRAS G12C. Allosteric compounds that access an inducible pocket formed by movement…”
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15
Intrinsic Selectivity of Notch 1 for Delta-like 4 Over Delta-like 1
Published in The Journal of biological chemistry (30-08-2013)“…Notch signaling makes critical contributions to cell fate determination in all metazoan organisms, yet remarkably little is known about the binding affinity of…”
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16
Accelerating inhibitor discovery for deubiquitinating enzymes
Published in Nature communications (08-02-2023)“…Deubiquitinating enzymes (DUBs) are an emerging drug target class of ~100 proteases that cleave ubiquitin from protein substrates to regulate many cellular…”
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Structure and Ubiquitination-Dependent Activation of TANK-Binding Kinase 1
Published in Cell reports (Cambridge) (01-03-2013)“…Upon stimulation by pathogen-associated inflammatory signals, TANK-binding kinase 1 (TBK1) induces type I interferon expression and modulates nuclear factor κB…”
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Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors
Published in Cell chemical biology (15-02-2018)“…Irreversible inhibition of transcriptional cyclin-dependent kinases (CDKs) provides a therapeutic strategy for cancers that rely on aberrant transcription;…”
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PARP1-driven poly-ADP-ribosylation regulates BRCA1 function in homologous recombination-mediated DNA repair
Published in Cancer discovery (01-12-2014)“…BRCA1 promotes homologous recombination-mediated DNA repair (HRR). However, HRR must be tightly regulated to prevent illegitimate recombination. We previously…”
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Sub1 and RPA Associate with RNA Polymerase II at Different Stages of Transcription
Published in Molecular cell (04-11-2011)“…Single-stranded DNA-binding proteins play many roles in nucleic acid metabolism, but their importance during transcription remains unclear. Quantitative…”
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