Search Results - "Buhrlage, Sara J"
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1
Akkermansia muciniphila phospholipid induces homeostatic immune responses
Published in Nature (London) (04-08-2022)“…Multiple studies have established associations between human gut bacteria and host physiology, but determining the molecular mechanisms underlying these…”
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2
Screening of DUB activity and specificity by MALDI-TOF mass spectrometry
Published in Nature communications (27-08-2014)“…Deubiquitylases (DUBs) are key regulators of the ubiquitin system which cleave ubiquitin moieties from proteins and polyubiquitin chains. Several DUBs have…”
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3
A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia
Published in Blood (15-08-2013)“…Myeloid differentiation factor 88 (MYD88) L265P somatic mutation is highly prevalent in Waldenström macroglobulinemia (WM) and supports malignant growth…”
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4
Inhibition of USP10 induces degradation of oncogenic FLT3
Published in Nature chemical biology (01-12-2017)“…An inhibitor of the deubiquitinase (DUB) USP10 regulates the degradation of oncogenic FLT3, thus defining USP10 as a DUB for FLT3 and providing a therapeutic…”
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5
Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells
Published in Molecular cancer therapeutics (01-12-2013)“…Inhibitor of DNA binding 1 (ID1) transcription factor is essential for the proliferation and progression of many cancer types, including leukemia. However, the…”
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6
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib
Published in Blood (23-06-2016)“…Activating mutations in MYD88 are present in ∼95% of patients with Waldenström macroglobulinemia (WM), as well as other B-cell malignancies including activated…”
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7
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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8
Integrating multi-omics data reveals function and therapeutic potential of deubiquitinating enzymes
Published in eLife (23-06-2022)“…Deubiquitinating enzymes (DUBs), ~100 of which are found in human cells, are proteases that remove ubiquitin conjugates from proteins, thereby regulating…”
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9
Strategies for Competitive Activity‐Based Protein Profiling in Small Molecule Inhibitor Discovery and Characterization
Published in Israel journal of chemistry (01-03-2023)“…Since its introduction by Cravatt and colleagues in 1999, activity‐based protein profiling (ABPP) has become widely utilized throughout academia, government,…”
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10
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases
Published in Biochemical journal (01-01-2014)“…The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1)…”
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11
Copy-number and gene dependency analysis reveals partial copy loss of wild-type SF3B1 as a novel cancer vulnerability
Published in eLife (08-02-2017)“…Genomic instability is a hallmark of human cancer, and results in widespread somatic copy number alterations. We used a genome-scale shRNA viability screen in…”
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12
Identification of deubiquitinase inhibitors via high-throughput screening using a fluorogenic ubiquitin-rhodamine assay
Published in STAR protocols (17-12-2021)“…Identification of selective deubiquitinase (DUB) inhibitors is critical for probe development to further understand and explore DUB biological function. Here,…”
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13
Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma
Published in Blood (14-07-2016)“…Diffuse large B-cell lymphoma (DLBCL) is the most common subtype of non-Hodgkin lymphoma, yet 40% to 50% of patients will eventually succumb to their disease,…”
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14
Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors
Published in Journal of medicinal chemistry (26-03-2020)“…Deubiquitinating enzymes, or DUBs, comprise a family of proteases that regulate ubiquitination dynamics. Since their discovery, genetic and functional studies…”
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15
Repurposing of Kinase Inhibitors for Treatment of COVID-19
Published in Pharmaceutical research (01-09-2020)“…The outbreak of COVID-19, the pandemic disease caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has spurred an intense search for…”
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16
Proteomic approaches to study ubiquitinomics
Published in Biochimica et biophysica acta. Gene regulatory mechanisms (01-06-2023)“…As originally described some 40 years ago, protein ubiquitination was thought to serve primarily as a static mark for protein degradation. In the ensuing…”
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17
Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development
Published in Cell (10-12-2020)“…Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-dependent degradation of proteins. TPD is of interest in drug…”
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18
Amphipathic Small Molecules Mimic the Binding Mode and Function of Endogenous Transcription Factors
Published in ACS chemical biology (15-05-2009)“…Small molecules that reconstitute the binding mode(s) of a protein and in doing so elicit a programmed functional response offer considerable advantages in the…”
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19
Crystal structure of human IRAK1
Published in Proceedings of the National Academy of Sciences - PNAS (19-12-2017)“…Interleukin 1 (IL-1) receptor-associated kinases (IRAKs) are serine/threonine kinases that play critical roles in initiating innate immune responses against…”
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DUB to the rescue
Published in Molecular cell (21-04-2022)“…Henning et al. (2022) report development of a novel class of agents, bivalent deubiquitinase (DUB)-targeting chimeras (DUBTACs), that can selectively stabilize…”
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