Search Results - "Tandeske, Laura"
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Defining the substrate envelope of SARS-CoV-2 main protease to predict and avoid drug resistance
Published in Nature communications (21-06-2022)“…Coronaviruses can evolve and spread rapidly to cause severe disease morbidity and mortality, as exemplified by SARS-CoV-2 variants of the COVID-19 pandemic…”
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RAF Inhibitors Activate the MAPK Pathway by Relieving Inhibitory Autophosphorylation
Published in Cancer cell (13-05-2013)“…ATP competitive inhibitors of the BRAFV600E oncogene paradoxically activate downstream signaling in cells bearing wild-type BRAF (BRAFWT). In this study, we…”
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Structural and biophysical comparisons of the pomalidomide- and CC-220-induced interactions of SALL4 with cereblon
Published in Scientific reports (12-12-2023)“…The design of cereblon-binding molecular glues (MGs) that selectively recruit a desired protein while excluding teratogenic SALL4 is an area of significant…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Inhibition of prenylated KRAS in a lipid environment
Published in PloS one (06-04-2017)“…RAS mutations lead to a constitutively active oncogenic protein that signals through multiple effector pathways. In this chemical biology study, we describe a…”
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Design of Novel Conformational and Genotype-Specific Antigens for Improving Sensitivity of Immunoassays for Hepatitis C Virus-Specific Antibodies
Published in Journal of Clinical Microbiology (01-08-2005)“…The current commercially licensed enzyme-linked immunosorbent assays (ELISAs) for hepatitis C virus (HCV) mainly use recombinant proteins containing linear…”
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Identification of Potent, Broad-Spectrum Coronavirus Main Protease Inhibitors for Pandemic Preparedness
Published in Journal of medicinal chemistry (10-10-2024)“…The COVID-19 pandemic highlights the ongoing risk of zoonotic transmission of coronaviruses to global health. To prepare for future pandemics, it is essential…”
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A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes
Published in Cell chemical biology (20-01-2022)“…While there are hundreds of predicted E3 ligases, characterizing their applications for targeted protein degradation has proved challenging. Here, we report a…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Discovery of Potent Pyrazoline‐Based Covalent SARS‐CoV‐2 Main Protease Inhibitors
Published in Chembiochem : a European journal of chemical biology (01-06-2023)“…While vaccines and antivirals are now being deployed for the current SARS‐CoV‐2 pandemic, we require additional antiviral therapeutics to not only effectively…”
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Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2017)“…A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs were designed as inhibitors of B-RAFV600E. Medicinal chemistry techniques were employed to explore the…”
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Abstract LB-28: RAF inhibitors activate MAPK pathway through relief of RAF auto-inhibition
Published in Cancer research (Chicago, Ill.) (15-04-2011)“…Abstract Mutations in the RAS/RAF/MEK/ERK pathway are among the most common in human cancers, and RAF small molecule kinase inhibitors are now being tested for…”
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Abstract B38: Inhibiting mutated KRAS, a broken switch of effector pathways
Published in Molecular cancer research (01-12-2014)“…Abstract Mutated forms of KRAS are no longer able to switch effectors between “on” and “off” states. It is known that the function of KRAS is controlled by key…”
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Hepatitis C virus polyprotein vaccine formulations capable of inducing broad antibody and cellular immune responses
Published in Journal of general virology (01-08-2006)“…1 Chiron Vaccines, 4560 Horton Street, Emeryville, CA 94608, USA 2 Chiron Vaccines, Via Fiorentina 1, 53100 Siena, Italy Correspondence Michael Houghton…”
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