Search Results - "Laufer, A."
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Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology
Published in Journal of medicinal chemistry (27-06-2019)“…Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by means of reactive groups, the so-called warheads. Currently, targeting…”
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Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors
Published in Drug resistance updates (01-05-2015)“…Abstract Multiple mutations in the EGFR gene are a major cause for the failure of Erlotinib and Gefitinib in the treatment of patients harboring non-small-cell…”
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Inhibitors of c‑Jun N‑Terminal Kinases: An Update
Published in Journal of medicinal chemistry (08-01-2015)“…The c-Jun N-terminal kinases (JNKs) are serine/threonine kinases implicated in the pathogenesis of various diseases. Recent advances in the development of…”
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Decisive role of water and protein dynamics in residence time of p38α MAP kinase inhibitors
Published in Nature communications (28-01-2022)“…Target residence time plays a crucial role in the pharmacological activity of small molecule inhibitors. Little is known, however, about the underlying causes…”
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Quantifying inter-individual anatomical variability in the subcortex using 7T structural MRI
Published in NeuroImage (Orlando, Fla.) (01-07-2014)“…Functional magnetic resonance imaging (MRI) data are usually registered into standard anatomical space. However, standard atlases, such as LPBA40, the…”
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6
Cryptic sub-ice geology revealed by a U-Pb zircon study of glacial till in Dronning Maud Land, East Antarctica
Published in Precambrian research (01-06-2017)“…•U-Pb zircon data of glacial drift reveal nature of East Antarcticás cryptic interior.•Evidence of significant extension of the TOAST southward.•TOAST has a…”
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Post-Campylobacter Guillain Barré Syndrome in the USA: secondary analysis of surveillance data collected during the 2009–2010 novel Influenza A (H1N1) vaccination campaign
Published in Epidemiology and infection (01-10-2018)“…Guillain Barré syndrome (GBS), which is triggered by autoantibodies produced in response to antigenic stimuli such as certain infections and vaccinations, is…”
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Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket
Published in Cell chemical biology (17-11-2016)“…Janus kinases (JAKs) are a family of cytoplasmatic tyrosine kinases that are attractive targets for the development of anti-inflammatory drugs given their…”
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Quantifying inter-individual anatomical variability in the subcortex using 7 T structural MRI
Published in NeuroImage (Orlando, Fla.) (01-07-2014)“…Functional magnetic resonance imaging (MRI) data are usually registered into standard anatomical space. However, standard atlases, such as LPBA40, the…”
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10
p38 MAPK inhibitors: a patent review (2012 - 2013)
Published in Expert opinion on therapeutic patents (01-05-2014)“…The p38 MAPK is a ubiquitous target in the research-based pharmaceutical industry. It plays a decisive role in the regulation of the production of…”
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Discovery of Polyphenolic Natural Products as SARS-CoV-2 Mpro Inhibitors for COVID-19
Published in Pharmaceuticals (Basel, Switzerland) (28-01-2023)“…The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has forced the development of direct-acting antiviral drugs due to the coronavirus disease…”
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Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding
Published in Proceedings of the National Academy of Sciences - PNAS (12-02-2013)“…The activity of protein kinase B (Akt)—a major kinase promoting cell proliferation and survival—oscillates during the cell cycle. To investigate whether…”
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13
The band alignment of Cu2O/ZnO and Cu2O/GaN heterostructures
Published in Applied physics letters (27-02-2012)“…Using photoelectron spectroscopy, we investigate the band alignments of the Cu2O/ZnO heterointerface and compare the findings with the corresponding values for…”
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The molecular interaction pattern of lenvatinib enables inhibition of wild-type or kinase-mutated FGFR2-driven cholangiocarcinoma
Published in Nature communications (12-02-2024)“…Fibroblast growth factor receptor (FGFR)−2 can be inhibited by FGFR-selective or non-selective tyrosine kinase inhibitors (TKIs). Selective TKIs are approved…”
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Stimulating Effect of Sclareol on Suicidal Death of Human Erythrocytes
Published in Cellular physiology and biochemistry (01-01-2016)“…Background/Aims: The diterpene alcohol Sclareol has been proposed for the treatment of malignancy. In analogy to apoptosis of nucleated cells, erythrocytes may…”
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Anticancer Drug Conjugates Incorporating Estrogen Receptor Ligands
Published in Pharmaceutics (26-12-2022)“…Hormone-dependent cancers, such as certain types of breast cancer are characterized by over-expression of estrogen receptors (ERs). Anticancer drug conjugates…”
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Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor
Published in Nature chemical biology (25-12-2011)“…Studies elucidating the role of p38α MAPK in diverse biological processes are limited by the lack of a specific inhibitor. Skepinone-L is a highly selective…”
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Outbreaks of Salmonella infections attributed to beef – United States, 1973–2011
Published in Epidemiology and infection (01-07-2015)“…Non-typhoidal Salmonella is estimated to be the most common bacterial cause of foodborne illness in the United States, causing an estimated one million…”
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Design, Synthesis and Biological Evaluation of 7-Chloro-9H-pyrimido[4,5-b]indole-based Glycogen Synthase Kinase-3β Inhibitors
Published in Molecules (Basel, Switzerland) (25-06-2019)“…Glycogen synthase kinase-3β (GSK-3β) represents a relevant drug target for the treatment of neurodegenerative pathologies including Alzheimer’s disease. We…”
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HLA-C Peptide Repertoires as Predictors of Clinical Response during Early SARS-CoV-2 Infection
Published in Life (Basel, Switzerland) (01-09-2024)“…The human leukocyte antigen (HLA) system plays a pivotal role in the immune response to viral infections, mediating the presentation of viral peptides to T…”
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