Lista de obras - Daniel Rauh - Dominio Público Uruguay

A Chemical Genetic Approach for Covalent Inhibition of Analogue-Sensitive Aurora Kinase

artículo científico publicado en 2012

A New Approach for Probing the Mobility and Lifetime of Photogenerated Charge Carriers in Organic Solar Cells Under Real Operating Conditions

article

A Scaffold-Tree-Merging Strategy for Prospective Bioactivity Annotation of γ-Pyrones

artículo científico publicado en 2010

A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer

artículo científico publicado en 2015

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant

artículo científico publicado en 2016

A framework for identification of actionable cancer genome dependencies in small cell lung cancer

artículo científico publicado en 2012

A new screening assay for allosteric inhibitors of cSrc

artículo científico publicado en 2009

A special thematic compilation/special issue crossover with Biochemistry, Journal of Medicinal Chemistry, and ACS Medicinal Chemistry Letters focused on kinases

artículo científico publicado en 2014

ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.

artículo científico publicado en 2011

ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds

artículo científico publicado en 2008

An Unusual Intramolecular Halogen Bond guides Conformational Selection.

artículo científico publicado en 2018

An unbiased cell morphology-based screen for new, biologically active small molecules

artículo científico publicado en 2005

Analysis of compound synergy in high-throughput cellular screens by population-based lifetime modeling

artículo científico publicado en 2010

Augmented Reality in Scientific Publications - Taking the Visualization of 3D Structures to the Next Level

artículo científico publicado en 2019

Augmented Reality in Scientific Publications-Taking the Visualization of 3D Structures to the Next Level

scientific article published on 01 March 2018

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA

artículo científico publicado en 2024

BSKs are partially redundant positive regulators of brassinosteroid signaling in Arabidopsis.

artículo científico publicado en 2013

Bioactivity-guided mapping and navigation of chemical space.

artículo científico publicado en 2009

Cell-autonomous and non-cell-autonomous mechanisms of transformation by amplified FGFR1 in lung cancer

artículo científico publicado en 2014

Cellular model system to dissect the isoform-selectivity of Akt inhibitors

artículo científico publicado en 2021

Change or be changed: reflections of the workshop 'Future in Medicinal Chemistry'.

artículo científico publicado en 2012

Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7)

scientific article published on 31 May 2019

Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance

artículo científico publicado en 2010

Chemical and structural biology to direct the repurposing of sulindac.

artículo científico publicado en 2009

Chemical biology--current and next challenges

scientific article published on 01 January 2013

Chemical modulation of transcription factors

artículo científico publicado en 2018

Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation

artículo científico publicado en 2010

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma

artículo científico publicado en 2015

Conformational selection vs. induced fit: insights into the binding mechanisms of p38α MAP Kinase inhibitors

artículo científico publicado en 2020

Correlating structure and ligand affinity in drug discovery: a cautionary tale involving second shell residues

artículo científico publicado en 2014

Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.

artículo científico

Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity

artículo científico publicado en 2019

Covalent-Allosteric Kinase Inhibitors.

artículo científico publicado en 2015

De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

artículo científico publicado en 2013

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

artículo científico publicado en 2017

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors

artículo científico publicado en 2009

Direct binding assay for the detection of type IV allosteric inhibitors of Abl.

artículo científico publicado en 2012

Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.

artículo científico publicado en 2014

Epidermal growth factor receptor (EGFR) signaling and covalent EGFR inhibition in lung cancer

artículo científico publicado en 2012

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations

artículo científico publicado en 2014

Fluorescence labels in kinases: a high-throughput kinase binding assay for the identification of DFG-out binding ligands.

artículo científico publicado en 2012

Fluorophore Labeled Kinase Detects Ligands That Bind within the MAPK Insert of p38α Kinase

artículo científico publicado en 2012

Fluorophore labeling of the glycine-rich loop as a method of identifying inhibitors that bind to active and inactive kinase conformations

artículo científico publicado en 2010

Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer.

artículo científico publicado en 2010

Highly Enantioselective Catalytic Synthesis of Neurite Growth-Promoting Secoyohimbanes

scientific article published on 01 April 2013

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products

artículo científico publicado en 2010

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

artículo científico publicado en 2015

Identification and further development of potent TBK1 inhibitors

artículo científico publicado en 2015

Identification of Ustilago maydis Aurora Kinase As a Novel Antifungal Target ⬇️

artículo científico publicado el 20 de junio de 2011

Identification of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase B.

artículo científico publicado en 2010

Identification of type II and III DDR2 inhibitors.

artículo científico publicado en 2014

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer

artículo científico publicado en 2009

Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S

scientific article published on 04 October 2019

Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.

artículo científico publicado en 2017

Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR

artículo científico publicado en 2016

Insights into the Kinetics of the Resistance Formation of Bacteria against Ciprofloxacin Poly(2-methyl-2-oxazoline) Conjugates

artículo científico publicado en 2018

Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer

artículo científico publicado en 2012

Interactive exploration of chemical space with Scaffold Hunter

artículo científico publicado en 2009

Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer

artículo científico publicado en 2015

Lessons to be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer.

artículo científico publicado en 2017

Linking chemistry and biology for the study of protein function

artículo científico publicado en 2007

Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood

artículo científico publicado en 2013

Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR.

artículo científico publicado en 2016

Monitoring ligand-induced conformational changes for the identification of estrogen receptor agonists and antagonists

scientific article published on 09 February 2015

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer

artículo científico publicado en 2011

Natural-product-derived fragments for fragment-based ligand discovery

artículo científico publicado en 2013

Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4

artículo científico publicado en 2015

New Cyanopeptide‐Derived Low MolecularWeight Thrombin Inhibitors ⬇️

artículo científico publicado el 1 de agosto de 2003

Overcoming EGFR-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

scientific article published in Nature Communications

Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores.

artículo científico publicado en 2013

Persister state-directed transitioning and vulnerability in melanoma

artículo científico publicado en 2022

Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer

artículo científico publicado en 2019

Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions

scientific article published on 18 May 2009

Proteus in the world of proteins: conformational changes in protein kinases.

artículo científico publicado en 2010

RAF kinase inhibitors in cancer treatment: like a bull in a China shop?

artículo científico publicado en 2010

RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics

article

Resistance to avapritinib in PDGFRA-driven GIST is caused by secondary mutations in the PDGFRA kinase domain

scientific article published on 24 September 2020

Selective detection of allosteric phosphatase inhibitors.

artículo científico publicado en 2013

Small-molecule inhibition of APT1 affects Ras localization and signaling

artículo científico publicado en 2010

Strategies for the selective regulation of kinases with allosteric modulators: exploiting exclusive structural features.

artículo científico

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt

artículo científico publicado en 2019

Structural characterization of the RLCK family member BSK8: a pseudokinase with an unprecedented architecture

artículo científico publicado en 2013

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR

artículo científico publicado en 2008

Structure Defines Function: Clinically Relevant Mutations in ErbB Kinases

scientific article published on 28 August 2019

Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.

artículo científico publicado en 2017

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

artículo científico publicado en 2015

Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α.

artículo científico publicado en 2011

Structure-based design, synthesis and crystallization of 2-arylquinazolines as lipid pocket ligands of p38α MAPK.

artículo científico publicado en 2017

Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor

artículo científico publicado en 2010

Synthesis of a cyanopeptide-analogue with trypsin activating properties

scientific article published on 01 April 2000

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach

artículo científico publicado en 2015

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.

artículo científico publicado en 2019

The therapeutic potential of phosphatase inhibitors

scientific article published on 04 May 2009

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.

artículo científico publicado en 2017

Trypsin mutants for structure-based drug design: expression, refolding and crystallisation.

artículo científico publicado en 2002

Tumor VEGF:VEGFR2 autocrine feed-forward loop triggers angiogenesis in lung cancer.

artículo científico publicado en 2013

Tumor VEGF:VEGFR2 autocrine feed-forward loop triggers angiogenesisin lung cancer

artículo científico publicado en 2013

Understanding protein-ligand interactions: the price of protein flexibility

artículo científico publicado en 2004

Using small molecules to target protein phosphatases

scientific article published in 2011

ZZ made EZ: influence of inhibitor configuration on enzyme selectivity.

artículo científico publicado en 2003

Lista de obras de Daniel Rauh

A Chemical Genetic Approach for Covalent Inhibition of Analogue-Sensitive Aurora Kinase

A New Approach for Probing the Mobility and Lifetime of Photogenerated Charge Carriers in Organic Solar Cells Under Real Operating Conditions

A Scaffold-Tree-Merging Strategy for Prospective Bioactivity Annotation of γ-Pyrones

A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant

A framework for identification of actionable cancer genome dependencies in small cell lung cancer

A new screening assay for allosteric inhibitors of cSrc

A special thematic compilation/special issue crossover with Biochemistry, Journal of Medicinal Chemistry, and ACS Medicinal Chemistry Letters focused on kinases

ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.

ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds

An Unusual Intramolecular Halogen Bond guides Conformational Selection.

An unbiased cell morphology-based screen for new, biologically active small molecules

Analysis of compound synergy in high-throughput cellular screens by population-based lifetime modeling

Augmented Reality in Scientific Publications - Taking the Visualization of 3D Structures to the Next Level

Augmented Reality in Scientific Publications-Taking the Visualization of 3D Structures to the Next Level

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA

BSKs are partially redundant positive regulators of brassinosteroid signaling in Arabidopsis.

Bioactivity-guided mapping and navigation of chemical space.

Cell-autonomous and non-cell-autonomous mechanisms of transformation by amplified FGFR1 in lung cancer

Cellular model system to dissect the isoform-selectivity of Akt inhibitors

Change or be changed: reflections of the workshop 'Future in Medicinal Chemistry'.

Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7)

Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance

Chemical and structural biology to direct the repurposing of sulindac.

Chemical biology--current and next challenges

Chemical modulation of transcription factors

Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma

Conformational selection vs. induced fit: insights into the binding mechanisms of p38α MAP Kinase inhibitors

Correlating structure and ligand affinity in drug discovery: a cautionary tale involving second shell residues

Covalent Lipid Pocket Ligands Targeting p38α MAPK Mutants.

Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity

Covalent-Allosteric Kinase Inhibitors.

De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors

Direct binding assay for the detection of type IV allosteric inhibitors of Abl.

Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.

Epidermal growth factor receptor (EGFR) signaling and covalent EGFR inhibition in lung cancer

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations

Fluorescence labels in kinases: a high-throughput kinase binding assay for the identification of DFG-out binding ligands.

Fluorophore Labeled Kinase Detects Ligands That Bind within the MAPK Insert of p38α Kinase

Fluorophore labeling of the glycine-rich loop as a method of identifying inhibitors that bind to active and inactive kinase conformations

Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer.

Highly Enantioselective Catalytic Synthesis of Neurite Growth-Promoting Secoyohimbanes

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

Identification and further development of potent TBK1 inhibitors

Identification of Ustilago maydis Aurora Kinase As a Novel Antifungal Target ⬇️

Identification of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase B.

Identification of type II and III DDR2 inhibitors.

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer

Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S

Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT.

Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR

Insights into the Kinetics of the Resistance Formation of Bacteria against Ciprofloxacin Poly(2-methyl-2-oxazoline) Conjugates

Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer

Interactive exploration of chemical space with Scaffold Hunter

Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer

Lessons to be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer.

Linking chemistry and biology for the study of protein function

Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood

Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR.

Monitoring ligand-induced conformational changes for the identification of estrogen receptor agonists and antagonists

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer

Natural-product-derived fragments for fragment-based ligand discovery

Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4

New Cyanopeptide‐Derived Low MolecularWeight Thrombin Inhibitors ⬇️

Overcoming EGFR-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores.

Persister state-directed transitioning and vulnerability in melanoma

Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib in KRAS-Mutant Pancreatic and Colorectal Cancer

Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions

Proteus in the world of proteins: conformational changes in protein kinases.

RAF kinase inhibitors in cancer treatment: like a bull in a China shop?

RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics

Resistance to avapritinib in PDGFRA-driven GIST is caused by secondary mutations in the PDGFRA kinase domain

Selective detection of allosteric phosphatase inhibitors.

Small-molecule inhibition of APT1 affects Ras localization and signaling