129 articles for S Knapp
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
University of Dundee
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Ludwig-Maximilians-Universit£T M£Nchen
Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis.
University of Athens
Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
University of Clermont Auvergne
Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.
University of Cambridge
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Boehringer Ingelheim Rcv
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Pfizer
Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.
Centre National de la Recherche Scientifique/INSERM/ULP
Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.
University of Oxford
Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.
University of Oxford
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Glaxosmithkline
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Technische Universit£T Braunschweig
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
Ku Leuven
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
Oxford University
Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.
The Institute of Cancer Research
X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
University of Oxford
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
University of Oxford
Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
University of Athens
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Pfizer
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Cnrs
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.
University of Oxford
Crystal structure of human aurora B in complex with INCENP and VX-680.
University of Oxford
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines.
The State University of New Jersey
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
University of Oxford
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Ludwig-Maximilians University of Munich
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
University of Oxford
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Universite£? De Rennes 1
Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.
Oxford University
Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.
Clermont Universit£
Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone.
UniversitäT TüBingen
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Goethe University Frankfurt
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Harvard Medical School
Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
Johann Wolfgang Goethe-University
Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.
Goethe University
Expanding the ligand spaces for E3 ligases for the design of protein degraders.
Goethe-University Frankfurt
Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines.
Universite Clermont Auvergne
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles.
Eberhard Karls University Tubingen
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties.
Ludwig-Maximilians-Universitat (LMU) Munchen
Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.
Goethe University Frankfurt
Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors.
Goethe University Frankfurt
Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
Universidade Estadual de Campinas
Tetrahydropyridine LIMK inhibitors: Structure activity studies and biological characterization.
University of Orleans
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
Max Planck Institute of Molecular Physiology
Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.
University of Orleans
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Perha Pharmaceuticals
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Perha Pharmaceuticals
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
University of North Carolina at Chapel Hill
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ.
The Scripps Research Institute
Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily.
Johann Wolfgang Goethe University
MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core.
Goethe University Frankfurt
Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2.
Johann Wolfgang Goethe-University
Incorporation of an Isohexide Subunit Improves the Drug-like Properties of Bioactive Compounds.
Rutgers The State University of New Jersey
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-
Goethe University Frankfurt
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
University of Clermont Auvergne
Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity.
Eberhard Karls Universit£T
TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.
Csic
Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Eberhard Karls Universit£T T£Bingen
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Goethe University Frankfurt
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
Johann Wolfgang Goethe University
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.
Goethe University Frankfurt Am Main
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
Johann Wolfgang Goethe-University
Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
Goethe-University
Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Johann Wolfgang Goethe University
Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors.
Eberhard Karls University T£Bingen
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Sanford Burnham Prebys Medical Discovery Institute
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
Goethe University
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
Eberhard Karls University T£Bingen
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
Goethe-University Frankfurt
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.
University of Campinas (Unicamp)
Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.
Goethe-University Frankfurt
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface.
Goethe-University Frankfurt
Design and Development of a Chemical Probe for Pseudokinase Ca
Goethe University Frankfurt Am Main
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.
Masaryk University
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
Goethe-University Frankfurt
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
University of North Carolina at Chapel Hill
An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.
University of Oxford
Selective targeting of the αC and DFG-out pocket in p38 MAPK.
Johann Wolfgang Goethe University
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.
Goethe University Frankfurt
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.
University of Oxford
Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.
Goethe University Frankfurt
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Institute
New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis.
University of Clermont Auvergne
LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
University of Oxford
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
University of Oxford
Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.
Cancer Research Uk Cancer Therapeutics Unit
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
University of Oxford
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
University of Oxford
Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
University of Oxford
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity
University of Nottingham
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
Goethe-University Frankfurt
Bioisosteric Replacement of Arylamide-Linked Spine Residues with
Federal University of Rio De Janeiro (Ufrj)
SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).
Johann Wolfgang Goethe University
Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.
Goethe-University Frankfurt
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1.
Goethe-University Frankfurt
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
The Institute of Cancer Research
A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
Goethe-University Frankfurt
Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors.
Johann Wolfgang Goethe-University
A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.
Goethe-University Frankfurt
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
University of Oxford
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
University of Oxford
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
University of Cambridge
Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.
Ku Leuven
Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL).
Goethe-University Frankfurt
Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.
University of Oxford
Characterization of a highly selective inhibitor of the Aurora kinases.
Harvard Medical School
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
St. Jude Children'S Research Hospital
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Eberhard Karls University T£Bingen
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
University College London
Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.
University College London
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.
University of Oxford
2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
Shanghai Haiyan Pharmaceutical Technology
Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen and their use
St George'S Hosptial Medical School
Pentachlorophenol hydroxylase, a poorly functioning enzyme required for degradation of pentachlorophenol by Sphingobium chlorophenolicum.
University of Colorado Boulder
Imidazenil: a new partial positive allosteric modulator of gamma-aminobutyric acid (GABA) action at GABAA receptors.
Georgetown University
Structural requirements for the occupancy of rat brain PACAP receptors and adenylate cyclase activation.
UniversitÉ
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
F. Hoffmann-La Roche