Fluorine NMR functional screening: from purified enzymes to human intact living cells

Perfluoro-tert-Butyl Hydroxyprolines as Sensitive, Conformationally Responsive Molecular Probes: Detection of Protein Kinase Activity by 19F NMR

(2020) Caitlin M. Tressler et al.   ACS Chemical Biology

Synthesis of Trifluoromethylated Purine Ribonucleotides and Their Evaluation as 19F NMR Probes

(2020) Mikolaj Chrominski et al.   JOURNAL OF ORGANIC CHEMISTRY

Ligand-Efficient Inhibitors of Trichomonas vaginalis Adenosine/Guanosine Preferring Nucleoside Ribohydrolase

(2019) Samantha N. Muellers et al.   ACS Infectious Diseases

Fast NMR methods for measuring in direct and/or competition mode the dissociation binding constants of chemical fragments interacting with a receptor

(2019) Alexey Rak et al.   ChemMedChem

19F-NMR in target-based drug discovery

(2019) Cong Bao Kang   CURRENT MEDICINAL CHEMISTRY

Nonafluoro-tert-butoxylation of Diaryliodonium Salts

(2019) Huan Meng et al.   ORGANIC LETTERS

Approaches to Obtaining Fluorinated α-Amino Acids

(2019) Johann Moschner et al.   CHEMICAL REVIEWS

Trifluridine/Tipiracil: A Review in Metastatic Gastric Cancer

(2019) Connie Kang et al.   DRUGS

Exposing Small-Molecule Nanoentities by a Nuclear Magnetic Resonance Relaxation Assay

(2019) Yann Ayotte et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Ligand-Efficient Scaffolds for the Design of Novel Trichomonas vaginalis Uridine Nucleoside Ribohydrolase Inhibitors Using Fragment Screening

(2019) Shannon Auletta et al.   ACS Omega

SAR by (Protein-Observed) 19F NMR

(2019) Anand Divakaran et al.   ACCOUNTS OF CHEMICAL RESEARCH

Applications of fluorine-containing amino acids for drug design

(2019) Haibo Mei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design

(2018) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

The inhibition of thymidine phosphorylase can reverse acquired 5FU-resistance in gastric cancer cells

(2018) Ryutaro Mori et al.   Gastric Cancer

Ligand-Based Fluorine NMR Screening: Principles and Applications in Drug Discovery Projects

(2018) Claudio Dalvit et al.   JOURNAL OF MEDICINAL CHEMISTRY

Trifluridine/tipiracil versus placebo in patients with heavily pretreated metastatic gastric cancer (TAGS): a randomised, double-blind, placebo-controlled, phase 3 trial

(2018) Kohei Shitara et al.   LANCET ONCOLOGY

Strategic incorporation of fluorine into taxoid anticancer agents for medicinal chemistry and chemical biology studies

(2017) Iwao Ojima   JOURNAL OF FLUORINE CHEMISTRY

NMR Methods for Identification of False Positives in Biochemical Screens

(2017) Anamarija Zega   JOURNAL OF MEDICINAL CHEMISTRY

Fluorine nuclear magnetic resonance-based assay in living mammalian cells

(2016) Marina Veronesi et al.   ANALYTICAL BIOCHEMISTRY

19F NMR matrix-assisted DOSY: a versatile tool for differentiating fluorinated species in mixtures

(2016) Guilherme Dal Poggetto et al.   MAGNETIC RESONANCE IN CHEMISTRY

Applications of 19F-NMR in Fragment-Based Drug Discovery

(2016) Raymond Norton et al.   MOLECULES

Biophysics in drug discovery: impact, challenges and opportunities

(2016) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis of Perfluoro-tert-butyl Tyrosine, for Application in 19F NMR, via a Diazonium-Coupling Reaction

(2016) Caitlin M. Tressler et al.   ORGANIC LETTERS

TAS-102, a novel antitumor agent: A review of the mechanism of action

(2015) Heinz-Josef Lenz et al.   CANCER TREATMENT REVIEWS

Development and Application of a Virtual Screening Protocol for the Identification of Multitarget Fragments

(2015) Giovanni Bottegoni et al.   ChemMedChem

A comparison of chemical shift sensitivity of trifluoromethyl tags: optimizing resolution in 19F NMR studies of proteins

(2015) Libin Ye et al.   JOURNAL OF BIOMOLECULAR NMR

Design, synthesis and application of fluorine-labeled taxoids as 19F NMR probes for the metabolic stability assessment of tumor-targeted drug delivery systems

(2015) Joshua D. Seitz et al.   JOURNAL OF FLUORINE CHEMISTRY

Protein-Observed Fluorine NMR: A Bioorthogonal Approach for Small Molecule Discovery

(2015) Keith E. Arntson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Fluorophosphate Nucleotide Analogues and Their Characterization as Tools for 19F NMR Studies

(2015) Marek R. Baranowski et al.   JOURNAL OF ORGANIC CHEMISTRY

Identification of proton-pump inhibitor drugs that inhibit Trichomonas vaginalis uridine nucleoside ribohydrolase

(2014) Tara A. Shea et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Repositioning the Substrate Activity Screening (SAS) Approach as a Fragment-Based Method for Identification of Weak Binders

(2014) Rafaela Gladysz et al.   CHEMBIOCHEM

(2S,4R)- and (2S,4S)-Perfluoro-tert-butyl 4-Hydroxyproline: Two Conformationally Distinct Proline Amino Acids for Sensitive Application in 19F NMR

(2014) Caitlin M. Tressler et al.   JOURNAL OF ORGANIC CHEMISTRY

19F NMR monitoring of the eukaryotic 20S proteasome chymotrypsin-like activity: an investigative tool for studying allosteric regulation

(2014) M. Keita et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Development of Fragment-Basedn-FABS NMR Screening Applied to the Membrane Enzyme FAAH

(2013) Chiara Lambruschini et al.   CHEMBIOCHEM

Fluorine NMR reporter for phosphate anions

(2013) Haiying Gan et al.   CHEMICAL COMMUNICATIONS

Fluoromethylated derivatives of carnitine biosynthesis intermediates – synthesis and applications

(2013) Anna M. Rydzik et al.   CHEMICAL COMMUNICATIONS

19F NMR: a valuable tool for studying biological events

(2013) Han Chen et al.   CHEMICAL SOCIETY REVIEWS

Design and Generation of Highly Diverse Fluorinated Fragment Libraries and their Efficient Screening with Improved19F NMR Methodology

(2013) Anna Vulpetti et al.   ChemMedChem

Fluorine NMR-Based Screening on Cell Membrane Extracts

(2013) Marina Veronesi et al.   ChemMedChem

Universal Caging Group for the in-Cell Detection of Glutathione Transferase Applied to 19F NMR and Bioluminogenic Probes

(2012) Mika Ito et al.   CHEMBIOCHEM

Fluorine local environment: from screening to drug design

(2012) Anna Vulpetti et al.   DRUG DISCOVERY TODAY

TAS-102 monotherapy for pretreated metastatic colorectal cancer: a double-blind, randomised, placebo-controlled phase 2 trial

(2012) Takayuki Yoshino et al.   LANCET ONCOLOGY

Technical and practical aspects of 19F NMR-based screening: toward sensitive high-throughput screening with rapid deconvolution

(2012) Claudio Dalvit et al.   MAGNETIC RESONANCE IN CHEMISTRY

Monitoring Biocatalytic Transformations Mediated by Polyketide Synthase Enzymes in Cell Lysate via Fluorine NMR

(2012) Adrian Keatinge-Clay et al.   SYNLETT

Fluorinated Amino-Derivatives of the Sesquiterpene Lactone, Parthenolide, as19F NMR Probes in Deuterium-Free Environments

(2011) James R. Woods et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)

(2011) Yuan Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Current applications of 19F NMR to studies of protein structure and dynamics

(2011) Julianne L. Kitevski-LeBlanc et al.   PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY

Simultaneous 19F NMR Screening of Prolyl Oligopeptidase and Dipeptidyl Peptidase IV Inhibitors

(2010) Nessim Kichik et al.   CHEMBIOCHEM

19F NMR chemical shift prediction with fluorine fingerprint descriptor

(2010) Anna Vulpetti et al.   JOURNAL OF FLUORINE CHEMISTRY

Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism

(2010) Jason R Clapper et al.   NATURE NEUROSCIENCE

Dual-Function Probe to Detect Protease Activity for Fluorescence Measurement and19F MRI

(2009) Shin Mizukami et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Identification of Allosteric PIF-Pocket Ligands for PDK1 using NMR-Based Fragment Screening and1H-15N TROSY Experiments

(2009) Brian J. Stockman et al.   Chemical Biology & Drug Design

Use of fluorinated functionality in enzyme inhibitor development: Mechanistic and analytical advantages

(2008) David B. Berkowitz et al.   JOURNAL OF FLUORINE CHEMISTRY

19F NMR applications in chemical biology

(2008) Steven L. Cobb et al.   JOURNAL OF FLUORINE CHEMISTRY

2-Fluoro-ATP as a Versatile Tool for19F NMR-Based Activity Screening

(2008) Brian J. Stockman   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Improved synthesis of polyfluorinated l-lysine for 19F NMR-based screening

(2008) Beatrice Malgesini et al.   MOLECULAR DIVERSITY