Fine-Tuning the Proteolytic Stability of Peptides with Fluorinated Amino Acids

Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity

(2017) Simon J. Middendorp et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Current State of Peptide Drug Discovery: Back to the Future?

(2017) Antoine Henninot et al.   JOURNAL OF MEDICINAL CHEMISTRY

Endomorphins: Promising Endogenous Opioid Peptides for the Development of Novel Analgesics

(2017) Zheng-Hui Gu et al.   NEUROSIGNALS

Angiotensin II for the Treatment of Vasodilatory Shock

(2017) Ashish Khanna et al.   NEW ENGLAND JOURNAL OF MEDICINE

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

(2016) Yu Zhou et al.   CHEMICAL REVIEWS

Oral Administration of Peptide-Based Drugs: Beyond Lipinski's Rule

(2016) Gabriela B. Santos et al.   ChemMedChem

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

(2015) Vanessa Baeriswyl et al.   ACS Chemical Biology

Peptide therapeutics: current status and future directions

(2015) Keld Fosgerau et al.   DRUG DISCOVERY TODAY

Effects of single substitutions with hexafluoroleucine and trifluorovaline on the hydrophobic core formation of a heterodimeric coiled coil

(2015) Susanne Huhmann et al.   JOURNAL OF FLUORINE CHEMISTRY

Synthesis of Mixed Opioid Affinity Cyclic Endomorphin-2 Analogues with Fluorinated Phenylalanines

(2015) Justyna Piekielna et al.   ACS Medicinal Chemistry Letters

Strategic Approaches to Optimizing Peptide ADME Properties

(2014) Li Di   AAPS Journal

Fluorinated Proteins: From Design and Synthesis to Structure and Stability

(2014) E. Neil G. Marsh   ACCOUNTS OF CHEMICAL RESEARCH

Impact of fluorination on proteolytic stability of peptides: a case study with α-chymotrypsin and pepsin

(2014) Vivian Asante et al.   AMINO ACIDS

Factor XII: a drug target for safe interference with thrombosis and inflammation

(2014) Ellinor Kenne et al.   DRUG DISCOVERY TODAY

Pharmacological characterization of endomorphin-2-based cyclic pentapeptides with methylated phenylalanine residues

(2014) Renata Perlikowska et al.   PEPTIDES

Synthesis of enantiomerically pure (2S,3S)-5,5,5-trifluoroisoleucine and (2R,3S)-5,5,5-trifluoro-allo-isoleucine

(2013) Holger Erdbrink et al.   Beilstein Journal of Organic Chemistry

Impact of fluorination on proteolytic stability of peptides in human blood plasma

(2013) Vivian Asante et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fluorine in Pharmaceutical Industry: Fluorine-Containing Drugs Introduced to the Market in the Last Decade (2001–2011)

(2013) Jiang Wang et al.   CHEMICAL REVIEWS

Development of a Selective Peptide Macrocycle Inhibitor of Coagulation Factor XII toward the Generation of a Safe Antithrombotic Therapy

(2013) Vanessa Baeriswyl et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis for the enhanced stability of highly fluorinated proteins

(2012) B. C. Buer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Fluorinated amino acids: compatibility with native protein structures and effects on protein–protein interactions

(2011) Mario Salwiczek et al.   CHEMICAL SOCIETY REVIEWS

Endomorphins: potential roles and therapeutic indications in the development of opioid peptide analgesic drugs

(2011) Wei X. Liu et al.   MEDICINAL RESEARCH REVIEWS

Fluorine in health care: Organofluorine containing blockbuster drugs

(2010) David O’Hagan   JOURNAL OF FLUORINE CHEMISTRY

Residue-specific global fluorination of Candida antarctica lipase B in Pichia pastoris

(2010) Nediljko Budisa et al.   Molecular BioSystems

Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors

(2009) Anna Łęgowska et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Positional effects of monofluorinated phenylalanines on histone acetyltransferase stability and activity

(2009) Natalya Voloshchuk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthetic therapeutic peptides: science and market

(2009) Patrick Vlieghe et al.   DRUG DISCOVERY TODAY

A new paradigm for protein design and biological self-assembly

(2009) Gizem Akçay et al.   JOURNAL OF FLUORINE CHEMISTRY

Fluorine in Protein Environments: A QM and MD Study

(2009) Sergey A. Samsonov et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Synthesis and biological evaluation of cyclic endomorphin-2 analogs

(2009) Renata Perlikowska et al.   PEPTIDES

The Fluorous Effect in Proteins: Properties of α4F6, a 4-α-Helix Bundle Protein with a Fluorocarbon Core†

(2008) Lindsey M. Gottler et al.   BIOCHEMISTRY

Using Fluorous Amino Acids to Modulate the Biological Activity of an Antimicrobial Peptide

(2008) Lindsey M. Gottler et al.   CHEMBIOCHEM

Influence of Selective Fluorination on the Biological Activity and Proteolytic Stability of Glucagon-like Peptide-1

(2008) He Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorine in medicinal chemistry

(2007) Sophie Purser et al.   CHEMICAL SOCIETY REVIEWS