SPR-based fragment screening with neurotensin receptor 1 generates novel small molecule ligands

Real-time monitoring of binding events on a thermostabilized human A2A receptor embedded in a lipid bilayer by surface plasmon resonance

(2015) Nicolas Bocquet et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties

(2015) John A. Christopher et al.   MedChemComm

Improving the apo-state detergent stability of NTS1 with CHESS for pharmacological and structural studies

(2014) Daniel J. Scott et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties

(2014) Michel Demeule et al.   JOURNAL OF CLINICAL INVESTIGATION

Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution inEscherichia coli

(2014) Pascal Egloff et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

NMR approaches in structure-based lead discovery: Recent developments and new frontiers for targeting multi-protein complexes

(2014) David M. Dias et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

Fragment screening by SPR and advanced application to GPCRs

(2014) Claire A. Shepherd et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

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

(2013) Anna Vulpetti et al.   ChemMedChem

Fragment-based drug discovery using NMR spectroscopy

(2013) Mary J. Harner et al.   JOURNAL OF BIOMOLECULAR NMR

Biophysical Fragment Screening of the β1-Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

(2013) John A. Christopher et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor

(2013) Tonia Aristotelous et al.   ACS Medicinal Chemistry Letters

Fragment Screening of GPCRs Using Biophysical Methods: Identification of Ligands of the Adenosine A2A Receptor with Novel Biological Activity

(2012) Dan Chen et al.   ACS Chemical Biology

Fragment-Based Approaches in Drug Discovery and Chemical Biology

(2012) Duncan E. Scott et al.   BIOCHEMISTRY

Direct Molecular Evolution of Detergent-Stable G Protein-Coupled Receptors Using Polymer Encapsulated Cells

(2012) Daniel J. Scott et al.   JOURNAL OF MOLECULAR BIOLOGY

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

Neuropeptide receptor ligands as drugs for psychiatric diseases: the end of the beginning?

(2012) Guy Griebel et al.   NATURE REVIEWS DRUG DISCOVERY

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

A crystal clear solution for determining G-protein-coupled receptor structures

(2012) Christopher G. Tate   TRENDS IN BIOCHEMICAL SCIENCES

Structure of the Acid-sensing ion channel 1 in complex with the gating modifier Psalmotoxin 1

(2012) Roger J.P. Dawson et al.   Nature Communications

Biacore analysis with stabilized G-protein-coupled receptors

(2010) Rebecca L. Rich et al.   ANALYTICAL BIOCHEMISTRY

Application of Fragment-Based Drug Discovery to Membrane Proteins: Identification of Ligands of the Integral Membrane Enzyme DsbB

(2010) Virginie Früh et al.   CHEMISTRY & BIOLOGY

NMR Screening and Hit Validation in Fragment Based Drug Discovery

(2010) Ramon Campos-Olivas   CURRENT TOPICS IN MEDICINAL CHEMISTRY

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

(2010) Nathan Robertson et al.   NEUROPHARMACOLOGY

From fragment to clinical candidate—a historical perspective

(2009) Gianni Chessari et al.   DRUG DISCOVERY TODAY