Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors

Fragment-to-Lead Medicinal Chemistry Publications in 2021

(2023) Louise Walsh et al.   Journal of Medicinal Chemistry

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

(2023) Beatrice Noce et al.   Frontiers in Pharmacology

Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications

(2023) Fei-Fei Yang et al.   Journal of Medicinal Chemistry

Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses

(2022) Andreas Luttens et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Asciminib: new therapeutic option in chronic phase CML with treatment failure.

(2022) David T Yeung et al.   BLOOD

Establishing Trypanosoma cruzi farnesyl pyrophosphate synthase as a viable target for biosensor driven fragment‐based lead discovery

(2020) Giulia Opassi et al.   PROTEIN SCIENCE

Macrocyclic Peptides Uncover a Novel Binding Mode for Reversible Inhibitors of LSD1

(2020) Jie Yang et al.   ACS Omega

Crystal Structure of the LSD1/CoREST Histone Demethylase Bound to Its Nucleosome Substrate

(2020) Sang-Ah Kim et al.   MOLECULAR CELL

Fragment‐Based Discovery of Non‐bisphosphonate Binders of Trypanosoma brucei Farnesyl Pyrophosphate Synthase

(2020) Lena Münzker et al.   CHEMBIOCHEM

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

(2020) David S. Hong et al.   NEW ENGLAND JOURNAL OF MEDICINE

Major kinds of drug targets in Chagas disease or American Trypanosomiasis

(2019) Vilma G Duschak   CURRENT DRUG TARGETS

Dynamic behaviors of α-synuclein and tau in the cellular context: New mechanistic insights and therapeutic opportunities in neurodegeneration

(2019) Fred Yeboah et al.   NEUROBIOLOGY OF DISEASE

Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS)

(2019) Yuting Feng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells

(2019) Shuai Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Open for collaboration: an academic platform for drug discovery and development at SciLifeLab

(2016) Per I. Arvidsson et al.   DRUG DISCOVERY TODAY

Structures of endothiapepsin–fragment complexes from crystallographic fragment screening using a novel, diverse and affordable 96-compound fragment library

(2016) Franziska U. Huschmann et al.   Acta Crystallographica Section F-Structural Biology Communications

Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor

(2015) William D. Tap et al.   NEW ENGLAND JOURNAL OF MEDICINE

Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor

(2015) Radovan Spurny et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The 'rule of three' for fragment-based drug discovery: where are we now?

(2013) Harren Jhoti et al.   NATURE REVIEWS DRUG DISCOVERY

Histaminergic pharmacology of homo-oligomeric β3 γ-aminobutyric acid type A receptors characterized by surface plasmon resonance biosensor technology

(2012) Christian Seeger et al.   BIOCHEMICAL PHARMACOLOGY

Deconstruction of Non-Nucleoside Reverse Transcriptase Inhibitors of Human Immunodeficiency Virus Type 1 for Exploration of the Optimization Landscape of Fragments

(2011) Peter Brandt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Quantification of interactions between drug leads and serum proteins by use of “binding efficiency”

(2010) Sofia S. Gustafsson et al.   ANALYTICAL BIOCHEMISTRY

Interaction Kinetic and Structural Dynamic Analysis of Ligand Binding to Acetylcholine-Binding Protein

(2010) Matthis Geitmann et al.   BIOCHEMISTRY

Fragment Library Screening and Lead Characterization Using SPR Biosensors

(2009) U. Danielson   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Identification of MMP-12 Inhibitors by Using Biosensor-Based Screening of a Fragment Library

(2008) Helena Nordström et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

(2008) J. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA