A. Ehler
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View article: A high-resolution data set of fatty acid-binding protein structures. II. Crystallographic overview, ligand classes and binding pose
A high-resolution data set of fatty acid-binding protein structures. II. Crystallographic overview, ligand classes and binding pose Open
Fatty acid-binding protein isoforms 4 and 5 are potential diabetes and atherosclerosis targets. During a drug-design program aiming at dual isoform-specific FABP4/5 inhibitors with little or no affinity for FABP3, a set of crystal structur…
View article: A high-resolution data set of fatty acid-binding protein structures. I. Dynamics of FABP4 and ligand binding
A high-resolution data set of fatty acid-binding protein structures. I. Dynamics of FABP4 and ligand binding Open
Fatty acid-binding proteins (FABPs) are involved in the uptake and intracellular trafficking of fatty acids for metabolic and gene-regulatory purposes. FABPs are known to associate with membranes and also enter the nucleus. Using NMR and a…
View article: A high-resolution data set of fatty acid-binding protein structures. III. Unexpectedly high occurrence of wrong ligands
A high-resolution data set of fatty acid-binding protein structures. III. Unexpectedly high occurrence of wrong ligands Open
FABP4 has been implicated as a therapeutic target for treating diabetes and atherosclerosis. Structure-based drug design (SBDD) based on initial hits from high-throughput and fragment screens yielded 216 ligand-bound structures of human FA…
View article: Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib Open
Addressing resistance to third-generation EGFR TKIs such as osimertinib via the EGFRC797S mutation remains a highly unmet need in EGFR-driven non-small-cell lung cancer (NSCLC). Herein, we present the discovery of the allosteric EGFR inhib…
View article: Prodrug-Activating Chain Exchange (PACE) converts targeted prodrug derivatives to functional bi- or multispecific antibodies
Prodrug-Activating Chain Exchange (PACE) converts targeted prodrug derivatives to functional bi- or multispecific antibodies Open
Driven by the potential to broaden the target space of conventional monospecific antibodies, the field of multi-specific antibody derivatives is growing rapidly. The production and screening of these artificial proteins entails a high comb…
View article: P329G-CAR-J: a novel Jurkat-NFAT-based CAR-T reporter system recognizing the P329G Fc mutation
P329G-CAR-J: a novel Jurkat-NFAT-based CAR-T reporter system recognizing the P329G Fc mutation Open
Monoclonal antibody-based therapeutics are an integral part of treatment of different human diseases, and the selection of suitable antibody candidates during the discovery phase is essential. Here, we describe a novel, cellular screening …
View article: Variable heavy–variable light domain and Fab-arm CrossMabs with charged residue exchanges to enforce correct light chain assembly
Variable heavy–variable light domain and Fab-arm CrossMabs with charged residue exchanges to enforce correct light chain assembly Open
Technologies for the production of bispecific antibodies need to overcome two major challenges. The first one is correct heavy chain assembly, which was solved by knobs-into-holes technology or charge interactions in the CH3 domains. The s…
View article: CCDC 802437: Experimental Crystal Structure Determination
CCDC 802437: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 802438: Experimental Crystal Structure Determination
CCDC 802438: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 802436: Experimental Crystal Structure Determination
CCDC 802436: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 802439: Experimental Crystal Structure Determination
CCDC 802439: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Design of Potent and Druglike Nonphenolic Inhibitors for Catechol <i>O</i>-Methyltransferase Derived from a Fragment Screening Approach Targeting the <i>S</i>-Adenosyl-<scp>l</scp>-methionine Pocket
Design of Potent and Druglike Nonphenolic Inhibitors for Catechol <i>O</i>-Methyltransferase Derived from a Fragment Screening Approach Targeting the <i>S</i>-Adenosyl-<span>l</span>-methionine Pocket Open
A fragment screening approach designed to target specifically the S-adenosyl-l-methionine pocket of catechol O-methyl transferase allowed the identification of structurally related fragments of high ligand efficiency and with activity on t…