Jörg Labahn
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View article: Identification, validation, and characterization of approved and investigational drugs interfering with the <scp>SARS</scp>‐<scp>CoV</scp>‐2 endoribonuclease Nsp15
Identification, validation, and characterization of approved and investigational drugs interfering with the <span>SARS</span>‐<span>CoV</span>‐2 endoribonuclease Nsp15 Open
Since the emergence of SARS‐CoV‐2 at the end of 2019, the virus has caused significant global health and economic disruptions. Despite the rapid development of antiviral vaccines and some approved treatments such as remdesivir and paxlovid…
View article: Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A<sub>2A</sub> Receptor with Preladenant Conjugates
Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A<sub>2A</sub> Receptor with Preladenant Conjugates Open
The G protein‐coupled adenosine A 2A receptor (A 2A AR) is an important new (potential) drug target in immuno‐oncology, and for neurodegenerative diseases. Preladenant and its derivatives belong to the most potent A 2A AR antagonists displ…
View article: Mutual Enhancement of Opioid and Adrenergic Receptors by Combinations of Opioids and Adrenergic Ligands Is Reflected in Molecular Complementarity of Ligands: Drug Development Possibilities
Mutual Enhancement of Opioid and Adrenergic Receptors by Combinations of Opioids and Adrenergic Ligands Is Reflected in Molecular Complementarity of Ligands: Drug Development Possibilities Open
Crosstalk between opioid and adrenergic receptors is well characterized and due to interactions between second messenger systems, formation of receptor heterodimers, and extracellular allosteric binding regions. Both classes of receptors b…
View article: QTY code enables design of detergent-free chemokine receptors that retain ligand-binding activities
QTY code enables design of detergent-free chemokine receptors that retain ligand-binding activities Open
Significance The QTY (glutamine, threonine, and tyrosine) code-designed detergent-free chemokine receptors may be useful in many applications. The QTY variants may be useful not only as reagents in deorphanization studies but also for desi…
View article: Adrenergic Agonists Bind to Adrenergic-Receptor-Like Regions of the Mu Opioid Receptor, Enhancing Morphine and Methionine-Enkephalin Binding: A New Approach to “Biased Opioids”?
Adrenergic Agonists Bind to Adrenergic-Receptor-Like Regions of the Mu Opioid Receptor, Enhancing Morphine and Methionine-Enkephalin Binding: A New Approach to “Biased Opioids”? Open
Extensive evidence demonstrates functional interactions between the adrenergic and opioid systems in a diversity of tissues and organs. While some effects are due to receptor and second messenger cross-talk, recent research has revealed an…
View article: Expression, purification, and preliminary characterization of human presenilin-2
Expression, purification, and preliminary characterization of human presenilin-2 Open
Presenilins (PS1 and PS2) exhibit similar γ-secretase-dependent and −independent functions with subtle variations. In this study, we established a cost-effective process to overexpress and purify full-length human PS2 in sufficient quantit…
View article: Fibril structure of amyloid-β(1–42) by cryo–electron microscopy
Fibril structure of amyloid-β(1–42) by cryo–electron microscopy Open
Elucidating pathological fibril structure Amyloid-β (Aβ) is a key pathological contributor to Alzheimer's disease. Gremer et al. used cryoelectron microscopy data to build a high-quality de novo atomic model of Aβ fibrils (see the Perspect…
View article: High-efficient production and biophysical characterisation of nicastrin and its interaction with APPC100
High-efficient production and biophysical characterisation of nicastrin and its interaction with APPC100 Open
Nicastrin, the largest member among the four components of the γ-secretase complex, has been identified to be the substrate recognizer for the proteolytic activity of the complex. Here we report that full-length human nicastrin (hNCT) can …
View article: Stray Light Correction in the Optical Spectroscopy of Crystals
Stray Light Correction in the Optical Spectroscopy of Crystals Open
It has long been known in spectroscopy that light not passing through a sample, but reaching the detector (i.e., stray light), results in a distortion of the spectrum known as absorption flattening. In spectroscopy with crystals, one must …