Christoph P. Sager
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View article: Time-resolved structures of β <sub>2</sub> -adrenergic receptor modulation by a photoswitchable beta-blocker
Time-resolved structures of β <sub>2</sub> -adrenergic receptor modulation by a photoswitchable beta-blocker Open
G protein-coupled receptors (GPCRs) regulate essential physiological responses and are important drug targets, yet their ligand-induced conformational dynamics remain poorly understood. The β 2 -adrenergic receptor (β 2 AR) is a prominent …
View article: Discovery of Galactopyranose‐1‐carboxamides as a New Class of Small, Novel, Potent, Selective, and Orally Active Galectin‐3 Inhibitors
Discovery of Galactopyranose‐1‐carboxamides as a New Class of Small, Novel, Potent, Selective, and Orally Active Galectin‐3 Inhibitors Open
Galectin‐3 (Gal‐3), a β‐galactoside‐binding lectin, is implicated in diverse cellular functions ranging from immune response modulation to tissue homeostasis. Notably, increased Gal‐3 expression has been linked to the progression of numero…
Which Properties Allow Ligands to Open and Bind to the Transient Binding Pocket of Human Aldose Reductase? Open
The transient specificity pocket of aldose reductase only opens in response to specific ligands. This pocket may offer an advantage for the development of novel, more selective ligands for proteins with similar topology that lack such an a…
Hydroxyl Groups in Synthetic and Natural-Product-Derived Therapeutics: A Perspective on a Common Functional Group Open
By forming extended hydrogen-bond networks, the contribution of hydroxyl groups to affinity can reach several orders of magnitude. However, because of the high directionality of their interactions, a maximal affinity gain can only be achie…
Front Cover: Improvement of Aglycone π‐Stacking Yields Nanomolar to Sub‐nanomolar FimH Antagonists (ChemMedChem 7/2019) Open
The Front Cover illustrates the adherence of uropathogenic E. coli to the bladder epithelium, depicting the initial step of a urinary tract infection (UTI). This adhesion is mediated by the adhesin FimH, located at the tip of type 1 pili o…
What contributes to an effective mannose recognition domain? Open
In general, carbohydrate–lectin interactions are characterized by high specificity but also low affinity. The main reason for the low affinities are desolvation costs, due to the numerous hydroxy groups present on the ligand, together with…
The price of flexibility – a case study on septanoses as pyranose mimetics Open
Interacting with lectins, mannose can be mimicked with seven-membered ring analogues but at the price of a substantial entropy penalty.
In-silico evaluation of carbohydrate–lectin interactions : bridging oligosaccharides and glycomimetics Open
Carbohydrates play a vital role in a variety of physiological and pathological processes and, hence, represent an exciting class of molecules for the development of new therapeutic approaches. \nHowever, carbohydrates have disadvantages su…