Results 291 to 300 of about 358,313 (362)

First Phosphonic‐Type Inhibitors and Activity‐Based Probes Specific to the O'nyong‐nyong Virus Capsid Protease

open access: yesChemMedChem, EarlyView.
The serine capsid protease (CP) catalyzes a crucial process of the alphaviral replication cycle; therefore, it constitutes an interesting therapy target. Herein, the O'nyong‐nyong virus CP profile activity with a specific fluorogenic substrate is analyzed and examines the inhibitory activity of a new series of phosphonic analogs of tryptophan and ...
Karolina Torzyk‐Jurowska   +5 more
wiley   +1 more source

Inhibition of Amyloid β-Protein Production in Neural Cells by the Serine Protease Inhibitor AEBSF

open access: bronze, 1996
Martin Citron   +5 more
openalex   +1 more source

Ligand Screening and Discovery Using Cocktail Soaking and Automated Microcrystal Electron Diffraction

open access: yesChemMedChem, EarlyView.
Cocktail soaking using single‐crystal X‐ray diffraction allows high‐throughput crystallographic ligand screening against protein targets. However, protein microcrystals are not amenable to this approach. Herein, a workflow integrating cocktail soaking with automated microcrystal electron diffraction to allow rapid ligand screening, structure ...
Jieye Lin   +3 more
wiley   +1 more source

New Pyridobenothiazolone Derivatives Display Nanomolar Pan‐Serotype Anti‐Dengue Virus Activity

open access: yesChemMedChem, EarlyView.
A ligand‐based strategy is employed, starting from hit compound 2, to develop the C‐2 modified pyridobenzothiazolone 19 as a pan‐serotype nanomolar DENV‐1‐4 inhibitor. Investigations of the mechanism reveal the peculiar ability to abolish the infectivity of virions in a second infection.
Tommaso Felicetti   +13 more
wiley   +1 more source

Deferasirox Derivatives as Inhibitors of Kallikrein‐Related Peptidases Associated to Neurodegenerative Diseases

open access: yesChemMedChem, EarlyView.
Dysregulated proteolysis mediated by kallikrein‐related peptidases (KLKs) and iron overload are involved in the progression of neurodegenerative diseases. Deferasirox, an clinically‐approved iron chelator, and its newly synthesized derivatives have been identified as inhibitors of major central nervous system KLKs with low cytotoxicity and effective ...
Rilès Boumali   +11 more
wiley   +1 more source

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