Peptide‐based ligand antagonists block a Vibrio cholerae adhesin
The structure of a peptide‐binding domain of the Vibrio cholerae adhesin FrhA was solved by X‐ray crystallography, revealing how the inhibitory peptide AGYTD binds tightly at its Ca2+‐coordinated pocket. Structure‐guided design incorporating D‐amino acids enhanced binding affinity, providing a foundation for developing anti‐adhesion therapeutics ...
Mingyu Wang +9 more
wiley +1 more source
Potent, multi-target serine protease inhibition achieved by a simplified β-sheet motif.
Engagement of an extended β-sheet is a common substrate/inhibitor interaction at the active site of serine proteases and is an important feature of Laskowski mechanism inhibitors that present a substrate-like loop to a target protease.
Xingchen Chen +10 more
doaj +1 more source
Plant Kunitz Inhibitors and Their Interaction with Proteases: Current and Potential Pharmacological Targets [PDF]
Camila Ramalho Bonturi +7 more
openalex +1 more source
A folding inhibitor of the HIV-1 Protease
Being the HIV-1 Protease (HIV-1-PR) an essential enzyme in the viral life cycle, its inhibition can control AIDS. The folding of single domain proteins, like each of the monomers forming the HIV-1-PR homodimer, is controlled by local elementary ...
Abkevich +35 more
core +1 more source
Disordered but rhythmic—the role of intrinsic protein disorder in eukaryotic circadian timing
Unstructured domains known as intrinsically disordered regions (IDRs) are present in nearly every part of the eukaryotic core circadian oscillator. IDRs enable many diverse inter‐ and intramolecular interactions that support clock function. IDR conformations are highly tunable by post‐translational modifications and environmental conditions, which ...
Emery T. Usher, Jacqueline F. Pelham
wiley +1 more source
Three cryo-EM structures of CD109 reveal its mechanism of protease inhibition
Summary: CD109 is a glycosylphosphatidylinositol-anchored protein. In addition to regulating transforming growth factor β (TGF-β) network signaling, CD109 is also a protease inhibitor. Protease cleavage of its bait region triggers a conformational change
Ana V. Almeida +7 more
doaj +1 more source
Background Host proteases have been shown to play important roles in many viral activities such as entry, uncoating, viral protein production and disease induction.
Winke Van der Gucht +7 more
doaj +1 more source
Identification of medicinal plant-based phytochemicals as a potential inhibitor for SARS-CoV-2 main protease (Mpro) using molecular docking and deep learning methods [PDF]
Alomgir Hossain +6 more
openalex +1 more source
Hepatitis C virus cell-cell transmission and resistance to direct-acting antiviral agents [PDF]
Hepatitis C virus (HCV) is transmitted between hepatocytes via classical cell entry but also uses direct cell-cell transfer to infect neighboring hepatocytes.
A Owsianka +72 more
core +7 more sources
The role of histone modifications in transcription regulation upon DNA damage
This review discusses the critical role of histone modifications in regulating gene expression during the DNA damage response (DDR). By modulating chromatin structure and recruiting repair factors, these post‐translational modifications fine‐tune transcriptional programmes to maintain genomic stability.
Angelina Job Kolady, Siyao Wang
wiley +1 more source

