Ubiquitination of transcription factors in cancer: unveiling therapeutic potential
In cancer, dysregulated ubiquitination of transcription factors contributes to the uncontrolled growth and survival characteristics of tumors. Tumor suppressors are degraded by aberrant ubiquitination, or oncogenic transcription factors gain stability through ubiquitination, thereby promoting tumorigenesis.
Dongha Kim, Hye Jin Nam, Sung Hee Baek
wiley +1 more source
In Vivo validation of a bioinformatics based tool to identify reduced replication capacity in HIV-1. [PDF]
Although antiretroviral drug resistance is common in treated HIV infected individuals, it is not a consistent indicator of HIV morbidity and mortality.
Kitchen, Christina MR+2 more
core +2 more sources
Measuring AMP‐activated protein kinase (AMPK) activity in vitro is crucial for testing AMPK activators or inhibitors with therapeutic potential. Here, we report an enzyme‐linked immunosorbent assay (ELISA)‐based AMPK activity assay with simple steps and high sensitivity, which offers a simple, robust, and cost‐effective alternative to traditional ...
Trezze P. Nguyen, Shangze Lyu, Yang Liu
wiley +1 more source
Drug design principles from electric field calculations: understanding SARS-CoV-2 main protease interaction with X77 non-covalent inhibitor [PDF]
Fast and effective drug discovery processes rely on rational drug design to circumvent the tedious and expensive trial and error approach. However, accurate predictions of new remedies, which are often enzyme inhibitors, require a clear understanding of the nature and function of the key players governing the interaction between the drug candidate and ...
arxiv
Cardiac Specific Overexpression of Mitochondrial Omi/HtrA2 Induces Myocardial Apoptosis and Cardiac Dysfunction. [PDF]
Myocardial apoptosis is a significant problem underlying ischemic heart disease. We previously reported significantly elevated expression of cytoplasmic Omi/HtrA2, triggers cardiomyocytes apoptosis.
Jiao, Kun+11 more
core +2 more sources
The impact of frailty syndrome on skeletal muscle histology: preventive effects of exercise
Frailty syndrome exacerbates skeletal muscle degeneration via increased ECM deposition and myofiber loss. This study, using a murine model, demonstrates that endurance exercise attenuates these histopathological alterations, preserving muscle integrity. Findings support exercise as a viable strategy to counteract frailty‐induced musculoskeletal decline
Fujue Ji+3 more
wiley +1 more source
Proposing a fungal metabolite-Flaviolin as a potential inhibitor of 3CLpro of novel coronavirus SARS-CoV2 using docking and molecular dynamics [PDF]
Here after performing docking and molecular dynamics of various small molecules derived as a secondary metabolite from fungi, we propose Flaviolin to act as potent inhibitor of 3-chymotrypsin (3C) like protease (3CLpro) of noval corona virus SARS-CoV2 responsible for pandemic condition caused by coronavirus disease 2019 (COVID-19).
arxiv
The impact of physiological stress conditions on protein structure and trypsin inhibition of serine protease inhibitor Kazal type 1 (SPINK1) and its N34S variant [PDF]
One of the most common mutations in the serine protease inhibitor Kazal type 1 (SPINK1) gene is the N34S variant which is strongly associated with chronic pancreatitis. Although it is assumed that N34S mutation constitutes a high-risk factor, the underlying pathologic mechanism is still unknown.
arxiv +1 more source
Reversal of aging-induced increases in aortic stiffness by targeting cytoskeletal protein-protein interfaces [PDF]
BACKGROUND: The proximal aorta normally functions as a critical shock absorber that protects small downstream vessels from damage by pressure and flow pulsatility generated by the heart during systole.
Chiu, Joanna+10 more
core +1 more source
Intraoral Drug Delivery: Bridging the Gap Between Academic Research and Industrial Innovations
Intraoral drug delivery offers a promising route for systemic and localized therapies, yet challenges such as enzymatic degradation, limited permeability, and microbial interactions hinder efficacy. This figure highlights innovative strategies—mucoadhesive materials, enzyme inhibitors, and permeation enhancers—to overcome these barriers.
Soheil Haddadzadegan+4 more
wiley +1 more source