Lifting the veils on transmembrane proteins: Potential anticancer targets.

Eur J Pharmacol

Department of Epidemiology and Health Statistics, School of Public Health, Southeast University, Nanjing, China; Key Laboratory of Environmental Medicine Engineering, Ministry of Education, School of Public Health, Southeast University, Nanjing, China. Electronic address:

Published: January 2024


Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

Cancer, as a prevalent cause of mortality, poses a substantial global health burden and hinders efforts to enhance life expectancy. Nevertheless, the prognosis of patients with malignant tumors remains discouraging, owing to the lack of specific diagnostic and therapeutic targets. Therefore, the development of early diagnostic indicators and novel therapeutic drugs for the prevention and treatment of cancer is essential. Transmembrane proteins (TMEMs) are a class of proteins that can span the phospholipid bilayer and are stably anchored. They are associated with fibrotic diseases, neurodegenerative diseases, autoimmune diseases, developmental disorders, and cancer. It has been found that the expression levels of TMEMs were elevated or reduced in cancer cells, exerting pro/anticancer effects. These aberrant expression levels have also been linked to the prognostic and clinicopathological features of diverse tumors. In this review, the structures, functions, and roles of TMEMs in cancer were discussed, and the scientific perspectives were described. This review also explored the potential of TMEMs as tumor drug candidates from the perspective of targeted therapies, and the challenges that need to be overcome in a wide range of preclinical and clinical anticancer research were summarized.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2023.176225DOI Listing

Publication Analysis

Top Keywords

transmembrane proteins
8
expression levels
8
cancer
5
lifting veils
4
veils transmembrane
4
proteins potential
4
potential anticancer
4
anticancer targets
4
targets cancer
4
cancer prevalent
4

Similar Publications

Agonist-induced interaction of G protein-coupled receptors (GPCRs) with β-arrestins (βarrs) is a critical mechanism that regulates the spatiotemporal pattern of receptor localization and signaling. While the underlying mechanism governing GPCR-βarr interaction is primarily conserved and involves receptor activation and phosphorylation, there are several examples of receptor-specific fine-tuning of βarr-mediated functional outcomes. Considering the key contribution of conformational plasticity of βarrs in driving receptor-specific functional responses, it is important to develop novel sensors capable of reporting distinct βarr conformations in cellular context.

View Article and Find Full Text PDF

Background: The approval of cystic fibrosis transmembrane conductance regulator modulators elexacaftor/tezacaftor/ivacaftor (ETI), has significantly improved pulmonary function for people with cystic fibrosis (pwCF). However, the effects on CF-related bone disease and body composition remain unclear.

Methods: This retrospective real-world study examined adults with CF who received ETI treatment.

View Article and Find Full Text PDF

Unlabelled: The study aimed to evaluate fecal calprotectin levels as indicators of intestinal inflammation in children with cystic fibrosis while examining their relationship with clinical signs, genetic mutations, and therapeutic approaches. Due to the limited number of patients with certain mutation types and the heterogeneity of mutations, patients were grouped accordingly for the analysis of fecal calprotectin levels, in relation to genetic mutation categories. This single-centre study at Istanbul Medical Faculty included 45 cystic fibrosis patients (19 girls, 26 boys) aged 1-18 years and 45 age- and sex-matched healthy controls.

View Article and Find Full Text PDF

A GFP Complementation-based Dual-expression System for Assessing Cell-Cell Contact Mediated by Cytonemes in Live Drosophila Wing Imaginal Discs.

J Vis Exp

August 2025

Institut de recherches cliniques de Montréal (IRCM); Programmes de biologie moléculaire, Université de Montréal; Département de Médecine, Université de Montréal;

Embryonic tissue growth and patterning are largely controlled by signals exchanged locally between cell populations within the tissues themselves. Cytonemes are a type of signaling filopodia first identified in Drosophila that connect and mediate exchange between signal-producing and signal-receiving cells. In the developing Drosophila wing imaginal disc, cytonemes are involved in signal exchange between distinct populations of cells within the disc proper (DP) epithelium, which will form the adult wing, as well as between DP cells and cells in adjacent disc-associated tissues.

View Article and Find Full Text PDF

Pentameric ligand-gated ion channels control synaptic neurotransmission via an allosteric mechanism, whereby agonist binding induces global protein conformational changes that open an ion-conducting pore. For the proton-activated bacterial () ligand-gated ion channel (GLIC), high-resolution structures are available in multiple conformational states. We used a library of atomistic molecular dynamics (MD) simulations to study conformational changes and to perform dynamic network analysis to elucidate the communication pathways underlying the gating process.

View Article and Find Full Text PDF