Results 91 to 100 of about 3,018,689 (332)

Potential therapeutic targeting of BKCa channels in glioblastoma treatment

open access: yesMolecular Oncology, EarlyView.
This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak   +4 more
wiley   +1 more source

Plecstatin inhibits hepatocellular carcinoma tumorigenesis and invasion through cytolinker plectin

open access: yesMolecular Oncology, EarlyView.
The ruthenium‐based metallodrug plecstatin exerts its anticancer effect in hepatocellular carcinoma (HCC) primarily through selective targeting of plectin. By disrupting plectin‐mediated cytoskeletal organization, plecstatin inhibits anchorage‐dependent growth, cell polarization, and tumor cell dissemination.
Zuzana Outla   +10 more
wiley   +1 more source

Combining antibody conjugates with cytotoxic and immune‐stimulating payloads maximizes anti‐cancer activity

open access: yesMolecular Oncology, EarlyView.
Methods to improve antibody–drug conjugate (ADC) treatment durability in cancer therapy are needed. We utilized ADCs and immune‐stimulating antibody conjugates (ISACs), which are made from two non‐competitive antibodies, to enhance the entry of toxic payloads into cancer cells and deliver immunostimulatory agents into immune cells.
Tiexin Wang   +3 more
wiley   +1 more source

Arrhythmogenic cardiomyopathy related DSG2 mutations affect desmosomal cadherin binding kinetics

open access: yesScientific Reports, 2017
Cadherins are calcium dependent adhesion proteins that establish the intercellular mechanical contact by bridging the gap to adjacent cells. Desmoglein-2 (Dsg2) is a specific cadherin of the cell-cell contact in cardiac desmosomes.
M. Dieding   +6 more
semanticscholar   +1 more source

Dammarenediol II enhances etoposide‐induced apoptosis by targeting O‐GlcNAc transferase and Akt/GSK3β/mTOR signaling in liver cancer

open access: yesMolecular Oncology, EarlyView.
Etoposide induces DNA damage, activating p53‐dependent apoptosis via caspase‐3/7, which cleaves PARP1. Dammarenediol II enhances this apoptotic pathway by suppressing O‐GlcNAc transferase activity, further decreasing O‐GlcNAcylation. The reduction in O‐GlcNAc levels boosts p53‐driven apoptosis and influences the Akt/GSK3β/mTOR signaling pathway ...
Jaehoon Lee   +8 more
wiley   +1 more source

New approaches for the reliable in vitro assessment of binding affinity based on high-resolution real-time data acquisition of radioligand-receptor binding kinetics

open access: yesEJNMMI Research, 2017
BackgroundResolving the kinetic mechanisms of biomolecular interactions have become increasingly important in early-phase drug development. Since traditional in vitro methods belong to dose-dependent assessments, binding kinetics is usually overlooked ...
M. Zeilinger   +6 more
semanticscholar   +1 more source

A general model for analysis of linear and hyperbolic enzyme inhibition mechanisms

open access: yesFEBS Open Bio, EarlyView.
We developed a general enzyme kinetic model that integrates these six basic inhibition mechanism onto a single one. From this model, we deduced a general enzyme kinetic equation that through modulation of simple parameters, γ (the relative inhibitor affinity for two binding sites) and β (the reactivity of the enzyme–substrate–inhibitor complex), is ...
Rafael S. Chagas, Sandro R. Marana
wiley   +1 more source

Kinetics of Multivalent Binding Processes

open access: yes, 2022
Multivalent bindings are a combination of several weaker bonds between two molecules such as a receptor and a ligand. Because the combined bonds are stronger than the individual ones, the molecules may interact longer. Thus, this concept is very interesting for targeted drug design.
openaire   +2 more sources

HSP70 governs permeability and mechanotransduction in primary human endothelial cells

open access: yesFEBS Open Bio, EarlyView.
HSP70 chemical inhibition reduces endothelial cell proliferation and increases permeability, the latter supported by normal interendothelial junctional protein distribution. HSP70 also plays a role in shear stress response, a hemodynamic force naturally present in blood vessels and correlated with vessel protection.
Andrea Pinto‐Martinez   +5 more
wiley   +1 more source

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