Aug 2026· Bioengineering· Vol 13, pp. 953· 0 citations· 66 references
Medicine
TL;DR
The results support the structural feasibility of a previously uncharacterized receptor interaction and provide a reproducible computational framework for exploring GPCR-associated effects of cytotoxic agents.
Abstract
Background: Paclitaxel is a cornerstone chemotherapeutic agent widely used in breast cancer treatment, primarily through the stabilization of microtubule dynamics. Beyond its canonical tubulin-targeting activity, increasing evidence suggests that paclitaxel may engage additional molecular targets, contributing to its complex pharmacological profile. In this study, an integrated computational workflow was applied to evaluate the structural compatibility between paclitaxel and the neurokinin-2 receptor (NK2R), a G protein-coupled receptor involved in tumor-associated inflammatory and proliferative signaling pathways. Physicochemical profiling and target prediction were performed using SwissADME and SwissTargetPrediction, followed by molecular docking and molecular dynamics simulations using AutoDock Vina and GROMACS 2024.1. Paclitaxel exhibited physicochemical properties consistent with transient interactions in hydrophobic transmembrane environments. Docking analysis identified a plausible binding mode within the NK2R transmembrane cavity, primarily stabilized by hydrophobic contacts. Molecular dynamics simulations over 100 ns revealed stable ligand occupancy and overall complex stability, while MM-PBSA calculations indicated a favorable transient association. The predicted interaction is consistent with secondary or non-canonical receptor engagement. While NK2R is not established as a pharmacological target of paclitaxel, the results support the structural feasibility of a previously uncharacterized receptor interaction and provide a reproducible computational framework for exploring GPCR-associated effects of cytotoxic agents.
Cyclin-dependent kinase 20 (CDK20) is a promising oncology target, but the lack of high-resolution complex structures limits drug development. Here, we investigated the spontaneous association of BMS-357075 with CDK20 using microsecond-scale unbiased molecular dynamics simulations, including an extended 2.0-μs trajecto...
Hai-Xia Zhu, Wen-Shuai Xuan, Yan-Hong Wang et al.· International Journal of Bio...· 0 citations
A structure-based computational strategy to identify and characterize novel ROCK2 inhibitors is presented, applicable to the discovery of both small-molecule and peptidomimetic inhibitors, supporting broader efforts in structure-guided drug design targeting kinases involved in cancer and other diseases.
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Overall, MD1-MD5 demonstrated excellent binding, structural stability, and pharmacokinetic properties, making them strong candidates for future CDK2-targeted anticancer research.
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Cyclin-dependent kinase 6 (CDK6) contributes to G1-to-S cell-cycle progression and represents an established therapeutic target in hormone receptor-positive breast cancer. However, adverse effects and acquired resistance associated with current CDK4/6 inhibitors support continued investigation of alternative chemical s...
Syarifuddin Husain, Ruzianisra Mohamed, Khairul Bariyyah Abd. Halim et al.· Journal of Molecular Graphic...· 0 citations
Histone deacetylases (HDACs) are well-established therapeutic targets in cancer due to their critical roles in regulating histone acetylation, chromatin structure, and gene expression, which are associated with cell growth, differentiation, and apoptosis. This study aims to investigate the binding interactions of hydro...
Parthiban Gunasingham, Dushanan Ramachandran, D. Dissanayake et al.· OUSL Journal· 0 citations