Development of an Integrated Computational Pipeline for PARP-1 Inhibitor Screening Using Hybrid Virtual Screening and Molecular Dynamics Simulations

利用混合虚拟筛选和分子动力学模拟开发用于PARP-1抑制剂筛选的集成计算流程

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Abstract

Despite the promising anticancer properties of PARP-1 inhibitors, their clinical use is hindered by side effects. It is crucial to explore new structural variants of these inhibitors to increase efficacy and minimize side effects, enhancing their clinical viability and therapeutic scope. In this study, we developed a virtual screening workflow that synergistically integrates the capabilities of TransFoxMol, KarmaDock, and AutoDock Vina. This workflow not only streamlines the identification of potential inhibitors but also ensures a systematic approach to prioritizing candidates. Through structural clustering, we identified ten promising PARP-1 inhibitors. Additionally, molecular dynamics simulations and MM/PBSA were employed to elucidate the binding modes of compounds 1, 3, 6, and 9 with PARP-1, providing valuable insights into their interaction mechanisms and supporting future drug development efforts. This workflow serves as a versatile tool for early-stage drug discovery, offering a strategic foundation for the rational design of new PARP-1 inhibitors.

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