Identifying new compounds that interact with a target is a crucial time-limiting step in the initial phases of drug discovery. Compound-protein complex structure-based affinity prediction models can expedite this process; however, their dependence on high-quality three-dimensional (3D) complex structures limits their practical application. Prediction models that do not require 3D complex structures for binding-affinity estimation offer a theoretically attractive alternative; however, accurately predicting affinity without interaction information presents significant challenges. We introduce BlendNet, a framework that employs a knowledge transfer strategy to improve affinity prediction accuracy by learning the interdependent relationships between compounds and proteins without relying on 3D complex structures. Compared with state-of-the-art models for affinity prediction, BlendNet demonstrated superior performance across various cold-start cases. The ability of BlendNet to interpret compound-protein interactions without utilizing complex structure data highlights its potential to accelerate and streamline drug development.
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http://dx.doi.org/10.1093/bib/bbae712 | DOI Listing |
J Chem Theory Comput
January 2025
Laboratory of Medicinal Chemistry, Rega Institute for Medicinal Research, Herestraat 49, Box 1030, Leuven B-3000, Belgium.
Synthetic nucleic acids, also defined as xenobiotic nucleic acids (XNAs), opened an avenue to address the limitations of nucleic acid therapeutics and the development of alternative carriers for genetic information in biotechnological applications. Two related XNA systems of high interest are the α-l-threose nucleic acid (TNA) and (3'-2') phosphonomethyl threosyl nucleic acid (tPhoNA), where TNAs show potential in antisense applications, whereas tPhoNAs are investigated for their predisposition toward orthogonal genetic systems. We present predictions on helical models of TNA and tPhoNA chemistry in homoduplexes and in complex with native ribose chemistries.
View Article and Find Full Text PDFJ Chem Theory Comput
January 2025
College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Computer-aided drug discovery (CADD) utilizes computational methods to accelerate the identification and optimization of potential drug candidates. Free energy perturbation (FEP) and thermodynamic integration (TI) play a critical role in predicting differences in protein binding affinities between drug molecules. Here, we implement SPONGE-FEP, which incorporates selective integrated tempering sampling (SITS) to enhance sampling efficiency and contains an automated workflow for relative binding free energy (RBFE) calculations.
View Article and Find Full Text PDFWe introduce Hydrogen-Exchange Experimental Structure Prediction (HX-ESP), a method that integrates hydrogen exchange (HX) data with molecular dynamics (MD) simulations to accurately predict ligand binding modes, even for targets requiring significant conformational changes. Benchmarking HX-ESP by fitting two ligands to PAK1 and four ligands to MAP4K1 (HPK1), and comparing the results to X-ray crystallography structures, demonstrated that HX-ESP successfully identified binding modes across a range of affinities significantly outperforming flexible docking for ligands necessitating large conformational adjustments. By objectively guiding simulations with experimental HX data, HX-ESP overcomes the long timescales required for binding predictions using traditional MD.
View Article and Find Full Text PDFFront Immunol
January 2025
Department of Neuro-oncology, Cancer Center, Beijing Tiantan Hospital, Capital Medical University, Beijing, China.
Introduction: Glioma is the most common primary malignant brain tumor. Despite advances in surgical techniques and treatment regimens, the therapeutic effects of glioma remain unsatisfactory. Immunotherapy has brought new hope to glioma patients, but its therapeutic outcomes are limited by the immunosuppressive nature of the tumor microenvironment (TME).
View Article and Find Full Text PDFRSC Adv
January 2025
LAQV and REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa Caparica Portugal
Despite significant strides in improving cancer survival rates, the global cancer burden remains substantial, with an anticipated rise in new cases. Immune checkpoints, key regulators of immune responses, play a crucial role in cancer evasion mechanisms. The discovery of immune checkpoint inhibitors (ICIs) targeting PD-1/PD-L1 has revolutionized cancer treatment, with monoclonal antibodies (mAbs) becoming widely prescribed.
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