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We report the results of our participation in the SAMPL8 GDCC Blind Challenge for host-guest binding affinity predictions. Absolute binding affinity prediction is of central importance to the biophysics of molecular association and…

Chemical Physics · Physics 2022-02-09 Solmaz Azimi , Joe Z. Wu , Sheenam Khuttan , Tom Kurtzman , Nanjie Deng , Emilio Gallicchio

We present our blind predictions for the Statistical Assessment of the Modeling of Proteins and Ligands (SAMPL), 9th challenge, focusing on binding of WP6 (carboxy-pillar[6]arene) with ammonium/diammonium cationic guests. Host-guest binding…

Chemical Physics · Physics 2022-05-11 Piero Procacci , Guido Guarnieri

The Alchemical Transfer Method (ATM) for the calculation of standard binding free energies of non-covalent molecular complexes is presented. The method is based on a coordinate displacement perturbation of the ligand between the receptor…

Chemical Physics · Physics 2021-01-21 Joe Z. Wu , Solmaz Azimi , Sheenam Khuttan , Nanjie Deng , Emilio Gallicchio

The Alchemical Transfer Method (ATM) is herein validated against the relative binding free energies of a diverse set of protein-ligand complexes. We employed a streamlined setup workflow, a bespoke force field, and the AToM-OpenMM software…

Chemical Physics · Physics 2023-08-21 Lieyang Chen , Yujie Wu , Chuanjie Wu , Ana Silveira , Woody Sherman , Huafeng Xu , Emilio Gallicchio

The accurate prediction of protein-ligand binding affinities is crucial for drug discovery. Alchemical free energy calculations have become a popular tool for this purpose. However, the accuracy and reliability of these methods can vary…

We present receptor hopping and receptor swapping free energy estimation protocols based on the Alchemical Transfer Method (ATM) to model the binding selectivity of a set of ligands to two arbitrary receptors. The receptor hopping protocol,…

Chemical Physics · Physics 2024-08-28 Solmaz Azimi , Emilio Gallicchio

We present an analytical description of the Alchemical Transfer Method (ATM) for molecular binding using the Potential Distribution Theory (PDT) formalism. ATM models the binding free energy by mapping the bound and unbound states of the…

Chemical Physics · Physics 2024-10-15 Solmaz Azimi , Emilio Gallicchio

We present an extension of Alchemical Transfer Method (ATM) for the estimation of relative binding free energies of molecular complexes applicable to conventional as well as scaffold-hopping alchemical transformations. The method, named…

Chemical Physics · Physics 2021-07-13 Solmaz Azimi , Sheenam Khuttan , Joe Z. Wu , Rajat K. Pal , Emilio Gallicchio

Predicting non-covalent host-guest recognition remains challenging due to the complex interplay of electrostatics, dispersion, and steric effects, and the limited transferability of existing docking approaches to synthetic supramolecular…

Chemical Physics · Physics 2026-01-21 Zidi Wang , Tao Zhang , Muyao Yu , Chuyi Zhou , Zezhao Xu , Huiyu Liu , Yuzhen Wen , Linjiang Chen , Jie Zheng , Shan Jiang

We present a parameterized analytical model of alchemical molecular binding. The model describes accurately the free energy profiles of linear single-decoupling alchemical binding free energy calculations. The parameters of the model, which…

Biomolecules · Quantitative Biology 2017-07-06 Emilio Gallicchio

Accurate prediction of binding free energies is critical to streamlining the drug development and protein design process. With the advent of GPU acceleration, absolute alchemical methods, which simulate the removal of ligand electrostatics…

Biological Physics · Physics 2021-03-17 Edward King , Ruxi Qi , Han Li , Ray Luo , Erick Aitchison

A rigorous formalism for estimating noncovalent binding free energies and thermodynamic expectations from calculations in which receptor configurations are sampled independently from the ligand is derived. Due to this separation, receptor…

Statistical Mechanics · Physics 2015-03-20 David D. L. Minh

We present a new method that combines alchemical transformation with physical pathway to accurately and efficiently compute the absolute binding free energy of receptor-ligand complex. Currently, the double decoupling method (DDM) and the…

Biomolecules · Quantitative Biology 2018-08-29 Nanjie Deng , Lauren Wickstrom , Emilio Gallicchio

We investigate the role of order/disorder transitions in alchemical simulations of protein-ligand absolute binding free energies. We show, in the context of a potential of mean force description, that for a benchmarking system (the complex…

Biomolecules · Quantitative Biology 2019-10-23 Rajat Kumar Pal , Emilio Gallicchio

We present the Alchemical Transfer with Coordinate Swapping (ATS) method to enable the calculation of the relative binding free energies between large congeneric ligands and single-point mutant peptides to protein receptors with the…

Chemical Physics · Physics 2024-12-31 Emilio Gallicchio

The theory of receptor-ligand binding equilibria has long been well-established in biochemistry, and was primarily constructed to describe dilute aqueous solutions. Accordingly, few computational approaches have been developed for making…

Quantitative Methods · Quantitative Biology 2018-10-02 Reza Salari , Thomas Joseph , Ruchi Lohia , Jerome Henin , Grace Brannigan

N6-methyladenosine (m6A) is a prevalent RNA post-transcriptional modification that plays crucial roles in RNA stability, structural dynamics, and interactions with proteins. The YT521-B (YTH) family of proteins, which are notable m6A…

Biomolecules · Quantitative Biology 2024-09-10 Valerio Piomponi , Miroslav Krepl , Jiri Sponer , Giovanni Bussi

Absolute Binding Free Energy (ABFE) methods are among the most accurate computational techniques for predicting protein-ligand binding affinities, but their utility is limited by the need for many simulations of alchemically modified…

Quantitative Methods · Quantitative Biology 2026-03-18 Michael Brocidiacono , Brandon Novy , Rishabh Dey , Konstantin I. Popov , Alexander Tropsha

Predicting the binding free energy between antibodies and antigens is a key challenge in structure-aware biomolecular modeling, with direct implications for antibody design. Most existing methods either rely solely on sequence embeddings or…

Biomolecules · Quantitative Biology 2025-08-28 Ciyuan Yu , Hongzong Li , Jiahao Ma , Shiqin Tang , Ye-Fan Hu , Jian-Dong Huang

Alchemical binding free energy (BFE) calculations offer an efficient and thermodynamically rigorous approach to in silico binding affinity predictions. As a result of decades of methodological improvements and recent advances in computer…

Statistical Mechanics · Physics 2021-07-13 Pengfei Li , Zhijie Li , Yu Wang , Huaixia Dou , Brian K. Radak , Woody Sherman , Huafeng Xu
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