Improving small molecule virtual screening strategies for the next generation of therapeutics

BM Wingert, CJ Camacho - Current opinion in chemical biology, 2018 - Elsevier
The new generation of post-genomic targets, such as protein–protein interactions (PPIs),
often require new chemotypes not well represented in current compound libraries. This is …

Absolute binding free energy calculations improve enrichment of actives in virtual compound screening

M Feng, G Heinzelmann, MK Gilson - Scientific Reports, 2022 - nature.com
We determined the effectiveness of absolute binding free energy (ABFE) calculations to
refine the selection of active compounds in virtual compound screening, a setting where the …

[HTML][HTML] Current advances in studying clinically relevant transporters of the solute carrier (SLC) family by connecting computational modeling and data science

A Türková, B Zdrazil - Computational and structural biotechnology journal, 2019 - Elsevier
Organic anion and cation transporting proteins (OATs, OATPs, and OCTs), as well as the
Multidrug and Toxin Extrusion (MATE) transporters of the Solute Carrier (SLC) family are …

Meta-analysis reveals that absolute binding free-energy calculations approach chemical accuracy

H Fu, Y Zhou, X Jing, X Shao, W Cai - Journal of Medicinal …, 2022 - ACS Publications
Systematic and quantitative analysis of the reliability of formally exact methods that in silico
calculate absolute protein–ligand binding free energies remains lacking. Here, we provide …

Taming multiple binding poses in alchemical binding free energy prediction: the β-cyclodextrin host–guest SAMPL9 blinded challenge

S Khuttan, S Azimi, JZ Wu, S Dick, C Wu… - Physical Chemistry …, 2023 - pubs.rsc.org
We apply the Alchemical Transfer Method (ATM) and a bespoke fixed partial charge force
field to the SAMPL9 bCD host–guest binding free energy prediction challenge that …

Resolving the ligand-binding specificity in c-MYC G-quadruplex DNA: absolute binding free energy calculations and SPR experiment

N Deng, L Wickstrom, P Cieplak, C Lin… - The Journal of Physical …, 2017 - ACS Publications
We report the absolute binding free energy calculation and surface plasmon resonance
(SPR) experiment for ligand binding with the c-MYC G-quadruplex DNA. The unimolecular …

Potts Hamiltonian Models and Molecular Dynamics Free Energy Simulations for Predicting the Impact of Mutations on Protein Kinase Stability

A Thakur, J Gizzio, RM Levy - The Journal of Physical Chemistry …, 2024 - ACS Publications
Single-point mutations in kinase proteins can affect their stability and fitness, and
computational analysis of these effects can provide insights into the relationships among …

Hybrid receptor structure/ligand-based docking and activity prediction in ICM: development and evaluation in D3R Grand Challenge 3

PCH Lam, R Abagyan, M Totrov - Journal of computer-aided molecular …, 2019 - Springer
In context of D3R Grand Challenge 3 we have investigated several ligand activity prediction
protocols that combined elements of a physics-based energy function (ICM VLS score) and …

Docking of small molecules to farnesoid X receptors using AutoDock Vina with the Convex-PL potential: lessons learned from D3R Grand Challenge 2

M Kadukova, S Grudinin - Journal of computer-aided molecular design, 2018 - Springer
Abstract The 2016 D3R Grand Challenge 2 provided an opportunity to test multiple protein–
ligand docking protocols on a set of ligands bound to farnesoid X receptor that has many …

Structure-based virtual screening workflow to identify antivirals targeting HIV-1 capsid

Q Sun, A Biswas, RSK Vijayan, P Craveur… - Journal of Computer …, 2022 - Springer
We have identified novel HIV-1 capsid inhibitors targeting the PF74 binding site. Acting as
the building block of the HIV-1 capsid core, the HIV-1 capsid protein plays an important role …