AlphaFold2 protein structure prediction: Implications for drug discovery

N Borkakoti, JM Thornton - Current opinion in structural biology, 2023 - Elsevier
The drug discovery process involves designing compounds to selectively interact with their
targets. The majority of therapeutic targets for low molecular weight (small molecule) drugs …

[HTML][HTML] A guide to in silico drug design

Y Chang, BA Hawkins, JJ Du, PW Groundwater… - Pharmaceutics, 2023 - mdpi.com
The drug discovery process is a rocky path that is full of challenges, with the result that very
few candidates progress from hit compound to a commercially available product, often due …

Epik: pKa and Protonation State Prediction through Machine Learning

RC Johnston, K Yao, Z Kaplan, M Chelliah… - Journal of chemical …, 2023 - ACS Publications
Epik version 7 is a software program that uses machine learning for predicting the p K a
values and protonation state distribution of complex, druglike molecules. Using an ensemble …

Alchemical Transformations and Beyond: Recent Advances and Real-World Applications of Free Energy Calculations in Drug Discovery

R Qian, J Xue, Y Xu, J Huang - Journal of Chemical Information …, 2024 - ACS Publications
Computational methods constitute efficient strategies for screening and optimizing potential
drug molecules. A critical factor in this process is the binding affinity between candidate …

Using AlphaFold and experimental structures for the prediction of the structure and binding affinities of GPCR complexes via induced fit docking and free energy …

D Coskun, M Lihan, JP Rodrigues, M Vass… - Journal of Chemical …, 2023 - ACS Publications
Free energy perturbation (FEP) remains an indispensable method for computationally
assaying prospective compounds in advance of synthesis. However, before FEP can be …

Rational and translational implications of D-amino acids for treatment-resistant schizophrenia: from neurobiology to the clinics

A de Bartolomeis, L Vellucci, MC Austin, G De Simone… - Biomolecules, 2022 - mdpi.com
Schizophrenia has been conceptualized as a neurodevelopmental disorder with synaptic
alterations and aberrant cortical–subcortical connections. Antipsychotics are the mainstay of …

[HTML][HTML] Quantum chemical package Jaguar: A survey of recent developments and unique features

Y Cao, T Balduf, MD Beachy, MC Bennett… - The Journal of …, 2024 - pubs.aip.org
This paper is dedicated to the quantum chemical package Jaguar, which is commercial
software developed and distributed by Schrödinger, Inc. We discuss Jaguar's scientific …

Chiral-Controlled Cyclic Chemiluminescence Reactions for the Analysis of Enantiomer Amino Acids

Y Zhong, Y Chen, L Chen, Y Hu, X **ao… - Analytical …, 2023 - ACS Publications
The similarity and complexity of chiral amino acids (AAs) in complex samples remain a
significant challenge in their analysis. In this work, the chiral metal–organic framework …

FEP Protocol Builder: Optimization of Free Energy Perturbation Protocols Using Active Learning

C de Oliveira, K Leswing, S Feng… - Journal of Chemical …, 2023 - ACS Publications
Significant improvements have been made in the past decade to methods that rapidly and
accurately predict binding affinity through free energy perturbation (FEP) calculations. This …

A Computational Physics-based Approach to Predict Unbound Brain-to-Plasma Partition Coefficient, Kp,uu

M Lawrenz, M Svensson, M Kato… - Journal of Chemical …, 2023 - ACS Publications
The blood–brain barrier (BBB) plays a critical role in preventing harmful endogenous and
exogenous substances from penetrating the brain. Optimal brain penetration of small …