[HTML][HTML] Computational methods in drug discovery

SP Leelananda, S Lindert - Beilstein journal of organic …, 2016‏ - beilstein-journals.org
The process for drug discovery and development is challenging, time consuming and
expensive. Computer-aided drug discovery (CADD) tools can act as a virtual shortcut …

Role of computer-aided drug design in modern drug discovery

SJY Macalino, V Gosu, S Hong, S Choi - Archives of pharmacal research, 2015‏ - Springer
Drug discovery utilizes chemical biology and computational drug design approaches for the
efficient identification and optimization of lead compounds. Chemical biology is mostly …

Predicting drug metabolism: experiment and/or computation?

J Kirchmair, AH Göller, D Lang, J Kunze… - Nature reviews Drug …, 2015‏ - nature.com
Drug metabolism can produce metabolites with physicochemical and pharmacological
properties that differ substantially from those of the parent drug, and consequently has …

Rigorous free energy simulations in virtual screening

Z Cournia, BK Allen, T Beuming… - Journal of Chemical …, 2020‏ - ACS Publications
Virtual high throughput screening (vHTS) in drug discovery is a powerful approach to identify
hits: when applied successfully, it can be much faster and cheaper than experimental high …

Emerging computational methods for the rational discovery of allosteric drugs

JR Wagner, CT Lee, JD Durrant, RD Malmstrom… - Chemical …, 2016‏ - ACS Publications
Allosteric drug development holds promise for delivering medicines that are more selective
and less toxic than those that target orthosteric sites. To date, the discovery of allosteric …

Using molecular docking and molecular dynamics to investigate protein-ligand interactions

CJ Morris, DD Corte - Modern Physics Letters B, 2021‏ - World Scientific
Molecular docking and molecular dynamics (MD) are powerful tools used to investigate
protein-ligand interactions. Molecular docking programs predict the binding pose and affinity …

Computational prediction of metabolism: sites, products, SAR, P450 enzyme dynamics, and mechanisms

J Kirchmair, MJ Williamson, JD Tyzack… - Journal of chemical …, 2012‏ - ACS Publications
Metabolism of xenobiotics remains a central challenge for the discovery and development of
drugs, cosmetics, nutritional supplements, and agrochemicals. Metabolic transformations …

Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators

DI Balourdas, AM Markl, A Krämer, G Settanni… - Cell Death & …, 2024‏ - nature.com
The cavity-creating p53 cancer mutation Y220C is an ideal paradigm for develo** small-
molecule drugs based on protein stabilization. Here, we have systematically analyzed the …

Rational drug design targeting intrinsically disordered proteins

H Wang, R **ong, L Lai - Wiley Interdisciplinary Reviews …, 2023‏ - Wiley Online Library
Intrinsically disordered proteins (IDPs) are proteins that perform important biological
functions without well‐defined structures under physiological conditions. IDPs can form …

Exploring the role of receptor flexibility in structure-based drug discovery

F Feixas, S Lindert, W Sinko, JA McCammon - Biophysical chemistry, 2014‏ - Elsevier
The proper understanding of biomolecular recognition mechanisms that take place in a drug
target is of paramount importance to improve the efficiency of drug discovery and …