Computer-aided synthesis planning (CASP) has garnered increasing attention in light of recent advancements in machine learning models. While the focus is on reverse synthesis or forward outcome prediction, optimizing reaction conditions remains a significant challenge. For datasets with multiple variables, the choice of descriptors and models is pivotal. This selection dictates the effective extraction of conditional features and the achievement of higher prediction accuracy. This review delineates the origins of data in conditional optimization, the criteria for descriptor selection, the response models, and the metrics for outcome evaluation, aiming to acquaint readers with the latest research trends and facilitate more informed research in this domain.
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http://dx.doi.org/10.1002/chem.202401626 | DOI Listing |
J Mol Graph Model
January 2025
Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, 160062, Punjab, India. Electronic address:
Elongation factor G (EF-G) is essential for protein synthesis in Mycobacterium tuberculosis (Mtb), positioning it as a promising target for anti-tubercular drug development. This study employs Structure-Based Drug Design (SBDD) to identify potential small molecule inhibitors that specifically target EF-G. Initially, binding hotspots on EF-G were pinpointed, and the binding modes of various compounds were analyzed.
View Article and Find Full Text PDFCell Commun Signal
January 2025
Chongqing Key Laboratory of Human Embryo Engineering and Precision Medicine, Center for Reproductive Medicine, Women and Children's Hospital of Chongqing Medical University, Chongqing, 400010, China.
Background: Asthenozoospermia (ASZ) accounts for about 20-40% of male infertility, and genetic factors, contributing to 30-40% of the causes of ASZ, still need further exploration. Radial spokes (RSs), a T-shaped macromolecular complex, connect the peripheral doublet microtubules (DMTs) to a central pair (CP), forming a CP-RS-DMT structure to regulate the beat frequency and amplitude of sperm flagella. To date, many components of RSs and their functions in human sperm flagella remain unclear.
View Article and Find Full Text PDFAnal Chem
January 2025
School of Basic Medical Sciences, Guangzhou Νational Laboratory, Guangzhou Medical University, Guangzhou 511436, China.
The farnesoid X receptor (FXR) regulates key physiological processes, such as bile acid homeostasis and lipid metabolism, making it an important target for drug discovery. However, the overactivation of FXR often leads to adverse effects. This study presents the development of a novel fluorescent probe utilizing the computer-aided drug design (CADD) approach to optimize linkers between more potent warhead and FITC fluorescent groups.
View Article and Find Full Text PDFJ Comput Chem
January 2025
Departamento de Fisicoquímica, Facultad de Química, Universidad Nacional Autónoma de México, Coyoacán, CDMX, Mexico.
The G protein-coupled receptor (GPCR) pharmacology accounts for a significant field in research, clinical studies, and therapeutics. Computer-aided drug discovery is an evolving suite of techniques and methodologies that facilitate accelerated progress in drug discovery and repositioning. However, the structure-activity relationships of molecules targeting GPCRs are highly challenging in many cases since slight structural modifications can lead to drastic changes in biological functionality.
View Article and Find Full Text PDFJ Cell Mol Med
January 2025
Department of Botany and Microbiology, College of Science, King Saud University, Riyadh, Saudi Arabia.
This study explores novel therapeutic avenues for diabetes, a global health concern marked by elevated blood glucose levels. We investigated the anti-diabetic potential of Gymnema Sylvestre's bioactive compounds, including Gymnemic acid I, Stigmasterol, Deacylgymnemic acid, Beta-Amyrin acetate, Longispinogenin, Gymnemic acid II, Gymnemic acid, Gymnemic acid X, Gymnemaside VI, Phytic acid and Gymnemic acid X. Employing network pharmacology, molecular docking and molecular dynamics (MD), we elucidated the potential mechanism of action.
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