Structure-based discovery of new chemical scaffolds acting as p38α MAPK inhibitors

webinar

Wed, 01 Mar 2017, 16:00 CET (Berlin)

Andrea Astolfi, Uni Perugia, Italy

Structure-based discovery of new chemical scaffolds acting as p38α MAPK inhibitors

p38α mitogen-activated protein kinase (MAPK) is an important molecular switch involved in the regulation of many pathways, such as pro-inflammatory signaling networks and cytokines biosynthesis. A large number of small molecules inhibiting p38α MAPK are described in literature; however, as no FDA drugs against this protein are present in the market, the identification of new p38α MAPK inhibitors is still a research field of tremendous interest.

Different types of p38α MAPK inhibitors are known, having different binding mode and/or mode of action. During the challenge Andrea Astolfi has focused his attention on the competitive Type-I (TI) and Type-I½ (TI½) inhibitors.

BioSolveIT software was used with the aim to identify novel p38α MAPK inhibitors. In particular, the integration of different BioSolveIT tools with the KNIME® platform enabled the group to build ad-hoc workflows to automate and accelerate the drug discovery process.

Current news

category
Publications
New Publication: Strategies for Identifying Molecules of Interest in Large Chemical Spaces
July 14, 2026 11:25 CEST
In collaboration with Pfizer, our team recently published a study in the Journal of Chemical Information and Modeling. The work represents fundamental research into molecular similarity, extended to ultra-large, combinatorial Chemical Spaces. Read the Full Publication (Open Access) Which Central Questions Were Addressed? Which similarity-score thresholds are meaningful? How do...
Read on
category
Challenge
Dylan Capitti Fenton Wins Scientific Challenge Summer 2025!
July 13, 2026 11:50 CEST
It is our greatest pleasure to announce the winner of the Summer 2025 edition of the Scientific Challenge: the winner is Dylan Capitti Fenton of California State University, Northridge (Van Nuys, United States) with his project ‘Structure-Based Drug Discovery of Bitter Taste Receptor Agonists for GLP-1 Release’. Focusing on the...
Read on
Tool of the Month - FlexS
June 30, 2026 10:59 CEST
This Summer, You Wear Molecule Alignment This July, see Similarity in 3D with FlexS as BioSolveIT’s Tool of the Month. In ligand-based drug discovery, the most interesting molecules are not always the ones that look similar on paper. Sometimes, the true connection only becomes visible in 3D. FlexS helps uncover...
Read on