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

What's So Special About The 'Activity Spotter'? Detailed Insights Into SeeSAR's New Mode
April 29, 2026 10:22 CEST
SeeSAR’s Activity Spotter Mode is designed to dismantle the barrier of raw data and actionable SAR. It helps to answer the most relevant fields in hit-to-lead and lead optimization campaigns: 3D SAR and pharmacophore modeling. Which structural features in my molecule set are associated with activity? Which ones are linked...
Read on
Tool of the Month - FlexX
April 29, 2026 08:53 CEST
Spring is Molecular Docking Season The bread and butter of computational chemistry: predicting potential binding modes, which serves as a crucial foundation for SAR analysis and design decisions, is being made available to everyone this month with the proprietary docking tool FlexX. Validated by over 10,000 citations of its original...
Read on
The 95 Billion Update: Access the REAL Space
April 9, 2026 13:57 CEST
The latest update of Enamine’s REAL Space brings a new expansion, now featuring over 94.5 billion accessible, drug-like products, approaching the 100 billion mark. Built from 173 curated reaction protocols and 202,620 in-stock reagents and building blocks based on Enamine’s in-house knowledge, this version further enhances the world’s largest commercially...
Read on