Professor Serge Mignani will be at the Madeira Chemistry Research Centre (CQM) next June 2024. He will be the invited lecturer of the Seminar "Innovative tools for prospecting target ligand bioactive molecules: Affinity selection mass spectrometry (AS-MS) and Hydrogen-Deuterium Exchange Mass Spectrometry (HDX-MS). From a medicinal chemistry point of view", to be held at the University of Madeira, 19th June, 15h00 (conference room 0.57). Registration to attend the seminar is required (link below).
ABSTRACT
Affinity selection mass spectrometry (AS-MS) is a powerful tool for identifying bioactive molecules from chemically diverse sources such as botanical, fungal, and microbial extracts. Based on binding interactions between macromolecular receptors and ligands of low molecular mass, AS-MS enables the rapid isolation of pharmacologically active small molecules from complex mixtures for mass spectrometric characterization and identification. The selection provided by the formation of the target-ligand complex allows identifying hits irrespective of their functional effect. Unlike most conventional high-throughput screening assays, AS-MS has fewer or no limitations regarding target selection. The AS-MS technologies mainly used with protein targets in solution are size exclusion chromatography (SEC) and pulsed ultrafiltration (PUF). Consequently, AS-MS is a high throughput screening (HTS) technique for identifying small molecule test compounds based on their binding affinity to a target.
Hydrogen deuterium exchange mass spectrometry (HDX-MS) is becoming part of molecular biologists' standard repertoire of techniques to investigate protein structure and dynamics. The increasing use of HDX-MS can be attributed to the broad range of proteins, that are suited to the technique, and its relatively low technical and theoretical barriers. One key aspect of the renaissance of HDX-MS is its ability to provide structural information on many challenging targets for drug discovery that represent a step-change in ambition from the well-ordered easily crystallizable small proteins that readily provided insight into structural–activity relationships between proteins and ligands.
The aim of this presentation, with a user's eye, is not to explain in detail the techniques of Affinity selection mass spectrometry (AS-MS) and Hydrogen-Deuterium Exchange Mass Spectrometry (HDX-MS) but to show their strong interest in such techniques for the discovery of new hits from vast synthetic and/or natural libraries that contain accessible complexity, and providing access to previously uncharted molecular space.
Professor Serge Mignani, from the Centre d’Etudes et de Recherche sur le Médicament de Normandie (UNICAEN, CERMN) and the Argobio Studio (France) was, for more than 40 years, researcher in one of the biggest pharmaceutical industries, Rhône-Poulenc, currently named Sanofi, where he served as director of the Medical Chemistry Department. He is now a consultant for several big and medium pharmaceutical industries (France and USA) and Institutes (France, China, Portugal, and India). He collaborates with the University of Madeira since 2013 and is officially a CQM researcher since 2017, being responsible for the Medicinal Chemistry area and nanomedicine translation activities.
ABSTRACT
Affinity selection mass spectrometry (AS-MS) is a powerful tool for identifying bioactive molecules from chemically diverse sources such as botanical, fungal, and microbial extracts. Based on binding interactions between macromolecular receptors and ligands of low molecular mass, AS-MS enables the rapid isolation of pharmacologically active small molecules from complex mixtures for mass spectrometric characterization and identification. The selection provided by the formation of the target-ligand complex allows identifying hits irrespective of their functional effect. Unlike most conventional high-throughput screening assays, AS-MS has fewer or no limitations regarding target selection. The AS-MS technologies mainly used with protein targets in solution are size exclusion chromatography (SEC) and pulsed ultrafiltration (PUF). Consequently, AS-MS is a high throughput screening (HTS) technique for identifying small molecule test compounds based on their binding affinity to a target.
Hydrogen deuterium exchange mass spectrometry (HDX-MS) is becoming part of molecular biologists' standard repertoire of techniques to investigate protein structure and dynamics. The increasing use of HDX-MS can be attributed to the broad range of proteins, that are suited to the technique, and its relatively low technical and theoretical barriers. One key aspect of the renaissance of HDX-MS is its ability to provide structural information on many challenging targets for drug discovery that represent a step-change in ambition from the well-ordered easily crystallizable small proteins that readily provided insight into structural–activity relationships between proteins and ligands.
The aim of this presentation, with a user's eye, is not to explain in detail the techniques of Affinity selection mass spectrometry (AS-MS) and Hydrogen-Deuterium Exchange Mass Spectrometry (HDX-MS) but to show their strong interest in such techniques for the discovery of new hits from vast synthetic and/or natural libraries that contain accessible complexity, and providing access to previously uncharted molecular space.
Professor Serge Mignani, from the Centre d’Etudes et de Recherche sur le Médicament de Normandie (UNICAEN, CERMN) and the Argobio Studio (France) was, for more than 40 years, researcher in one of the biggest pharmaceutical industries, Rhône-Poulenc, currently named Sanofi, where he served as director of the Medical Chemistry Department. He is now a consultant for several big and medium pharmaceutical industries (France and USA) and Institutes (France, China, Portugal, and India). He collaborates with the University of Madeira since 2013 and is officially a CQM researcher since 2017, being responsible for the Medicinal Chemistry area and nanomedicine translation activities.
GENERAL INFORMATION
Date: 19 June 2024
Schedule: 15h00-16h30 (PT, Lisbon time)
Venue: University of Madeira, Campus of Penteada, Conference Room 0.57.
Fee: Free admittance.
Date: 19 June 2024
Schedule: 15h00-16h30 (PT, Lisbon time)
Venue: University of Madeira, Campus of Penteada, Conference Room 0.57.
Fee: Free admittance.
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Registration until 18 June 2024. |
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Registration form (CLOSED!) - limited seats available |