Jörg Hüser studied Biology at the Ruhr-University in Bochum, Germany. He received a PhD in Physiology working on excitation-contraction coupling in cardiac muscle cells. Following a postdoctural training at Loyola University in Chicago, Stritch School of Medicine, in Maywood, IL, USA, he joined Bayer AG’s Pharma Research in Wuppertal, Germany. During his almost 25 year tenure at Bayer, he held different management positions, leading research units in Lead Discovery and Heart & Vascular Disease Research. In June 2023 he joined Axxam as Chief Scientific Officer.
Protein – Protein Interactions:
Not so intractable after all
Cell function depends on a multitude of dynamic protein-protein interactions (PPIs) organized in complex networks and intricately orchestrated in time and space. In turn, dysregulation of specific PPIs is known to cause or contribute to disease, rendering PPIs important targets for drug intervention. The perception on targeting intracellular PPIs with small molecules has witnessed remarkable changes over the last two decades. Considered “undruggable” for a long time, success stories derived, for example, from covalent binders and new molecular mode of actions, like targeted protein degradation, have resulted in a renaissance of PPIs in discovery project portfolios. Today, a large spectrum of different assay techniques is available to probe small molecule modulation of PPIs.
In our webinar, we will focus on the particular strength of cell-free, biochemical assays in dissecting molecular recognition events to enhance assay resolution identifying also weakly interfering compounds. Finally, we briefly discuss how this process can be supported by computational methodologies in the future.
Interaction assays; High-throughput screening; Hit validation; TR-FRET; Fluorescence polarization; Generative Machine Learning; Virtual Screening; Virtual High-Throughput Screening; Library Design.
Jörg Hüser, CSO, Axxam
Daniele Carettoni, Head of Biochemistry, Axxam
Davide Sala, Computational chemist, Axxam
Daniele Carettoni has been Head of Biochemistry at Axxam since its foundation in 2001, leading the efforts for recombinant protein production and development of functional assays to support high-throughput screening campaigns on diverse enzyme targets and proximity assays. Previously, he was a research scientist at Bayer, working at the configuration of uHTS enzymatic assays, and at GlaxoWellcome, where he was involved in a collaborative project aimed at the characterization and validation of novel anti-infective targets. Daniele Carettoni did his post-doctoral training in Italian national pharmaceutical companies, working mainly on expression and functional characterization of recombinant proteins, and received his Ph.D. in Molecular and Cellular Biology from University of Milan, studying DNA-processing enzymes.
Davide Sala is a computational chemist and structural biologist focusing on virtual high-throughput screening and design of small-molecules libraries with machine-learning approaches. Davide obtained a Master’s Degree (MSc) in Bioinformatics at the university of Milano-Bicocca and a PhD in Structural Biology from the Center of Magnetic Resonance (CERM) in Florence. After three years as a Post-Doctoral Researcher at the Institute for Drug Discovery in Leipzig (DE), he moved to Axxam in 2023.