121st General Meeting of the KCS

Type Poster Presentation
Area Organic Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code ORGN.P-440
Subject Development of novel photo-crosslinking probes to investigate protein-protein interactions (PPIs)
Authors Dhiraj Murale, Se-young Jang1, Jun-Seok Lee*
Molecular Recognition Research Center, Korea Institute of Science and Technology, Korea
1Korea Institute of Science and Technology, Korea
Abstract Protein-protein interactions (PPIs) trigger a wide range of biological signaling pathways that are crucial for biomedical research and drug discovery. Various techniques have been used to study specific proteins, including affinity chromatography, activity-based probes, affinity-based probes and photo-affinity labeling (PAL). Photo-affinity labeling (PAL) has been emerged as a powerful strategy in chemical proteomics to study protein-protein interactions (PPIs). Photo-crosslinker generates highly reactive radical species upon photo irradiation, and they lead to generate the direct covalent labeling with the adjacent molecules. Despite of their capability of spatiotemporal engagement controls in live cell condition, the low crosslinking efficiency remains a major critical challenge, especially for those of low abundant proteins which makes it very difficult to study their PPIs. One way to overcome this limitation could be the use of an excess amount of photo-crosslinkers, but it could lead the unintended nonspecific labeling. It has been known these nonspecific interactions are based on hydrophobic and electrostatic interaction effects of biomolecules. Therefore, the more effective strategy to overcome this issue is improving the photo-crosslinking efficiency. To improve the photo-crosslinking efficiency we have been extensively studying wide range of the PAL agents based on BODIPY so called photo-crosslinking BODIPY fluorophore (pcBD). Traditionally, photo-crosslinking chemical probes are designed based on three functional groups namely benzophenone, diazirine and aryl azide. We decided to compare all these three functional groups and incorporated them onto BODIPY core by simple chemical modifications for their photo-crosslinking efficiencies.
E-mail dhiraj.murale@gmail.com