A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family …
2022年1月5日 · The potential to screen compounds that engage both the HP1 and HP2 pockets simultaneously to increase affinity led us to consider DEL technology for LC3 ligand discovery. …
The autophagy component LC3 regulates lymphocyte adhesion …
2025年2月4日 · Inhibiting Mst1 kinase-mediated LC3 phosphorylation promoted LC3-mediated LFA1 recruitment to the contact surface through direct interaction with RAPL, uncovering an …
Critical assessment of LC3/GABARAP ligands used for degrader
2024年11月25日 · Data based on approximately 1000 crystal structures revealed that most fragments bound to the HP2 but not to the HP1 pocket within the LIR docking site, suggesting …
Solution structure of the autophagy-related protein LC3C reveals a ...
2019年10月2日 · From Ser18 to Ala120, MAP1LC3C forms an α-helix followed by the ubiquitin-like tertiary fold with two hydrophobic binding pockets used by MAP1LC3/GABARAP proteins …
Compounds bind to LC3's HP1 and HP2. Novobiocin and its …
Novobiocin and its derivative dihydronovobiocin show good ligandability with LC3A and LC3B adapter proteins. Fragments 1-1, 2-3 and 2-10 are verified to bind with LC3's HP2. Targeted …
Machine learning approaches for the identification of ligands of …
2023年12月1日 · In the present study, we created a PubChem library of 749 compounds having a structure based on the central scaffold of novobiocin, a reported LC3A ligand. A robust, rapid …
Selective binding of mitophagy receptor protein Bcl-rambo to LC3 ...
2020年9月10日 · Within the interaction, W/F/Y of the LIR motif is located in HP1, while I/L/V is located in HP2. The charged characteristics of HP1 and the hydrophobic grooves of HP2 of …
2023年10月5日 · The data revealed that most fragments bound to the HP2, but not the HP1 pocket of the LC3- interacting region (LIR) docking site, suggesting favorable druggability of …
LC3B: A microtubule-associated protein influences disease …
2025年2月1日 · LC3B, a member of the LC3/GABARAP family, is a ubiquitin-like protein that orchestrates autophagy alongside phosphatidylethanolamine (PE) through a series of E1-E2 …
Structural and functional analysis of the GABARAP interaction …
2017年6月27日 · Structural studies have shown that the side chains of the aromatic residue (Θ) within the core LIR motif are placed deep inside of a hydrophobic pocket (HP1) on the …