Article
Mutational analysis reveals the importance of residues of the access tunnel inhibitor site to human P-glycoprotein (ABCB1)-mediated transport.
Protein science : a publication of the Protein Society - 1 Sept 2024
Salazar Paula B, Murakami Megumi, Ranganathan Nandhini, Durell Stewart R, Ambudkar Suresh V
Abstract excerpt
Human P-glycoprotein (P-gp) utilizes energy from ATP hydrolysis for the efflux of chemically dissimilar amphipathic small molecules and plays an important role in the development of resistance to chemotherapeutic agents in most cancers. Efforts to overcome drug resistance have focused on inhibiting P-gp-mediated drug efflux. Understanding the features distinguishing P-gp inhibitors from substrates is critical....
Topics
- Humans
- ATP Binding Cassette Transporter, Subfamily B
- Binding Sites
- Quinolines
- Mutation
- Models, Molecular