P-glycoprotein Inhibition for Optimal Drug Delivery
By Md Lutful Amin. Drug Target Insights, 2013
600 citations recorded by the source corpus.
P-glycoprotein (P-gp), an efflux membrane transporter, is widely distributed throughout the body and is responsible for limiting cellular uptake and the distribution of xenobiotics and toxic substances. Hundreds of structurally diverse therapeutic agents are substrates to it and it impedes the absorption, permeability, and retention of the drugs, extruding them out of the cells. It is overexpressed in cancer cells and accountable for obstructing cell internalization of chemotherapeutic agents and for developing transporter mediated resistance by cancer cells during anti-tumor treatments. As it jeopardizes the success of drug delivery and cancer targeting, strategies are being developed to overcome P-gp mediated drug transport. This concise review represents a brief discussion on P-gp mediated drug transport and how it hinders the success of various therapies. Its main focus is on various strategies used to tackle this curb in the field of drug delivery and targeting.
Subfields: Biomaterials, Oncology, Pediatrics, Perinatology and Child Health
View Paper: https://www.semanticscholar.org/paper/3d2c88081c5ca5d2a0d8573d62a6a0d40d011d43
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In Biomaterials
In Oncology
In Pediatrics, Perinatology and Child Health
Citations in the corpus
- Getting Across the Cell Membrane: An Overview for Small Molecules, Peptides, and Proteins (2015, background): “A variety of structurally unrelated compounds, including small-molecule drugs, are substrates of efflux pumps in the ATP-binding cassette (ABC) transporter family such as the multidrug resistance protein (MRP) family [65], the P-glycoprotein pump (P-gp, also known as multidrug resistance protein 1(M”
- Therapeutics Data Commons: Machine Learning Datasets and Tasks for Drug Discovery and Development (2021, background): “TDC.Pgp_Broccatelli: P-glycoprotein (Pgp) is an ABC transporter protein involved in intestinal absorption, drug metabolism, and brain penetration, and its inhibition can seriously alter a drug’s bioavailability and safety (Amin 2013).”