Drug uptake discovery could allow IV medications to be taken orally

A team of scientists has uncovered the mechanism of cellular uptake for large and polar drugs and devised a novel strategy to optimize the capacity of drug-delivery into these cells. The team was led by Hong-yu Li, Ph.D., professor of medicinal chemistry and chemical biology with the Department of Pharmacology and the Barshop Institute at the University of Texas Health Science Center at San Antonio (UT Health San Antonio), together with teams from Duke University (Duke) and the University of Arkansas for Medical Sciences (UAMS)

Published in Cell, the study creates a strategy called chemical endocytic medicinal chemistry that may revolutionize how endocytic drugs in the future are designed and developed.

“Chemical endocytic medicinal chemistry has the potential to impact every aspect of endocytic drugs from drug discovery and development to clinical practice,” said Li.

In this novel process, drug molecules are designed to better engage with CD36, a protein receptor found on the surface of many cells. By optimizing chemical interactions with CD36, the team was able to enhance the natural function of CD36, essentially increasing the gateway for larger and polar drug compounds to enter the cell.

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