PEGylation would not work on smallmolecule drugs 500 Da beca

PEGylation would not work on small-molecule drugs (~500 Da) because: (SELECT ALL THAT APPLY)

A- PEG cannot be attached to small molecules

B- The PEG moiety would sterically hinder the small molecule\'s activity [the polyethylene glycol (PEG)} chain is likely significantly bigger than the pharmacophore

C- The PEG moiety would cause rapid excretion of the drug

D- PEGylation would make the drug insoluble

Solution

PEGlyation is the process of attachment of PEG polymer chains to molecules and macrostructures like drugs or therapeutic proteins. PEG is water soluble, non-toxic, and is currently an integral part of seven approved macromolecular drugs. However, PEGlyation of small molecule drugs has encountered a few problems. While attachment to the small molecule is possible, there are only few sites that PEG can attach to without harming functionality of the drug. Bioavailability and water solubility of the drug may be unchanged, but attachment of PEG to the molecule could cause steric hindrance, which would in turn affect target binding of the molecule.

Thus, the correct answer is: B) The PEG moeity would sterically hinder the small molecule\'s activity [the polyethylene glycol(PEG) chain is likely significantly bigger than the pharmacophore]