1567941-39-2Relevant academic research and scientific papers
Undesired versus designed enzymatic cleavage of linkers for liver targeting
Chirapu, Srinivas R.,Bauman, Jonathan N.,Eng, Heather,Goosen, Theunis C.,Strelevitz, Timothy J.,Sinha, Subhash C.,Dow, Robert L.,Finn
, p. 1144 - 1147 (2014/03/21)
A design for the selective release of drug molecules in the liver was tested, involving the attachment of a representative active agent by an ester linkage to various 2-substituted 5-aminovaleric acid carbamates. The anticipated pathway of carboxylesterase-1-mediated carbamate cleavage followed by lactamization and drug release was frustrated by unexpectedly high sensitivity of the ester linkage toward hydrolysis by carboxylesterase-2 and other microsomal components.
