| Title : Undesired versus designed enzymatic cleavage of linkers for liver targeting - Chirapu_2014_Bioorg.Med.Chem.Lett_24_1144 |
| Author(s) : Chirapu SR , Bauman JN , Eng H , Goosen TC , Strelevitz TJ , Sinha SC , Dow RL , Finn MG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 24 :1144 , 2014 |
|
Abstract :
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. |
| PubMedSearch : Chirapu_2014_Bioorg.Med.Chem.Lett_24_1144 |
| PubMedID: 24461291 |
Chirapu SR, Bauman JN, Eng H, Goosen TC, Strelevitz TJ, Sinha SC, Dow RL, Finn MG (2014)
Undesired versus designed enzymatic cleavage of linkers for liver targeting
Bioorganic & Medicinal Chemistry Lett
24 :1144
Chirapu SR, Bauman JN, Eng H, Goosen TC, Strelevitz TJ, Sinha SC, Dow RL, Finn MG (2014)
Bioorganic & Medicinal Chemistry Lett
24 :1144