Synthesis of Non-Steroidal Estrogen Receptor Proteolysis Targeting Chimeric Molecules (Protacs)
type: CreativeWork
description: To make the PROTAC design more useful, a small molecule E3 ligase peptide mimic is desirable. The HIF-1alpha E3 ligase destruction sequence utilized in the PROTAC design requires a hydroxylated proline residue for recognition by the VCB E3 ligase. The synthesis of a tetrahydrofuran-based hydroxyproline analog was attempted with encouraging results. Upon completion of the synthesis, this analog can be attached to an ER ligand in place of the HIF-1alpha destruction sequence and tested as the first non-peptide based PROTAC.
abstract: To make the PROTAC design more useful, a small molecule E3 ligase peptide mimic is desirable. The HIF-1alpha E3 ligase destruction sequence utilized in the PROTAC design requires a hydroxylated proline residue for recognition by the VCB E3 ligase. The synthesis of a tetrahydrofuran-based hydroxyproline analog was attempted with encouraging results. Upon completion of the synthesis, this analog can be attached to an ER ligand in place of the HIF-1alpha destruction sequence and tested as the first non-peptide based PROTAC.
author: Mann, Meagan K.
language: eng
keywords: Chemistry, Biochemistry
date published: 2015-09-25T22:13:55Z
date modified: 2026-07-22T22:26:23Z
provider: University of Illinois - Urbana-Champaign
publisher: Networked Digital Library of Theses and Dissertations
type: WebPage
source organization: University of Illinois at Urbana-Champaign

PropertyValue
property ID: Handle
value: http://hdl.handle.net/2142/84317