1.
Acta Pharmaceutica Sinica B
;
(6): 1315-1328, 2021.
Article
in English
| WPRIM
| ID: wpr-881201
ABSTRACT
Bcr-Abl threonine 315 to isoleucine 315 (T315I) gatekeeper mutation induced drug resistance remains an unmet clinical challenge for the treatment of chronic myeloid leukemia (CML). Chemical degradation of Bcr-Abl
2.
Acta Pharmaceutica Sinica B
;
(6): 1300-1314, 2021.
Article
in English
| WPRIM
| ID: wpr-881200
ABSTRACT
HMG-CoA reductase (HMGCR) protein is usually upregulated after statin (HMGCR inhibitor) treatment, which inevitably diminishes its therapeutic efficacy, provoking the need for higher doses associated with adverse effects. The proteolysis targeting chimera (PROTAC) technology has recently emerged as a powerful approach for inducing protein degradation. Nonetheless, due to their bifunctional nature, developing orally bioavailable PROTACs remains a great challenge. Herein, we identified a powerful HMGCR-targeted PROTAC (