The DOI matches its Crossref record; 37 of the 37 references it cites were found in a registry or an index.
Aptamer‐PROTAC Conjugates (APCs) for Tumor‐Specific Targeting in Breast Cancer
Abstract
Development of proteolysis targeting chimeras (PROTACs) is emerging as a promising strategy for targeted protein degradation. However, the drug development using the heterobifunctional PROTAC molecules is generally limited by poor membrane permeability, low in vivo efficacy and indiscriminate distribution. Herein an aptamer‐PROTAC conjugation approach was developed as a novel strategy to improve the tumor‐specific targeting ability and in vivo antitumor potency of conventional PROTACs. As proof of concept, the first aptamer‐PROTAC conjugate (APC) was designed by conjugating a BET‐targeting PROTAC to the nucleic acid aptamer AS1411 (AS) via a cleavable linker. Compared with the unmodified BET PROTAC, the designed molecule (APR) showed improved tumor targeting ability in a MCF‐7 xenograft model, leading to enhanced in vivo BET degradation and antitumor potency and decreased toxicity. Thus, the APC strategy may pave the way for the design of tumor‐specific targeting PROTACs and have broad applications in the development of PROTAC‐based drugs.
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Cited by
PROTACs: past, present and future
Li, K., & Crews, C. M. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00193d · Cited by 869
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
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Metadata
- Authors
- He, S., Gao, F., Ma, J., Ma, H., Dong, G., & Sheng, C.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2021-08-11
- Volume
- 60
- Issue
- 43
- Pages
- 23299-23305
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W3178147999
- Cited by
- 299
- References
- 37
- FWCI
- 11.74
- Type
- journal article
- Language
- en
- Open access
- closed
- Funders
- National Natural Science Foundation of China (82030105, 82003567)
- National Key Research and Development Program of China (2020YFA0509100)
- Natural Science Foundation of Shanghai (21ZR1422600)
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- He, S., Gao, F., Ma, J., Ma, H., Dong, G., & Sheng, C. (2021). Aptamer‐PROTAC Conjugates (APCs) for Tumor‐Specific Targeting in Breast Cancer. Angewandte Chemie International Edition. https://doi.org/10.1002/anie.202107347
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