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Cited by 299

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

He, Shipeng, Gao, Fei, Ma, Junhui, Ma, Haoqian, Dong, Guoqiang, Sheng, Chunquan·2021·Angewandte Chemie International Edition

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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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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CoChat. (2026). Citation check: Aptamer‐PROTAC Conjugates (APCs) for Tumor‐Specific Targeting in Breast Cancer. https://app.cochat.ai/papers/10.1002/anie.202107347
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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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Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.