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Relevant bibliographies by topics / Proteolysis targeting chimera (PROTAC)

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Academic literature on the topic 'Proteolysis targeting chimera (PROTAC)'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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Journal articles on the topic "Proteolysis targeting chimera (PROTAC)"

1

Wan, Yichao, Chunxing Yan, Han Gao, and Tingting Liu. "Small-molecule PROTACs: novel agents for cancer therapy." Future Medicinal Chemistry 12, no. 10 (2020): 915–38. http://dx.doi.org/10.4155/fmc-2019-0340.

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Proteolysis-targeting chimera (PROTAC) is a new technology to selectively degrade target proteins via ubiquitin-proteasome system. PROTAC molecules (PROTACs) are a class of heterobifunctional molecules, which contain a ligand targeting the protein of interest, a ligand recruiting an E3 ligase and a linker connecting these two ligands. They provide several advantages over traditional inhibitors in potency, selectivity and drug resistance. Thus, many promising PROTACs have been developed in the recent two decades, especially small-molecule PROTACs. In this review, we briefly introduce the mechan

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2

Smalley, Joshua P., Grace E. Adams, Christopher J. Millard, et al. "PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes." Chemical Communications 56, no. 32 (2020): 4476–79. http://dx.doi.org/10.1039/d0cc01485k.

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We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. Our PROTAC decreased HDAC 1, 2 & 3 protein abundance, increased histone acetylation levels and compromised colon cancer HCT116 cell viability.

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3

Robb, Caroline M., Jacob I. Contreras, Smit Kour, et al. "Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)." Chemical Communications 53, no. 54 (2017): 7577–80. http://dx.doi.org/10.1039/c7cc03879h.

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4

Xia, Li-Wen, Meng-Yu Ba, Wei Liu, et al. "Triazol: a privileged scaffold for proteolysis targeting chimeras." Future Medicinal Chemistry 11, no. 22 (2019): 2919–73. http://dx.doi.org/10.4155/fmc-2019-0159.

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Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer a

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5

Cimas, Francisco J., Enrique Niza, Alberto Juan, et al. "Controlled Delivery of BET-PROTACs: In Vitro Evaluation of MZ1-Loaded Polymeric Antibody Conjugated Nanoparticles in Breast Cancer." Pharmaceutics 12, no. 10 (2020): 986. http://dx.doi.org/10.3390/pharmaceutics12100986.

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Bromo and extraterminal domain (BET) inhibitors-PROteolysis TArgeting Chimera (BETi-PROTAC) is a new family of compounds that induce proteasomal degradation through the ubiquitination of the tagged to BET inhibitors Bromodomain proteins, BRD2 and BRD. The encapsulation and controlled release of BET-PROTACs through their vectorization with antibodies, like trastuzumab, could facilitate their pharmacokinetic and efficacy profile. Antibody conjugated nanoparticles (ACNPs) using PROTACs have not been designed and evaluated. In this pioneer approach, the commercial MZ1 PROTAC was encapsulated into

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6

Koravović, Mladen, Gordana Tasić, Milena Rmandić, and Bojan Marković. "Photocontrollable PROTAC molecules: Structure and mechanism of action." Arhiv za farmaciju 71, no. 3 (2021): 161–76. http://dx.doi.org/10.5937/arhfarm71-30785.

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Traditional drug discovery strategies are usually focused on occupancy of binding sites that directly affect functions of proteins. Hence, proteins that lack such binding sites are generally considered pharmacologically intractable. Modulators of protein activity, especially inhibitors, must be applied in appropriate dosage regimens that often lead to high systemic drug exposures in order to maintain sufficient protein inhibition in vivo. Consequently, there is a risk of undesirable off-target drug binding and side effects. Recently, PROteolysis TArgeting Chimera (PROTAC) technology has emerge

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7

Liu, Jing, He Chen, Leina Ma, et al. "Light-induced control of protein destruction by opto-PROTAC." Science Advances 6, no. 8 (2020): eaay5154. http://dx.doi.org/10.1126/sciadv.aay5154.

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By hijacking endogenous E3 ligase to degrade protein targets via the ubiquitin-proteasome system, PROTACs (PRoteolysis TArgeting Chimeras) provide a new strategy to inhibit protein targets that were regarded as undruggable before. However, the catalytic nature of PROTAC potentially leads to uncontrolled degradation that causes systemic toxicity issues, limiting the application of PROTAC in the clinic. Here, we introduce a light-inducible switch on PROTACs, thereafter termed as opto-PROTAC, to enable the degradation of protein targets in a spatiotemporal manner. By adding a photolabile caging g

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8

Wang, Pingyuan, and Jia Zhou. "Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery." Current Topics in Medicinal Chemistry 18, no. 16 (2018): 1354–56. http://dx.doi.org/10.2174/1568026618666181010101922.

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9

Cao, Fangyuan, Sander de Weerd, Deng Chen, Martijn R. H. Zwinderman, Petra E. van der Wouden, and Frank J. Dekker. "Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC)." European Journal of Medicinal Chemistry 208 (December 2020): 112800. http://dx.doi.org/10.1016/j.ejmech.2020.112800.

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10

Zeng, Shenxin, Wenhai Huang, Xiaoliang Zheng, et al. "Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges." European Journal of Medicinal Chemistry 210 (January 2021): 112981. http://dx.doi.org/10.1016/j.ejmech.2020.112981.

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