E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

E3 ligase ligands in successful PROTACs: an overview of syntheses and linker attachment points

A Bricelj, C Steinebach, R Kuchta, M Gütschow… - Frontiers in …, 2021 - frontiersin.org
Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new
and exciting class of therapeutic agents that promise to significantly impact drug discovery …

Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders

C Steinebach, YLD Ng, I Sosič, CS Lee, S Chen… - Chemical …, 2020 - pubs.rsc.org
Cyclin-dependent kinase 6 (CDK6) is an important regulator of the cell cycle. Together with
CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 …

Hydrophobic tag-based protein degradation: Development, opportunity and challenge

Q He, X Zhao, D Wu, S Jia, C Liu, Z Cheng… - European Journal of …, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a promising approach for drug
development, particularly for undruggable targets. TPD technology has also been …

Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: past, present and future perspectives

S Ha, J Zhu, H Xiang, G Luo - Chinese Chemical Letters, 2023 - Elsevier
Small molecule inhibitors have dominated the pharmaceutical landscape for a long time as
the primary therapeutic paradigm targeting pathogenic proteins. However, their efficacy …

[HTML][HTML] Overexpression of hsa_circ_0002874 promotes resistance of non-small cell lung cancer to paclitaxel by modulating miR-1273f/MDM2/p53 pathway

J Xu, L Ni, F Zhao, X Dai, J Tao, J Pan, A Shi… - Aging (Albany …, 2021 - ncbi.nlm.nih.gov
Background: This study aimed to investigate the aberrant expression of hsa_circ_0002874
in non-small cell lung cancer (NSCLC) and elucidate associated molecular mechanisms that …

Applications of bacterial degrons and degraders—toward targeted protein degradation in bacteria

MA Izert, MM Klimecka, MW Górna - Frontiers in molecular …, 2021 - frontiersin.org
A repertoire of proteolysis-targeting signals known as degrons is a necessary component of
protein homeostasis in every living cell. In bacteria, degrons can be used in place of …

Targeted Degradation of DNA/RNA binding proteins via covalent hydrophobic tagging

Y Wang, J Zhang, J Deng, C Wang, L Fang… - CCS …, 2023 - chinesechemsoc.org
Targeted protein degradation (TPD) holds great promise for biological inquiry and
therapeutic development. However, it still remains elusive to destruct DNA/RNA binding …

Hydrophobic tagging-mediated degradation of transcription coactivator SRC-1

SR Choi, HM Wang, MH Shin, HS Lim - International Journal of Molecular …, 2021 - mdpi.com
Steroid receptor coactivator-1 (SRC-1) is a transcription coactivator playing a pivotal role in
mediating a wide range of signaling pathways by interacting with related transcription factors …

Emerging TACnology: heterobifunctional small molecule inducers of targeted posttranslational protein modifications

P Heitel - Molecules, 2023 - mdpi.com
Posttranslational modifications (PTMs) play an important role in cell signaling and they are
often deregulated in disease. This review addresses recent advances in the development of …