E1 enzymes as therapeutic targets in cancer

SH Barghout, AD Schimmer - Pharmacological reviews, 2021 - ASPET
Post-translational modifications of cellular substrates with ubiquitin and ubiquitin-like
proteins (UBLs), including ubiquitin, SUMOs, and neural precursor cell–expressed …

Regulation of EZH2 protein stability: new mechanisms, roles in tumorigenesis, and roads to the clinic

Y Guo, R Cheng, Y Wang, ME Gonzalez, H Zhang… - …, 2024 - thelancet.com
The importance of EZH2 as a key methyltransferase has been well documented
theoretically. Practically, the first EZH2 inhibitor Tazemetostat (EPZ6438), was approved by …

PROTACs: current trends in protein degradation by proteolysis-targeting chimeras

J Madan, VK Ahuja, K Dua, S Samajdar… - BioDrugs, 2022 - Springer
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …

Druggable genome and precision medicine in cancer: current challenges

CA Dupont, K Riegel, M Pompaiah, H Juhl… - The FEBS …, 2021 - Wiley Online Library
The past decades have seen tremendous developments with respect to “specific”
therapeutics that target key signaling molecules to conquer cancer. The key advancements …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …

RGS proteins and their roles in cancer: friend or foe?

L Li, Q Xu, C Tang - Cancer Cell International, 2023 - Springer
As negative modulators of G-protein-coupled receptors (GPCRs) signaling, regulators of G
protein signaling (RGS) proteins facilitate various downstream cellular signalings through …

Triple-negative breast cancer: Identification of circRNAs with efficacy in preclinical in vivo models

UH Weidle, F Birzele - Cancer Genomics & Proteomics, 2023 - cgp.iiarjournals.org
Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer with
insufficient options for therapy. In order to identify new targets and treatment modalities we …

[HTML][HTML] Emerging drug design strategies in anti-influenza drug discovery

C Liu, L Hu, G Dong, Y Zhang… - … Pharmaceutica Sinica B, 2023 - Elsevier
Influenza is an acute respiratory infection caused by influenza viruses (IFV), According to the
World Health Organization (WHO), seasonal IFV epidemics result in approximately 3–5 …

E3 ubiquitin ligases in breast cancer metastasis: a systematic review of pathogenic functions and clinical implications

Y Wang, J Dai, Y Zeng, J Guo, J Lan - Frontiers in Oncology, 2021 - frontiersin.org
Female breast cancer has become the most commonly occurring cancer worldwide.
Although it has a good prognosis under early diagnosis and appropriate treatment, breast …

Long non-coding RNAs with in vitro and in vivo efficacy in preclinical models of esophageal squamous cell carcinoma which act by a non-microRNA sponging …

UH Weidle, F Birzele - Cancer Genomics & Proteomics, 2022 - cgp.iiarjournals.org
Esophageal squamous cell carcinoma is a type of cancer with dismal prognosis. Surgery,
chemo-and radiation therapy, as well as immune checkpoint-blocking immunotherapy lead …