Design, synthesis and biological characterization of histone deacetylase 8 (HDAC8) proteolysis targeting chimeras (PROTACs) with anti-neuroblastoma activity

S Darwish, E Ghazy, T Heimburg, D Herp… - International journal of …, 2022 - mdpi.com
In addition to involvement in epigenetic gene regulation, histone deacetylases (HDACs)
regulate multiple cellular processes through mediating the activity of non-histone protein …

Innovative approaches for treatment of osteosarcoma

E Rothzerg, AL Pfaff, S Koks - Experimental Biology and …, 2022 - journals.sagepub.com
Osteosarcoma (OS) is the most common primary malignant bone tumor, which usually
occurs in children and adolescents. It is generally a high-grade malignancy presenting with …

Modulating the activity of androgen receptor for treating breast cancer

CP You, H Tsoi, EPS Man, MH Leung… - International Journal of …, 2022 - mdpi.com
The androgen receptor (AR) is a steroid hormone receptor widely detected in breast cancer.
Evidence suggests that the AR might be a tumor suppressor in estrogen receptor alpha …

The clinical utility of ESR1 mutations in hormone receptor-positive, HER2-negative advanced breast cancer

A Grinshpun, ZM Sandusky… - Hematology/Oncology …, 2023 - hemonc.theclinics.com
Estrogen receptor a (ER), encoded by the ESR1 gene, is a nuclear receptor transcription
factor whose cognate ligand is estradiol. Following estradiol binding to ER, the receptor …

PROTACs in gastrointestinal cancers

Y Chen, Q Yang, J Xu, L Tang, Y Zhang, F Du… - Molecular Therapy …, 2022 - cell.com
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein
degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase …

Targeting SHP2 phosphatase in hematological malignancies

R Kanumuri, S Kumar Pasupuleti… - Expert opinion on …, 2022 - Taylor & Francis
Introduction Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a
ubiquitously expressed, non-receptor protein tyrosine phosphatase encoded by the PTPN11 …

Design, synthesis and biological evaluation of KRASG12C-PROTACs

X Zhang, T Zhao, M Sun, P Li, M Lai, L Xie… - Bioorganic & Medicinal …, 2023 - Elsevier
Several small-molecule covalent inhibitors of KRAS G 12 C have made breakthrough
progress in the treatment of KRAS mutant cancer. However, the clinical application of KRAS …

An Update on Protein Kinases as Therapeutic Targets—Part I: Protein Kinase C Activation and Its Role in Cancer and Cardiovascular Diseases

S Silnitsky, SJS Rubin, M Zerihun, N Qvit - International Journal of …, 2023 - mdpi.com
Protein kinases are one of the most significant drug targets in the human proteome,
historically harnessed for the treatment of cancer, cardiovascular disease, and a growing …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy: present and future

R Li, M Liu, Z Yang, J Li, Y Gao, R Tan - Molecules, 2022 - mdpi.com
The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the
selective degradation of target proteins via the ubiquitin–proteasome system. Compared …

Potential application of heat shock proteins as therapeutic targets in Parkinson's disease

H Guo, J Yi, F Wang, T Lei, H Du - Neurochemistry International, 2023 - Elsevier
Parkinson's disease (PD) is a common chronic neurodegenerative disease, and the heat
shock proteins (HSPs) are proved to be of great value for PD. In addition, HSPs can maintain …