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 …
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 …
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 …
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 …
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 …
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 …
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 …
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
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 …
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 …
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 …
shock proteins (HSPs) are proved to be of great value for PD. In addition, HSPs can maintain …