[HTML][HTML] Discovery of a potent BTK and IKZF1/3 triple degrader through reversible covalent BTK PROTAC development
Building on our previous work on ibrutinib-based reversible covalent Bruton's tyrosine
kinase (BTK) PROTACs, we explored a different irreversible BTK inhibitor poseltinib as the …
kinase (BTK) PROTACs, we explored a different irreversible BTK inhibitor poseltinib as the …
MZ1 co-operates with trastuzumab in HER2 positive breast cancer
MM Noblejas-López, C Nieto-Jiménez… - Journal of Experimental …, 2021 - Springer
Background Although the anti-HER2 antibody trastuzumab augments patient survival in
HER2+ breast cancer, a relevant number of patients progress to this treatment. In this …
HER2+ breast cancer, a relevant number of patients progress to this treatment. In this …
Advances in research on potential inhibitors of multiple myeloma
G Tang, S Huang, J Luo, Y Wu, S Zheng, R Tong… - European Journal of …, 2023 - Elsevier
Multiple myeloma (MM) is a common hematological malignancy. Although recent clinical
applications of immunomodulatory drugs, proteasome inhibitors and CD38-targeting …
applications of immunomodulatory drugs, proteasome inhibitors and CD38-targeting …
It is theoretically possible to avoid misfolding into non-covalent lasso entanglements using small molecule drugs
A novel class of protein misfolding characterized by either the formation of non-native
noncovalent lasso entanglements in the misfolded structure or loss of native entanglements …
noncovalent lasso entanglements in the misfolded structure or loss of native entanglements …
Photopharmacology of proteolysis-targeting chimeras: a new frontier for drug discovery
S Zeng, H Zhang, Z Shen, W Huang - Frontiers in Chemistry, 2021 - frontiersin.org
Photopharmacology is an emerging field that uses light to precisely control drug activity. This
strategy promises to improve drug specificity for reducing off-target effects. Proteolysis …
strategy promises to improve drug specificity for reducing off-target effects. Proteolysis …
Selective degradation of hyperphosphorylated tau by proteolysis-targeting chimeras ameliorates cognitive function in Alzheimer's disease model mice
D Yao, T Li, L Yu, M Hu, Y He, R Zhang, J Wu… - Frontiers in …, 2024 - frontiersin.org
Alzheimer's disease (AD) is one of the most common chronic neurodegenerative diseases.
Hyperphosphorylated tau plays an indispensable role in neuronal dysfunction and synaptic …
Hyperphosphorylated tau plays an indispensable role in neuronal dysfunction and synaptic …
It'sa TRIM-endous view from the top: the varied roles of TRIpartite Motif proteins in brain development and disease
J Dudley-Fraser, K Rittinger - Frontiers in Molecular Neuroscience, 2023 - frontiersin.org
The tripartite motif (TRIM) protein family members have been implicated in a multitude of
physiologies and pathologies in different tissues. With diverse functions in cellular …
physiologies and pathologies in different tissues. With diverse functions in cellular …
[HTML][HTML] Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in …
Y He, Y Luo, L Huang, D Zhang, H Hou, Y Liang… - European Journal of …, 2024 - Elsevier
Our previous research has revealed phosphoglycerate kinase 1 (PGK1) enhances
tumorigenesis and sorafenib resistance of kidney renal clear cell carcinoma (KIRC) by …
tumorigenesis and sorafenib resistance of kidney renal clear cell carcinoma (KIRC) by …
[HTML][HTML] Nano-Proteolysis Targeting Chimeras (Nano-PROTACs) in Cancer Therapy
Y Song, QQ Dong, YK Ni, XL Xu… - International Journal of …, 2024 - ncbi.nlm.nih.gov
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules that have the
capability to induce specific protein degradation. While playing a revolutionary role in …
capability to induce specific protein degradation. While playing a revolutionary role in …
An Overview of PROTACs Targeting MDM2 as a Novel Approach for Cancer Therapy
H Li, X Cai, X Yang, X Zhang - European Journal of Medicinal Chemistry, 2024 - Elsevier
MDM2 genes amplification or altered expression is commonly observed in various cancers
bearing wild-type TP53. Directly targeting the p53-binding pocket of MDM2 to activate the …
bearing wild-type TP53. Directly targeting the p53-binding pocket of MDM2 to activate the …