PROTACs: A novel strategy for cancer drug discovery and development
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …
Impact of tissue-agnostic approvals on management of primary brain tumors
Novel tissue-agnostic therapeutics targeting driver mutations in tumor cells have been
recently approved by FDA, driven by basket trials that have demonstrated their efficacy and …
recently approved by FDA, driven by basket trials that have demonstrated their efficacy and …
Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer
H Luo, D Si, X Sun, M Wang, Y Yang, B Wang… - European Journal of …, 2023 - Elsevier
The function of the p53 protein is impaired by the overexpression of its negative regulator
murine double minute 2 protein (MDM2) and homologous protein MDMX. Disruption of the …
murine double minute 2 protein (MDM2) and homologous protein MDMX. Disruption of the …
Antagonizing MDM2 overexpression induced by MDM4 inhibitor CEP-1347 effectively reactivates wild-type p53 in malignant brain tumor cells
Y Mitobe, S Suzuki, Y Nakagawa-Saito, K Togashi… - Cancers, 2023 - mdpi.com
Simple Summary In human cancer, the major tumor suppressor p53 is often functionally
inactivated through the deregulation of its negative regulators MDM2 and MDM4. The …
inactivated through the deregulation of its negative regulators MDM2 and MDM4. The …
Refined criteria for p53 expression in ovarian mucinous tumours are highly concordant with TP53 mutation status, but p53 expression/TP53 status lack prognostic …
P Dundr, N Hájková, MK Bártů, D Cibula, J Drozenová… - Pathology, 2023 - Elsevier
In gynecological neoplasms, immunohistochemical (IHC) expression of p53 is generally an
accurate predictor of TP53 mutation status if correctly interpreted by the pathologist …
accurate predictor of TP53 mutation status if correctly interpreted by the pathologist …
The Novel MDM4 Inhibitor CEP-1347 Activates the p53 Pathway and Blocks Malignant Meningioma Growth In Vitro and In Vivo
Y Mitobe, S Suzuki, Y Nakagawa-Saito, K Togashi… - Biomedicines, 2023 - mdpi.com
A significant proportion of meningiomas are clinically aggressive, but there is currently no
effective chemotherapy for meningiomas. An increasing number of studies have been …
effective chemotherapy for meningiomas. An increasing number of studies have been …
Hybrid molecules of protoflavones and spirooxindole derivatives with selective cytotoxicity against triple-negative breast cancer cells
G Girst, EA Lopes, LM Gonçalves… - RSC Medicinal …, 2023 - pubs.rsc.org
The combination of compounds with complementary bioactivities into hybrid molecules is an
emerging concept in drug discovery. In this study, we aimed to synthesize new hybrid …
emerging concept in drug discovery. In this study, we aimed to synthesize new hybrid …
Synthesis and biological evaluation of 4-imidazolidinone–containing compounds as potent inhibitors of the MDM2/p53 interaction
Z Lin, C Liu, Z Yan, J Cheng, X Wang, F Zhou… - European Journal of …, 2024 - Elsevier
Inhibition of MDM2/p53 interaction with small-molecule inhibitors stabilizes p53 from MDM2
mediated degradation, which is a promising strategy for the treatment of cancer. In this …
mediated degradation, which is a promising strategy for the treatment of cancer. In this …
Low-dose brain radiation: lowering hyperphosphorylated-tau without increasing DNA damage or oncogenic activation
D Iacono, EK Murphy, CD Stimpson, DP Perl… - Scientific Reports, 2023 - nature.com
Brain radiation has been medically used to alter the metabolism of cancerous cells and
induce their elimination. Rarely, though, brain radiation has been used to interfere with the …
induce their elimination. Rarely, though, brain radiation has been used to interfere with the …
p53/MDM2 signaling pathway in aging, senescence and tumorigenesis
Y Huang, X Che, PW Wang, X Qu - Seminars in Cancer Biology, 2024 - Elsevier
A wealth of evidence has emerged that there is an association between aging, senescence
and tumorigenesis. Senescence, a biological process by which cells cease to divide and …
and tumorigenesis. Senescence, a biological process by which cells cease to divide and …