Targeting mutant p53 for cancer therapy: direct and indirect strategies

J Hu, J Cao, W Topatana, S Juengpanich, S Li… - Journal of hematology & …, 2021 - Springer
TP53 is a critical tumor-suppressor gene that is mutated in more than half of all human
cancers. Mutations in TP53 not only impair its antitumor activity, but also confer mutant p53 …

Targeting p53 pathways: mechanisms, structures, and advances in therapy

H Wang, M Guo, H Wei, Y Chen - Signal transduction and targeted …, 2023 - nature.com
The TP53 tumor suppressor is the most frequently altered gene in human cancers, and has
been a major focus of oncology research. The p53 protein is a transcription factor that can …

Acetylation targeting chimera enables acetylation of the tumor suppressor p53

M Kabir, N Sun, X Hu, TC Martin, J Yi… - Journal of the …, 2023 - ACS Publications
With advances in chemically induced proximity technologies, heterobifunctional modalities
such as proteolysis targeting chimeras (PROTACs) have been successfully advanced to …

Discovery of nanomolar-affinity pharmacological chaperones stabilizing the oncogenic p53 mutant Y220C

JR Stephenson Clarke, LR Douglas… - ACS pharmacology & …, 2022 - ACS Publications
The tumor suppressor protein p53 is inactivated in the majority of human cancers and
remains a prime target for develo** new drugs to reactivate its tumor suppressing activity …

Structural basis of reactivation of oncogenic p53 mutants by a small molecule: methylene quinuclidinone (MQ)

O Degtjarik, D Golovenko, Y Diskin-Posner… - Nature …, 2021 - nature.com
In response to genotoxic stress, the tumor suppressor p53 acts as a transcription factor by
regulating the expression of genes critical for cancer prevention. Mutations in the gene …

Targeting mutant p53 for cancer treatment: moving closer to clinical use?

MJ Duffy, M Tang, S Rajaram, S O'Grady, J Crown - Cancers, 2022 - mdpi.com
Simple Summary Cancer is largely caused by genetic alterations such as mutations in a
group of genes known as cancer driver genes. Many of the key advances in cancer …

Programmable protein expression using a genetically encoded m6A sensor

BF Marayati, MG Thompson, CL Holley… - Nature …, 2024 - nature.com
Abstract The N 6-methyladenosine (m6A) modification is found in thousands of cellular
mRNAs and is a critical regulator of gene expression and cellular physiology. m6A …

Structural and drug targeting insights on mutant p53

AS Gomes, H Ramos, A Inga, E Sousa, L Saraiva - Cancers, 2021 - mdpi.com
Simple Summary The tumor suppressor protein p53 is frequently mutated in human cancers,
and its reactivation represents an encouraging hope for precision anticancer therapy …

Advanced strategies for therapeutic targeting of wild-type and mutant p53 in cancer

S Zhang, L Carlsen, L Hernandez Borrero, AA Seyhan… - Biomolecules, 2022 - mdpi.com
TP53 is a tumor suppressor gene that encodes a sequence-specific DNA-binding
transcription factor activated by stressful stimuli; it upregulates target genes involved in …

Therapeutic strategies to activate p53

A Aguilar, S Wang - Pharmaceuticals, 2022 - mdpi.com
The p53 protein has appropriately been named the “guardian of the genome”. In almost all
human cancers, the powerful tumor suppressor function of p53 is compromised by a variety …