Translating p53-based therapies for cancer into the clinic
S Peuget, X Zhou, G Selivanova - Nature Reviews Cancer, 2024 - nature.com
Inactivation of the most important tumour suppressor gene TP53 occurs in most, if not all,
human cancers. Loss of functional wild-type p53 is achieved via two main mechanisms …
human cancers. Loss of functional wild-type p53 is achieved via two main mechanisms …
Pharmacological reactivation of p53 in the era of precision anticancer medicine
A Tuval, C Strandgren, A Heldin… - Nature Reviews …, 2024 - nature.com
Abstract p53, which is encoded by the most frequently mutated gene in cancer, TP53, is an
attractive target for novel cancer therapies. Despite major challenges associated with this …
attractive target for novel cancer therapies. Despite major challenges associated with this …
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 …
mRNAs and is a critical regulator of gene expression and cellular physiology. m6A …
High-throughput evaluation of genetic variants with prime editing sensor libraries
SI Gould, AN Wuest, K Dong, GA Johnson, A Hsu… - Nature …, 2024 - nature.com
Tumor genomes often harbor a complex spectrum of single nucleotide alterations and
chromosomal rearrangements that can perturb protein function. Prime editing has been …
chromosomal rearrangements that can perturb protein function. Prime editing has been …
Understanding the complexity of p53 in a new era of tumor suppression
Summary p53 was discovered 45 years ago as an SV40 large T antigen binding protein,
coded by the most frequently mutated TP53 gene in human cancers. As a transcription …
coded by the most frequently mutated TP53 gene in human cancers. As a transcription …
Cell fate regulation governed by p53: Friends or reversible foes in cancer therapy
B Song, P Yang, S Zhang - Cancer Communications, 2024 - Wiley Online Library
Cancer is a leading cause of death worldwide. Targeted therapies aimed at key oncogenic
driver mutations in combination with chemotherapy and radiotherapy as well as …
driver mutations in combination with chemotherapy and radiotherapy as well as …
Design, synthesis, and characterization of cinnamic acid derivatives with two novel acrylohydrazones on HeLa and CHO-1 cancer cell lines: the experimental and …
Purpose To investigate the effect of derivatives of cinnamic acid on the proliferation of CHO-
1 and HeLa cell lines. Methods Three Acrylohydrazones (7–9) derived from cinnamic acid …
1 and HeLa cell lines. Methods Three Acrylohydrazones (7–9) derived from cinnamic acid …
Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators
The cavity-creating p53 cancer mutation Y220C is an ideal paradigm for developing small-
molecule drugs based on protein stabilization. Here, we have systematically analyzed the …
molecule drugs based on protein stabilization. Here, we have systematically analyzed the …
Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality
A systematic strategy to develop dual-warhead inhibitors is introduced to circumvent the
limitations of conventional covalent inhibitors such as vulnerability to mutations of the …
limitations of conventional covalent inhibitors such as vulnerability to mutations of the …
Evaluation of a Covalent Library of Diverse Warheads (CovLib) Binding to JNK3, USP7, or p53
T Klett, M Schwer, LN Ernst… - Drug Design …, 2024 - Taylor & Francis
Purpose Over the last few years, covalent fragment-based drug discovery has gained
significant importance. Thus, striving for more warhead diversity, we conceived a library …
significant importance. Thus, striving for more warhead diversity, we conceived a library …