How to sensitize glioblastomas to temozolomide chemotherapy: A gap-centered view

A Miramova, A Gartner, D Ivanov - Frontiers in Cell and …, 2024 - frontiersin.org
Temozolomide (TMZ) is a methylating agent used as the first-line drug in the chemotherapy
of glioblastomas. However, cancer cells eventually acquire resistance, necessitating the …

Structure-based discovery of first inhibitors targeting the helicase activity of human PIF1

MJA Wever, FR Scommegna… - Nucleic acids …, 2024 - academic.oup.com
PIF1 is a conserved helicase and G4 DNA binding and unwinding enzyme, with roles in
genome stability. Human PIF1 (hPIF1) is poorly understood, but its functions can become …

Oncological characteristics, treatments and prognostic outcomes in MMR-deficient colorectal cancer

WX Fan, F Su, Y Zhang, XL Zhang, YY Du, YJ Gao… - Biomarker …, 2024 - Springer
Colorectal cancer (CRC) ranks as the third most prevalent cancer globally. It's recognized
that the molecular subtype of CRC, characterized by mismatch repair deficiency (dMMR) or …

Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity

A Ghoshal, KH Asressu, MA Hossain… - Journal of Medicinal …, 2024 - ACS Publications
Despite their widespread impact on human health, there are no approved drugs for
combating alphavirus infections. The heterocyclic β-aminomethyl vinyl sulfone RA-0002034 …

Covalent Inhibitors: To Infinity and Beyond

YS Raouf - Journal of Medicinal Chemistry, 2024 - ACS Publications
A future perspective on the “history of drug discovery” would more than likely characterize
the 20th century (1901− 1999) as one of the most significant collections of decades with …

WRN Helicase: Is There More to MSI-H than Immunotherapy?

ZA Wainberg - Cancer Discovery, 2024 - aacrjournals.org
In this issue, Picco and colleagues provide further evidence that WRN inhibitors are
synthetically lethal in microsatellite instability-high (MSI-H) cancers and function by blocking …

Ligand discovery by activity-based protein profiling

MJ Niphakis, BF Cravatt - Cell Chemical Biology, 2024 - cell.com
Genomic technologies have led to massive gains in our understanding of human gene
function and disease relevance. Chemical biologists are a primary beneficiary of this …

Design, Synthesis, and Structure− Activity Relationship Studies of Triazolo-pyrimidine Derivatives as WRN Inhibitors for the Treatment of MSI Tumors

Q Sui, Y Zhou, M Li, D Wang, R Cui, X Cai, J Liu… - European Journal of …, 2024 - Elsevier
Werner syndrome RecQ helicase (WRN), a member of the RecQ helicase family, has
recently been identified as a synthetic lethal target in microsatellite instability (MSI) tumors …

Systematic targeting of protein complexes with molecular COUPLrs

D Yang, S Harry, H Chong, E Zhang, N Nordenfelt… - bioRxiv, 2024 - biorxiv.org
Molecular glues that engage protein complexes have transformed the study of cell biology
and have had a direct impact on clinical oncology. However, the identification of new glue …

An Update on Small Molecule Compounds Targeting Synthetic Lethality for Cancer Therapy

J Luo, Y Li, Y Zhang, D Wu, Y Ren, J Liu… - European Journal of …, 2024 - Elsevier
Targeting cancer-specific vulnerabilities through synthetic lethality (SL) is an emerging
paradigm in precision oncology. A SL strategy based on PARP inhibitors has demonstrated …