This real‐world study of ROS1+ NSCLC highlights fusion diversity, treatment outcomes with crizotinib and lorlatinib, and in vitro experiments with resistance mechanisms. G2032R drives strong resistance to ROS1‐targeted TKIs, especially lorlatinib. Fusion partner location does not affect overall survival to crizotinib or lorlatinib. Findings support the
Fenneke Zwierenga+8 more
wiley +1 more source
The Medicinal Chemistry at the “Polo de Xistoquímica” of the IQ‐UFRJ
Joaquim F.M. Silva+4 more
openalex +1 more source
The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4-Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria. [PDF]
Woodland JG+33 more
europepmc +1 more source
We investigated whether hypomethylating agents (HMAs) used in myeloid malignancies induce somatic retrotransposition. Our findings indicate that HMA treatment increases L1‐encoded protein expression but does not lead to detectable de novo retrotransposition events in either patient samples or cell lines.
Šárka Pavlová+14 more
wiley +1 more source
Synthetic Approaches, Properties, and Applications of Acylals in Preparative and Medicinal Chemistry. [PDF]
Keydel T, Link A.
europepmc +1 more source
YAP1::TFE3 mediates endothelial‐to‐mesenchymal plasticity in epithelioid hemangioendothelioma
The YAP1::TFE3 fusion protein drives endothelial‐to‐mesenchymal transition (EndMT) plasticity, resulting in the loss of endothelial characteristics and gain of mesenchymal‐like properties, including resistance to anoikis, increased migratory capacity, and loss of contact growth inhibition in endothelial cells.
Ant Murphy+9 more
wiley +1 more source
Structural insights, regulation, and recent advances of RAS inhibitors in the MAPK signaling cascade: a medicinal chemistry perspective. [PDF]
Prajapati V+9 more
europepmc +1 more source
SensRORing cholesterol to drive protumoral myelopoiesis
Bleve et al. uncover a cholesterol‐driven immune evasion pathway, where RORγ‐dependent myelopoiesis shapes tumor immunosuppression. Targeting RORγ and PCSK9 emerges as a strategy to boost cancer immunotherapy. Protumoral myelopoiesis is a determinant of immunoevasion and tumor spread in many malignancies.
Sara Gennari, Luigi Nezi, Teresa Manzo
wiley +1 more source
Syntheses and medicinal chemistry of spiro heterocyclic steroids. [PDF]
Romero-Hernández LL+5 more
europepmc +1 more source
Emerging role of ARHGAP29 in melanoma cell phenotype switching
This study gives first insights into the role of ARHGAP29 in malignant melanoma. ARHGAP29 was revealed to be connected to tumor cell plasticity, promoting a mesenchymal‐like, invasive phenotype and driving tumor progression. Further, it modulates cell spreading by influencing RhoA/ROCK signaling and affects SMAD2 activity. Rho GTPase‐activating protein
Beatrice Charlotte Tröster+3 more
wiley +1 more source