Abstract

Highlights| March 02 2023 Selected Articles from This Issue Author & Article Information Online ISSN: 1538-8514 Print ISSN: 1535-7163 ©2023 American Association for Cancer Research2023American Association for Cancer Research Mol Cancer Ther (2023) 22 (3): 289. https://doi.org/10.1158/1535-7163.MCT-22-3-HI Related Content A commentary has been published: Venadaparib Is a Novel and Selective PARP Inhibitor with Improved Physicochemical Properties, Efficacy, and Safety A commentary has been published: Daclatasvir, an Antiviral Drug, Downregulates Tribbles 2 Pseudokinase and Resensitizes Enzalutamide-Resistant Prostate Cancer Cells A commentary has been published: A Bispecific METxMET Antibody–Drug Conjugate with Cleavable Linker Is Processed in Recycling and Late Endosomes View more A commentary has been published: Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma View less Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Facebook Twitter LinkedIn MailTo Tools Icon Tools Get Permissions Cite Icon Cite Search Site Article Versions Icon Versions Version of Record March 2 2023 Citation Selected Articles from This Issue. Mol Cancer Ther 1 March 2023; 22 (3): 289. https://doi.org/10.1158/1535-7163.MCT-22-3-HI Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest Search Advanced Search Combination of BRAF inhibitor and MEK inhibitor is current Standard of Care (SoC) for BRAF-mutated melanoma. However, almost all patients develop resistance to these agents and one of the resistance mechanisms is BRAF overexpression. To overcome this kind of resistance, Takano and colleagues discovered novel ATP-competitive MEK inhibitors, DS56771486 and DS03090629. These compounds tended to retain their activities in BRAF overexpressed A375 cell line whereas currently used BRAF inhibitor and MEK inhibitor got attenuated in this cell line compared to parental A375. These results indicate the potential of these compounds to overcome the resistance to current SoC in BRAF-mutated melanoma. PARP inhibitors are widely available to patients with homologous recombination deficient breast, ovarian, pancreatic, or prostate cancers. The use of current PARP inhibitors as chemo-potentiating agents have been limited due to toxicities. Lee and colleagues developed a next generation PARP inhibitor venadaparib. Molecular characteristics of venadaparib translated to superior efficacy... You do not currently have access to this content.

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