{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Lantermans HC"],"funding":["CSC | Chinese Government Scholarship","KWF Kankerbestrijding (Dutch Cancer Society)","Lymph&Co","International Waldenstrom’s Macroglobulinemia Foundation","KWF Kankerbestrijding"],"pagination":["1570-1580"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11216997"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["38(7)"],"pubmed_abstract":["Although Bruton's tyrosine kinase (BTK) inhibitors (BTKi) have significantly improved patient prognosis, mantle cell lymphoma (MCL) is still considered incurable due to primary and acquired resistance. We have recently shown that aberrant expression of the Src-family tyrosine kinase hematopoietic cell kinase (HCK) in MCL correlates with poor prognosis, and that genetic HCK perturbation impairs growth and integrin-mediated adhesion of MCL cells. Here, we show that KIN-8194, a dual inhibitor of BTK and HCK with in vivo activity against Myd88-L265P-driven diffuse large B-cell lymphoma and Waldenström Macroglobulinemia, has a potent growth inhibitory effect in MCL cell lines and primary MCL cells, irrespective of their sensitivity to BTKi (ibrutinib and acalabrutinib). In BTKi-resistant cells "],"journal":["Leukemia"],"pubmed_title":["The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma."],"pmcid":["PMC11216997"],"funding_grant_id":["7873"],"pubmed_authors":["Yasinoglu S","Yang G","Treon SP","Lantermans HC","Wang J","Kersten MJ","Kuil A","Gray NS","Spaargaren M","Pals ST","van Kesteren S","Buhrlage SJ","Ma F"],"additional_accession":[]},"is_claimable":false,"name":"The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma.","description":"Although Bruton's tyrosine kinase (BTK) inhibitors (BTKi) have significantly improved patient prognosis, mantle cell lymphoma (MCL) is still considered incurable due to primary and acquired resistance. We have recently shown that aberrant expression of the Src-family tyrosine kinase hematopoietic cell kinase (HCK) in MCL correlates with poor prognosis, and that genetic HCK perturbation impairs growth and integrin-mediated adhesion of MCL cells. Here, we show that KIN-8194, a dual inhibitor of BTK and HCK with in vivo activity against Myd88-L265P-driven diffuse large B-cell lymphoma and Waldenström Macroglobulinemia, has a potent growth inhibitory effect in MCL cell lines and primary MCL cells, irrespective of their sensitivity to BTKi (ibrutinib and acalabrutinib). In BTKi-resistant cells ","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Jul","modification":"2025-04-04T12:54:16.645Z","creation":"2025-04-04T12:54:16.645Z"},"accession":"S-EPMC11216997","cross_references":{"pubmed":["38454120"],"doi":["10.1038/s41375-024-02207-9"]}}