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Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells
TLDR
A compound, designed to inhibit the Abl protein tyrosine kinase, was evaluated for its effects on cells containing the Bcr–Abl fusion protein and it was found that this compound may be useful in the treatment of bcr–abl–positive leukemias.
Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug
TLDR
This work describes how this drug discovery programme led to the discovery and continuing development of Glivec (Gleevec in the United States), the first selective tyrosine-kinase inhibitor to be approved for the treatment of a cancer.
The development of imatinib as a therapeutic agent for chronic myeloid leukemia.
TLDR
The preclinical and clinical development of imatinib for the therapy of CML, resistance and strategies that may help to eliminate resistant or residual leukemia are reviewed.
Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative.
TLDR
An inhibitor (CGP 57148) of the Abl and platelet-derived growth factor (PDGF) receptor protein-tyrosine kinases from the 2-phenylaminopyrimidine class is described, which is highly active in vitro and in vivo and may have therapeutic potential for the treatment of diseases that involve abnormal cellular proliferation induced by Abl protein-tiesine kinase deregulation or PDGF receptor activation.
Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia
TLDR
The results implicate Src family kinases as therapeutic targets in Ph+ B-ALL and suggest that simultaneous inhibition of Src and Bcr-Abl kinases may benefit individuals with Ph+ acute leukemia.
PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after
TLDR
A novel compound with therapeutic potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role, PTK787/ZK 222584 is very well tolerated and does not impair wound healing.
CGP 57148, a tyrosine kinase inhibitor, inhibits the growth of cells expressing BCR-ABL, TEL-ABL, and TEL-PDGFR fusion proteins.
TLDR
It is shown that cells expressing an activated PDGFR tyrosine kinase, TEL-PDGFR, are sensitive to CGP 57148, and this compound may be useful for the treatment of a variety of BCR-ABL-positive leukemias and for treatment of the subset of chronic myelomonocytic leukemia patients with a Tel-PDgFR fusion protein.
Inhibition of platelet-derived growth factor receptors reduces interstitial hypertension and increases transcapillary transport in tumors.
TLDR
Interference with PDGF receptors, or their ligands, as a novel strategy to increase drug uptake and therapeutic effectiveness of cancer chemotherapy is suggested.
Imatinib Mesylate Is a Potent Inhibitor of the ABCG2 (BCRP) Transporter and Reverses Resistance to Topotecan and SN-38 in Vitro
TLDR
It is shown that imatinib mesylate potently reverses ABCG2-mediated resistance to topotecan and SN-38 and significantly increases accumulation of topotECan only in cells expressing functional ABCG 2.
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