Synthesis and biological evaluation of diversely substituted indolin-2-ones (2008)
Bouchikhi, Fadoua, Rossignol, Emilie, Sancelme, Martine, Aboab, Bettina, Anizon, Fabrice, Fabbro, Doriano, ...
The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these...
Synthesis and biological evaluation of diversely substituted indolin-2-ones (2008)
Bouchikhi, Fadoua, Rossignol, Emilie, Sancelme, Martine, Aboab, Bettina, Anizon, Fabrice, Fabbro, Doriano, ...
The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these...
Synthesis and biological evaluation of diversely substituted indolin-2-ones (2008)
Bouchikhi, Fadoua, Rossignol, Emilie, Sancelme, Martine, Aboab, Bettina, Anizon, Fabrice, Fabbro, Doriano, ...
The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these...
Synthesis and biological evaluation of diversely substituted indolin-2-ones (2008)
Bouchikhi, Fadoua, Rossignol, Emilie, Sancelme, Martine, Aboab, Bettina, Anizon, Fabrice, Fabbro, Doriano, ...
The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these...
Chen, Jing, Lee, Benjamin H, McDowell, Elizabeth, Adelsperger, Jennifer, ...
AMN107 is a small molecule tyrosine kinase inhibitor developed, in the first instance, as a potent inhibitor of breakpoint cluster region-abelson (BCR-ABL). We tested its effectiveness against fusion...
Furet, Pascal, Fabbro, Doriano, Clark, Jennifer J, Griffin, James D, ...
Mutations in the receptor tyrosine kinase FLT3 occur frequently in patients with acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). Small molecules that selectively inhibit FLT3...
Stover, Elizabeth H, Boulton, Christina L, Gotlib, Jason, Legare, Robert D, Amaral, Sonia M, ...
FIP1L1-PDGFRalpha causes hypereosinophilic syndrome (HES) and is inhibited by the tyrosine kinase inhibitor imatinib (Gleevec). Imatinib is a potent inhibitor of ABL, ARG, PDGFRalpha, PDGFRbeta, and...
Soni, Rajeev, O'Reilly, Terence, Furet, Pascal, Muller, Lionel, Stephan, Christine, Zumstein-Mecker, Sabine, ...
Background: Cyclin-dependent kinase 4 (Cdk4) represents a prime target for the treatment of cancer because most human cancers are characterized by overexpression of its activating partner cyclin D1,...
Selective redistribution of protein kinase C isozymes by thapsigargin and staurosporine (1992)
Kiley, Susan C., Parker, Peter J., Fabbro, Doriano, Jaken, Susan
Protein kinase C (PKC) is the major cellular receptor for tumor promoting phorbol esters. Phorbol esters activate α-, β-, δ- and є-PKCs in GH4C1 rat pituitary cells and cause their...
The protein kinases of GH3 cells / (1980)
Thesis (doctoral)--Universität Basel, 1980.
Monia, Brett P., Sasmor, Henri, Johnston, Joseph F., Freier, Susan M., Lesnik, Elena A., Muller, Marcel, ...
To determine the mechanism of action responsible for the in vivo antitumor activity of a phosphorothioate antisense inhibitor targeted against human C-raf kinase (ISIS 5132, also known as CGP69846A),...
Chen, Jing, Wall, Nathan R., Kocher, Kerry, Duclos, Nicole, Fabbro, Doriano, Neuberg, Donna, ...
Small molecule inhibitors, such as imatinib, are effective therapies for tyrosine kinase fusions BCR-ABL–TEL-PDGFβR–mediated human leukemias, but resistance may develop. The unique fusion...
Chen, Jing, DeAngelo, Daniel J., Kutok, Jeffery L., Williams, Ifor R., Lee, Benjamin H., Wadleigh, Martha, ...
Human stem cell leukemia-lymphoma syndrome usually presents itself as a myeloproliferative disorder (MPD) that evolves to acute myeloid leukemia and/or lymphoma. The syndrome associated with...
Sarno, Stefania, De Moliner, Erika, Ruzzene, Maria, Pagano, Mario A, Battistutta, Roberto, Bain, Jenny, ...
IQA [[5-oxo-5,6-dihydro-indolo(1,2-a)quinazolin-7-yl]acetic acid] is a novel ATP/GTP site-directed inhibitor of CK2 ('casein kinase 2'), a pleiotropic and constitutively active protein kinase whose...
Monia, Brett P., Sasmor, Henri, Johnston, Joseph F., Freier, Susan M., Lesnik, Elena A., Muller, Marcel, ...
To determine the mechanism of action responsible for the in vivo antitumor activity of a phosphorothioate antisense inhibitor targeted against human C-raf kinase (ISIS 5132, also known as CGP69846A),...
Chen, Jing, Wall, Nathan R., Kocher, Kerry, Duclos, Nicole, Fabbro, Doriano, Neuberg, Donna, ...
Small molecule inhibitors, such as imatinib, are effective therapies for tyrosine kinase fusions BCR-ABL–TEL-PDGFβR–mediated human leukemias, but resistance may develop. The unique fusion...
Chen, Jing, DeAngelo, Daniel J., Kutok, Jeffery L., Williams, Ifor R., Lee, Benjamin H., Wadleigh, Martha, ...
Human stem cell leukemia-lymphoma syndrome usually presents itself as a myeloproliferative disorder (MPD) that evolves to acute myeloid leukemia and/or lymphoma. The syndrome associated with...
Sarno, Stefania, De Moliner, Erika, Ruzzene, Maria, Pagano, Mario A, Battistutta, Roberto, Bain, Jenny, ...
IQA [[5-oxo-5,6-dihydro-indolo(1,2-a)quinazolin-7-yl]acetic acid] is a novel ATP/GTP site-directed inhibitor of CK2 ('casein kinase 2'), a pleiotropic and constitutively active protein kinase whose...
Seo, Man Seong, Kwak, Nohoon, Ozaki, Hiroaki, Yamada, Haruhiko, Okamoto, Naoyuki, Yamada, Eri, ...
The most common cause of new blindness in young patients is retinal neovascularization, and in the elderly is choroidal neovascularization. Therefore, there has been a great deal of attention focused...
Growney, Joseph D., Clark, Jennifer J., Adelsperger, Jennifer, Stone, Richard, Fabbro, Doriano, Griffin, James D., ...
Constitutively activated forms of the transmembrane receptor tyrosine kinase c-KIT have been associated with systemic mast cell disease, acute myeloid leukemia, and gastrointestinal stromal tumors....
Stover, Elizabeth H., Chen, Jing, Lee, Benjamin H., Cools, Jan, McDowell, Elizabeth, Adelsperger, Jennifer, ...
AMN107 is a small molecule tyrosine kinase inhibitor developed, in the first instance, as a potent inhibitor of breakpoint cluster region-abelson (BCR-ABL). We tested its effectiveness against fusion...
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias
Weisberg, Ellen, Catley, Laurie, Wright, Renee D., Moreno, Daisy, Banerji, Lolita, Ray, Arghya, ...
Drug resistance resulting from emergence of imatinib-resistant BCR-ABL point mutations is a significant problem in advanced-stage chronic myelogenous leukemia (CML). The BCR-ABL inhibitor, nilotinib...
Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia
Cowan-Jacob, Sandra W., Fendrich, Gabriele, Floersheimer, Andreas, Furet, Pascal, Liebetanz, Janis, Rummel, Gabriele, ...
A case study showing how the determination of multiple cocrystal structures of the protein tyrosine kinase c-Abl was used to support drug discovery, resulting in a compound effective in the treatment...