Results 21 to 30 of about 98,172 (269)

Allosteric inhibition of BCR-ABL [PDF]

Cell Cycle, 2010
Impaired regulation of kinase activity can lead to a variety of diseases, including cancer. Inhibition of kinase activity has, therefore, been considered an attractive anti-cancer therapeutic strategy. The success of targeted therapy with kinase inhibitors has been well documented with BCR-ABL, where imatinib specifically inhibits kinase activity with ...
Sreenath V. Sharma, Markus Warmuth, A. Quamrul Hassan   +2 more
openaire   +3 more sources

A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL

bioRxiv, 2020
Targeted protein degradation (TPD) and proteolysis-targeting chimeras (PROTACs) have arisen as powerful therapeutic modalities for degrading specific protein targets in a proteasome-dependent manner.
Bingqi Tong, Jessica N. Spradlin, Luiz F. T. Novaes, Erika Zhang, Xirui Hu, M. Moeller, S. Brittain, L. McGregor, J. McKenna, John A. Tallarico, M. Schirle, T. Maimone, Daniel K. Nomura   +12 more
semanticscholar   +1 more source

Interactions of CBL with BCR-ABL and CRKL in BCR-ABL-transformed Myeloid Cells [PDF]

Journal of Biological Chemistry, 1997
The Philadelphia chromosome, detected in virtually all cases of chronic myelogenous leukemia (CML), is formed by a reciprocal translocation between chromosomes 9 and 22 that fuses BCR-encoded sequences upstream of exon 2 of c-ABL. The BCR-ABL fusion creates a gene whose protein product, p210BCR-ABL, has been implicated as the cause of the disease ...
Tsukasa Oda, Sayuri Ohno-Jones, Conor Heaney, Kathryn S. Kolibaba, Brian J. Druker, Arun Bhat   +5 more
openaire   +3 more sources

Small interfering RNA against BCR-ABL transcripts sensitize mutated T315I cells to nilotinib

Haematologica, 2010
Background Selective inhibition of the BCR-ABL tyrosine kinase by RNA interference has been demonstrated in leukemic cells. We, therefore, evaluated specific BCR-ABL small interfering RNA silencing in BCR-ABL-positive cell lines, including those ...
Michael Koldehoff, Lambros Kordelas, Dietrich W. Beelen, Ahmet H. Elmaagacli   +3 more
doaj   +1 more source

Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia.

New England Journal of Medicine, 2001
BACKGROUND BCR-ABL is a constitutively activated tyrosine kinase that causes chronic myeloid leukemia (CML). Since tyrosine kinase activity is essential to the transforming function of BCR-ABL, an inhibitor of the kinase could be an effective treatment ...
B. Druker, M. Talpaz, D. Resta, B. Peng, E. Buchdunger, J. Ford, N. Lydon, H. Kantarjian, R. Capdeville, Sayuri Ohno-Jones, C. Sawyers   +10 more
semanticscholar   +1 more source

Expression of BCR/ABL p210 from a Knockin Allele Enhances Bone Marrow Engraftment without Inducing Neoplasia

Cell Reports, 2013
Chronic myeloid leukemia (CML) and some acute lymphoblastic leukemias are characterized by the t(9;22) chromosome, which encodes the BCR/ABL oncogene. Multiple mouse models of CML express BCR/ABL at high levels from non-Bcr promoters, resulting in the ...
Samantha B. Foley, Zacariah L. Hildenbrand, Abigail A. Soyombo, Jeffery A. Magee, Yipin Wu, Katherine I. Oravecz-Wilson, Theodora S. Ross   +6 more
doaj   +1 more source

Sensitive detection of pre-existing BCR-ABL kinase domain mutations in CD34+ cells of newly diagnosed chronic-phase chronic myeloid leukemia patients is associated with imatinib resistance: implications in the post-imatinib era. [PDF]

PLoS ONE, 2013
BACKGROUND: BCR-ABL kinase domain mutations are infrequently detected in newly diagnosed chronic-phase chronic myeloid leukemia (CML) patients. Recent studies indicate the presence of pre-existing BCR-ABL mutations in a higher percentage of CML patients ...
Zafar Iqbal, Aamer Aleem, Mudassar Iqbal, Mubashar Iqbal Naqvi, Ammara Gill, Abid Sohail Taj, Abdul Qayyum, Najeeb ur-Rehman, Ahmad Mukhtar Khalid, Ijaz Hussain Shah, Muhammad Khalid, Riazul Haq, Mahwish Khan, Shahid Mahmood Baig, Abid Jamil, Muhammad Naeem Abbas, Muhammad Absar, Amer Mahmood, Mahmood Rasool, Tanveer Akhtar   +19 more
doaj   +1 more source

Effect of HSP90AB1 and CC domain interaction on Bcr-Abl protein cytoplasm localization and function in chronic myeloid leukemia cells

Cell Communication and Signaling, 2021
Background The fusion oncoprotein Bcr-Abl is mostly located in the cytoplasm, which causes chronic myeloid leukemia (CML). After moving into the nucleus, the fusion protein can induce apoptosis of CML cells.
Yuhang Peng, Zhenglan Huang, Fangzhu Zhou, Teng Wang, Ke Mou, Wenli Feng   +5 more
doaj   +1 more source

Suppression of autophagy by BCR ABL

Frontiers in Bioscience, 2012
Imatinib and second generation BCR/ABL tyrosine kinase inhibitors (TKIs) serve now as standard therapies for patients with chronic myelogenous leukemia (CML); however, CML stem cells are intrinsically insensitive to the cell death-inducing effects of TKIs, allowing the persistence of a "reservoir" of BCR/ABL-expressing CML-initiating cells potentially ...
CALABRETTA, Bruno, SALOMONI, Paolo
openaire   +5 more sources

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

Angewandte Chemie, 2016
Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative therapeutic strategy with the potential to address many of the challenges currently faced in modern drug development programs.
Ashton C Lai, M. Toure, D. Hellerschmied, J. Salami, S. Jaime-Figueroa, Eunhwa Ko, J. Hines, C. Crews   +7 more
semanticscholar   +1 more source