Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance

M Azam, V Nardi, WC Shakespeare… - Proceedings of the …, 2006 - National Acad Sciences
… forms of ABL and SRC resemble one another, we tested two dual SRC-ABL kinase inhibitors,
AP23464 and PD166326, against 58 imatinib-resistant (IM R ) BCR/ABL kinase variants. …

Combined Abl inhibitor therapy for minimizing drug resistance in chronic myeloid leukemia: Src/Abl inhibitors are compatible with imatinib

T O'Hare, DK Walters, EP Stoffregen… - Clinical Cancer …, 2005 - AACR
… inhibitors are smaller than imatinib, contact fewer residues, and require fewer AblSrc/Abl
inhibitors should inhibit most imatinib-resistant mutants and showed previously that two Src/Abl

Evidence that resistance to nilotinib may be due to BCR-ABL, Pgp, or Src kinase overexpression

FX Mahon, S Hayette, V Lagarde, F Belloc, B Turcq… - Cancer research, 2008 - AACR
… Two Src kinase inhibitors (PP1 and PP2) partially removed resistance but did not significantly
inhibit Bcr-Abl … In contrast, dasatinib, a dual Bcr-Abl and Src kinase inhibitor, inhibited the …

Kinase inhibitors and cytotoxic drug resistance

S Grant, P Dent - Clinical cancer research, 2004 - AACR
… For example, the constitutively activated Bcr/abl kinase, a mutant form of Abl, a nonreceptor
… that Src inhibitors could circumvent cytotoxic drug resistance stemming from increased drug

Novel dual Src/Abl inhibitors for hematologic and solid malignancies

S Schenone, C Brullo, F Musumeci… - … on investigational drugs, 2010 - Taylor & Francis
… AZD0530 monotherapy initially retarded xenograft growth, but drug resistance rapidly
emerged, while the combined regimen anastrozole/AZD0530 reduced drug resistance and …

[PDF][PDF] Paradoxical activation of c-Src as a drug-resistant mechanism

M Higuchi, K Ishiyama, M Maruoka, R Kanamori… - Cell Reports, 2021 - cell.com
… c-Src is one of the target molecules for anti-cancer kinase inhibitors, yet the precise mechanism
by which c-Src confers drug resistance … cell-edge translocation of c-Abl, we proposed that …

[HTML][HTML] Novel Src/Abl tyrosine kinase inhibitor bosutinib suppresses neuroblastoma growth via inhibiting Src/Abl signaling

S Bieerkehazhi, Z Chen, Y Zhao, Y Yu, H Zhang… - Oncotarget, 2017 - ncbi.nlm.nih.gov
… Mechanistically, bosutinib effectively decreased the activity of Src/Abl and PI3K/AKT/mTOR, …
that Src and c-Abl are potential therapeutic targets in NB and that the novel Src/Abl inhibitor …

Second-generation Src/Abl inhibitor bosutinib effectively induces apoptosis in human esophageal squamous cell carcinoma (ESCC) cells via inhibiting Src/Abl …

YNE Ha, Y Dai, D Wufuer, M Pidayi, G Anasihan… - …, 2020 - search.ebscohost.com
… In summary, our results reveal that Src and Abl are potential therapeutic targets in ESCC …
drug like doxorubicin (Dox). Taken together, our results suggest that Src and Abl are potential …

Targeted CML therapy: controlling drug resistance, seeking cure

T O'Hare, AS Corbin, BJ Druker - Current opinion in genetics & …, 2006 - Elsevier
… kinase [21], dasatinib is predicted to bind to the active conformation, which is more structurally
conserved between ABL and SRC kinases than is the inactive conformation [21]. This …

Last findings on dual inhibitors of abl and SRC tyrosine-kinases

S Schenone, F Manetti, M Botta - Mini Reviews in Medicinal …, 2007 - ingentaconnect.com
Src is increased in hematopoietic cells expressing Bcr-Abl … classical Bcr-Abl inhibitors, various
dual Src/Abl inhibitors have … and delaying the onset of acquired drug resistance [123, 94]. …