Mechanisms of resistance to ABL kinase inhibition in chronic myeloid leukemia and the development of next generation ABL kinase inhibitors

AB Patel, T O'Hare… - Hematology/Oncology …, 2017 - hemonc.theclinics.com
Every year, more than 8000 new cases of chronic myeloid leukemia (CML) are diagnosed in
the United States. 1 BCR-ABL1, a fusion protein kinase derived from a reciprocal …

The role of new tyrosine kinase inhibitors in chronic myeloid leukemia

PA Pophali, MM Patnaik - The Cancer Journal, 2016 - journals.lww.com
Imatinib mesylate was the first tyrosine kinase inhibitor (TKI) approved for the management
of chronic myeloid leukemia. Imatinib produces acceptable responses in approximately 60 …

Dual allosteric inhibition of SHP2 phosphatase

M Fodor, E Price, P Wang, H Lu, A Argintaru… - ACS chemical …, 2018 - ACS Publications
SHP2 is a cytoplasmic protein tyrosine phosphatase encoded by the PTPN11 gene and is
involved in cell proliferation, differentiation, and survival. Recently, we reported an allosteric …

Designing drugs and chemical probes with the dualsteric approach

J Zha, J He, C Wu, M Zhang, X Liu… - Chemical Society Reviews, 2023 - pubs.rsc.org
Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

[HTML][HTML] Strategies to overcome drug resistance using SHP2 inhibitors

M Liu, S Gao, RM Elhassan, X Hou, H Fang - Acta Pharmaceutica Sinica B, 2021 - Elsevier
Encoded by PTPN11, the SHP2 (Src homology-2 domain-containing protein tyrosine
phosphatase-2) is widely recognized as a carcinogenic phosphatase. As a promising anti …

Current challenges in clinical development of “targeted therapies”: the case of acute myeloid leukemia

E Estey, RL Levine, B Löwenberg - Blood, The Journal of the …, 2015 - ashpublications.org
A fundamental difficulty in testing “targeted therapies” in acute myeloid leukemia (AML) is
the limitations of preclinical models in capturing inter-and intrapatient genomic …

Control of Ph+ and additional chromosomal abnormalities in chronic myeloid leukemia by tyrosine kinase inhibitors

S Ansari, M Verma - Medical Oncology, 2023 - Springer
Chronic myeloid leukemia (CML) is a type of blood cancer that is known to affect
hematopoietic stem cells. The presence of the Philadelphia chromosome (Ph+) is the major …

Identification and inhibition of the druggable allosteric site of SARS-CoV-2 NSP10/NSP16 methyltransferase through computational approaches

S Faisal, SL Badshah, B Kubra, M Sharaf, AH Emwas… - Molecules, 2022 - mdpi.com
Since its emergence in early 2019, the respiratory infectious virus, SARS-CoV-2, has
ravaged the health of millions of people globally and has affected almost every sphere of …

Resistance in chronic myeloid leukemia: definitions and novel therapeutic agents

C Talati, J Pinilla-Ibarz - Current Opinion in Hematology, 2018 - journals.lww.com
We categorize the resistance into BCR–ABL-dependent and BCR–ABL-independent
subgroups to further describe the complex molecular pathways which can potentially serve …

[HTML][HTML] The new allosteric inhibitor asciminib is susceptible to resistance mediated by ABCB1 and ABCG2 overexpression in vitro

LN Eadie, VA Saunders, S Branford, DL White… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Abstract Asciminib (previously ABL001), which binds the myristate-binding pocket of the Bcr-
Abl kinase domain, is in phase I clinical trials as monotherapy and in combination with …