Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis
CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …
including cancer, has fostered incremental efforts on drug discovery programs over the past …
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 United States. 1 BCR-ABL1, a fusion protein kinase derived from a reciprocal …
A clinician perspective on the treatment of chronic myeloid leukemia in the chronic phase
V García-Gutiérrez, M Breccia, E Jabbour… - Journal of Hematology & …, 2022 - Springer
Tyrosine kinase inhibitors (TKIs) have vastly improved long-term outcomes for patients with
chronic myeloid leukemia (CML). After imatinib (a first-generation TKI), second-and third …
chronic myeloid leukemia (CML). After imatinib (a first-generation TKI), second-and third …
[PDF][PDF] Small molecule protein kinase inhibitors approved by regulatory agencies outside of the United States
R Roskoski Jr - Pharmacol. Res, 2023 - researchgate.net
Owing to genetic alterations and overexpression, the dysregulation of protein kinases plays
a significant role in the pathogenesis of many autoimmune and neoplastic disorders and …
a significant role in the pathogenesis of many autoimmune and neoplastic disorders and …
[HTML][HTML] Chronic myeloid leukemia-from the Philadelphia chromosome to specific target drugs: A literature review
MM Sampaio, MLC Santos, HS Marques… - World journal of …, 2021 - ncbi.nlm.nih.gov
Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm and was the first
neoplastic disease associated with a well-defined genotypic anomaly―the presence of the …
neoplastic disease associated with a well-defined genotypic anomaly―the presence of the …
Protein tyrosine kinases: their roles and their targeting in leukemia
K K. Bhanumathy, A Balagopal, FS Vizeacoumar… - Cancers, 2021 - mdpi.com
Simple Summary Protein phosphorylation is a key regulatory mechanism that controls a
wide variety of cellular responses. This process is catalysed by the members of the protein …
wide variety of cellular responses. This process is catalysed by the members of the protein …
Approved and experimental small‐molecule oncology kinase inhibitor drugs: a mid‐2016 overview
PM Fischer - Medicinal research reviews, 2017 - Wiley Online Library
Kinase inhibitor research is a comparatively recent branch of medicinal chemistry and
pharmacology and the first small‐molecule kinase inhibitor, imatinib, was approved for …
pharmacology and the first small‐molecule kinase inhibitor, imatinib, was approved for …
The c-Abl inhibitor, Radotinib HCl, is neuroprotective in a preclinical Parkinson's disease mouse model
Accumulating evidence suggests that the non-receptor tyrosine kinase c-Abl plays an
important role in the progression of Parkinson's disease (PD) and c-Abl inhibition could be …
important role in the progression of Parkinson's disease (PD) and c-Abl inhibition could be …
Targeting c-KIT (CD117) by dasatinib and radotinib promotes acute myeloid leukemia cell death
SK Heo, EK Noh, JY Kim, YK Jeong, JC Jo, Y Choi… - Scientific reports, 2017 - nature.com
Dasatinib and radotinib are oral BCR-ABL tyrosine kinase inhibitors that were developed as
drugs for the treatment of chronic myeloid leukemia. We report here that the c-KIT (CD117) …
drugs for the treatment of chronic myeloid leukemia. We report here that the c-KIT (CD117) …
Phase III clinical trial (RERISE study) results of efficacy and safety of radotinib compared with imatinib in newly diagnosed chronic phase chronic myeloid leukemia
JY Kwak, SH Kim, SJ Oh, DY Zang, H Kim, JA Kim… - Clinical Cancer …, 2017 - AACR
Purpose: Radotinib is a second-generation BCR-ABL1 tyrosine kinase inhibitor (TKI)
approved in Korea for chronic phase chronic myeloid leukemia (CML-CP) in patients newly …
approved in Korea for chronic phase chronic myeloid leukemia (CML-CP) in patients newly …