Trends in kinase drug discovery: targets, indications and inhibitor design
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
Management of chronic myeloid leukemia in 2023–common ground and common sense
J Senapati, K Sasaki, GC Issa, JH Lipton… - Blood cancer …, 2023 - nature.com
With the improving knowledge of CML and its management, the goals of therapy need to be
revisited to ensure an optimal use of the BCR:: ABL1 TKIs in the frontline and later-line …
revisited to ensure an optimal use of the BCR:: ABL1 TKIs in the frontline and later-line …
The NCI-MATCH trial: lessons for precision oncology
Abstract The NCI-MATCH (Molecular Analysis for Therapy Choice) trial (NCT02465060) was
launched in 2015 as a genomically driven, signal-seeking precision medicine platform trial …
launched in 2015 as a genomically driven, signal-seeking precision medicine platform trial …
Resistance to tyrosine kinase inhibitors in chronic myeloid leukemia—from molecular mechanisms to clinical relevance
Simple Summary Chronic myeloid leukemia (CML) is a myeloproliferative neoplasia
associated with a molecular alteration, the fusion gene BCR-ABL1, that encodes the tyrosine …
associated with a molecular alteration, the fusion gene BCR-ABL1, that encodes the tyrosine …
A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo
A Kaneshige, L Bai, M Wang, D McEachern… - Nature Chemical …, 2023 - nature.com
Signal transducer and activator of transcription 5 (STAT5) is an attractive therapeutic target,
but successful targeting of STAT5 has proved to be difficult. Here we report the development …
but successful targeting of STAT5 has proved to be difficult. Here we report the development …
Pathogenesis and management of accelerated and blast phases of chronic myeloid leukemia
J Senapati, E Jabbour, H Kantarjian, NJ Short - Leukemia, 2023 - nature.com
The treatment of chronic myeloid leukemia (CML) with tyrosine kinase inhibitors (TKIs) has
been a model for cancer therapy development. Though most patients with CML have a …
been a model for cancer therapy development. Though most patients with CML have a …
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry
Coumarin and benzimidazole are privileged structures in medicinal chemistry and are
widely used in drug discovery and development due to their vast biological properties. The …
widely used in drug discovery and development due to their vast biological properties. The …
Third-line therapy for chronic myeloid leukemia: current status and future directions
J Cortes, F Lang - Journal of Hematology & Oncology, 2021 - Springer
Chronic myeloid leukemia (CML) is driven by the BCR-ABL1 fusion protein, formed by a
translocation between chromosomes 9 and 22 that creates the Philadelphia chromosome …
translocation between chromosomes 9 and 22 that creates the Philadelphia chromosome …
Long non-coding RNAs (lncRNAs); roles in tumorigenesis and potentials as biomarkers in cancer diagnosis
S Najafi, SH Khatami, M Khorsand, Z Jamali… - Experimental cell …, 2022 - Elsevier
New research has indicated that long non-coding RNAs (lncRNAs) play critical roles in a
broad range of biological processes, including the pathogenesis of many complex human …
broad range of biological processes, including the pathogenesis of many complex human …
Treatment‐free remission in patients with chronic myeloid leukemia following the discontinuation of tyrosine kinase inhibitors
Tyrosine kinase inhibitors (TKIs) discontinuation in patients with Philadelphia‐chromosome‐
positive chronic myeloid leukemia (Ph‐positive CML) is increasingly considered. We aim to …
positive chronic myeloid leukemia (Ph‐positive CML) is increasingly considered. We aim to …