Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
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 …

[HTML][HTML] 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 …

The NCI-MATCH trial: lessons for precision oncology

PJ O'Dwyer, RJ Gray, KT Flaherty, AP Chen, S Li… - Nature medicine, 2023 - nature.com
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 …

[HTML][HTML] Resistance to tyrosine kinase inhibitors in chronic myeloid leukemia—from molecular mechanisms to clinical relevance

R Alves, AC Gonçalves, S Rutella, AM Almeida… - Cancers, 2021 - mdpi.com
Simple Summary Chronic myeloid leukemia (CML) is a myeloproliferative neoplasia
associated with a molecular alteration, the fusion gene BCR-ABL1, that encodes the tyrosine …

[HTML][HTML] 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 …

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 …

Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry

R Gondru, Y Li, J Banothu - European Journal of Medicinal Chemistry, 2022 - Elsevier
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 …

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 …

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 …

[PDF][PDF] Tailored tyrosine kinase inhibitor (TKI) treatment of chronic myeloid leukemia (CML) based on current evidence.

R Çiftçiler, IC Haznedaroglu - European Review for Medical & …, 2021 - europeanreview.org
Philadelphia (Ph*)/BCR-ABL1-positive chronic myeloid leukemia (CML) is a neoplastic
hematologic disorder, which is a functionally curable chronic disease via using tyrosine …