Kinase-targeted cancer therapies: progress, challenges and future directions

KS Bhullar, NO Lagarón, EM McGowan, I Parmar… - Molecular cancer, 2018 - Springer
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

Is target-based drug discovery efficient? Discovery and “off-target” mechanisms of all drugs

A Sadri - Journal of medicinal chemistry, 2023 - ACS Publications
Target-based drug discovery is the dominant paradigm of drug discovery; however, a
comprehensive evaluation of its real-world efficiency is lacking. Here, a manual systematic …

Clinical and biological implications of target occupancy in CLL treated with the BTK inhibitor acalabrutinib

C Sun, P Nierman, EK Kendall… - Blood, The Journal …, 2020 - ashpublications.org
Inhibition of the B-cell receptor pathway, and specifically of Bruton tyrosine kinase (BTK), is a
leading therapeutic strategy in B-cell malignancies, including chronic lymphocytic leukemia …

Bruton's tyrosine kinase (BTK) as a promising target in solid tumors

J Molina-Cerrillo, T Alonso-Gordoa, P Gajate… - Cancer Treatment …, 2017 - Elsevier
Bruton's tyrosine kinase (BTK) is a non-receptor intracellular kinase that belongs to the TEC-
family tyrosine kinases together with bone marrow-expressed kinase (BMX), redundant …

Turning liabilities into opportunities: Off-target based drug repurposing in cancer

V Palve, Y Liao, LLR Rix, U Rix - Seminars in cancer biology, 2021 - Elsevier
Targeted drugs and precision medicine have transformed the landscape of cancer therapy
and significantly improved patient outcomes in many cases. However, as therapies are …

Resisting the Resistance: Navigating BTK Mutations in Chronic Lymphocytic Leukemia (CLL)

A Chirino, S Montoya, A Safronenka, J Taylor - Genes, 2023 - mdpi.com
Bruton's tyrosine kinase (BTK) plays a key role in the B-cell receptor (BCR) signaling
pathway and confers anti-apoptotic and proliferative properties to malignant B-cells in …

Ibrutinib reverses IL-6-induced osimertinib resistance through inhibition of Laminin α5/FAK signaling

L Li, Z Li, C Lu, J Li, K Zhang, C Lin, X Tang… - Communications …, 2022 - nature.com
Osimertinib, a 3rd generation epidermal growth factor receptor tyrosine kinase inhibitor
(EGFR-TKI), is the first-line standard-of-care for EGFR-mutant non-small cell lung cancer …

Novel indications for Bruton's tyrosine kinase inhibitors, beyond hematological malignancies

R Campbell, G Chong, EA Hawkes - Journal of clinical medicine, 2018 - mdpi.com
Bruton's tyrosine kinase (BTK) is a critical terminal enzyme in the B-cell antigen receptor
(BCR) pathway. BTK activation has been implicated in the pathogenesis of certain B-cell …

Auranofin enhances Ibrutinib's anticancer activity in EGFR-mutant lung adenocarcinoma

J Hu, H Zhang, M Cao, L Wang, S Wu, B Fang - Molecular cancer …, 2018 - AACR
We previously found that ibrutinib has anticancer activity in EGFR-mutant non–small cell
lung cancer (NSCLC). One of our recent studies showed that auranofin, a gold complex that …

MicroRNA-214 targets PTK6 to inhibit tumorigenic potential and increase drug sensitivity of prostate cancer cells

P Cagle, S Niture, A Srivastava, M Ramalinga… - Scientific reports, 2019 - nature.com
Prostate cancer is the most commonly diagnosed cancer in men with African American men
disproportionally suffering from the burden of this disease. Biomarkers that could …