Journal
BIOORGANIC CHEMISTRY
Volume 105, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104377
Keywords
BTK; HZ-A-005; Preclinical studies; Anti-proliferative activity; Stability; Safety
Funding
- Health Commission of Zhejiang Province [WJK-ZJ-1918, 2019KY365, 2019RC141]
- National Natural Science Funds of China [81803372]
- Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province [2019E10021]
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Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase, is a member of the Tec kinases family and is essential for B cell receptor (BCR) mediated signaling. BTK inhibitors such as ibrutinib hold a prominent role in the treatment of B cell malignancies. Here we disclose a potent, selective, and covalent BTK inhibitor, HZ-A-005, currently in preclinical development. HZ-A-005 demonstrated dose-dependent activity in two xenograft models of lymphoma in vivo. It showed highly favourable safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles in preclinical studies. On the basis of its potency, selectivity, and covalent mode of inhibition, HZ-A-005 reveals the potential to be a promising BTK inhibitor for a wide range of cancer indications.
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