Advances in covalent drug discovery
L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
Kinase drug discovery 20 years after imatinib: progress and future directions
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …
BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies
A Alu, H Lei, X Han, Y Wei, X Wei - Journal of Hematology & Oncology, 2022 - Springer
Bruton's tyrosine kinase (BTK) is an essential component of multiple signaling pathways that
regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising …
regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising …
Kinase inhibitors: the road ahead
FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …
Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology
M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
[PDF][PDF] Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor
MR Janes, J Zhang, LS Li, R Hansen, U Peters, X Guo… - Cell, 2018 - cell.com
Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …
[PDF][PDF] Treatment-induced tumor dormancy through YAP-mediated transcriptional reprogramming of the apoptotic pathway
Eradicating tumor dormancy that develops following epidermal growth factor receptor
(EGFR) tyrosine kinase inhibitor (TKI) treatment of EGFR-mutant non-small cell lung cancer …
(EGFR) tyrosine kinase inhibitor (TKI) treatment of EGFR-mutant non-small cell lung cancer …
The ascension of targeted covalent inhibitors
J Singh - Journal of Medicinal Chemistry, 2022 - ACS Publications
Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …
Advances in covalent kinase inhibitors
A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …
discovery. Covalency affords a unique set of advantages as well as challenges relative to …
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 …
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …