[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

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] Signaling pathways in rheumatoid arthritis: implications for targeted therapy

Q Ding, W Hu, R Wang, Q Yang, M Zhu, M Li… - Signal transduction and …, 2023 - nature.com
Rheumatoid arthritis (RA) is an incurable systemic autoimmune disease. Disease
progression leads to joint deformity and associated loss of function, which significantly …

[HTML][HTML] Payload diversification: a key step in the development of antibody–drug conjugates

L Conilh, L Sadilkova, W Viricel, C Dumontet - Journal of Hematology & …, 2023 - Springer
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that
currently combines the selectivity of monoclonal antibodies with the potency of a payload …

Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Recent advances in the treatment of IBD: Targets, mechanisms and related therapies

J Liu, B Di, L Xu - Cytokine & Growth Factor Reviews, 2023 - Elsevier
Inflammatory bowel disease (IBD), as a representative inflammatory disease, currently has
multiple effective treatment options available and new therapeutic strategies are being …

[HTML][HTML] PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …

[HTML][HTML] Toll-like receptor signalling in B cells during systemic lupus erythematosus

S Fillatreau, B Manfroi, T Dörner - Nature Reviews Rheumatology, 2021 - nature.com
B lymphocytes have a central role in autoimmune diseases, which are often defined by
specific autoantibody patterns and feature a loss of B cell tolerance. A prototypic disease …

[HTML][HTML] Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor therapy

Y Liu, Y Li, Y Wang, C Lin, D Zhang, J Chen… - Journal of Hematology & …, 2022 - Springer
Vascular endothelial growth factor receptors (VEGFRs) are a family of receptor protein
tyrosine kinases that play an important role in the regulation of tumor-induced angiogenesis …

[HTML][HTML] Mapping the degradable kinome provides a resource for expedited degrader development

KA Donovan, FM Ferguson, JW Bushman, NA Eleuteri… - Cell, 2020 - cell.com
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …