[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 …

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 …

[HTML][HTML] A comprehensive overview of globally approved JAK inhibitors

AM Shawky, FA Almalki, AN Abdalla, AH Abdelazeem… - Pharmaceutics, 2022 - mdpi.com
Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …

[HTML][HTML] Anti-rheumatoid drugs advancements: New insights into the molecular treatment of rheumatoid arthritis

RB Mrid, N Bouchmaa, H Ainani, R El Fatimy… - Biomedicine & …, 2022 - Elsevier
Rheumatoid arthritis (RA) is one of more than 100 types of arthritis. This chronic autoimmune
disorder affects the lining of synovial joints in about 0.5% of people and may induce severe …

[HTML][HTML] Rule of five violations among the FDA-approved small molecule protein kinase inhibitors

R Roskoski Jr - Pharmacological Research, 2023 - Elsevier
Because genetic alterations including mutations, overexpression, translocations, and
dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this …

Lessons learned from past cyclin-dependent kinase drug discovery efforts

Z Xie, S Hou, X Yang, Y Duan, J Han… - Journal of Medicinal …, 2022 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) has become an effective therapeutic strategy
for treating various diseases, especially cancer. Over almost three decades, although great …

[PDF][PDF] Small molecule protein kinase inhibitors approved by regulatory agencies outside of the United States

R Roskoski Jr - Pharmacol. Res, 2023 - researchgate.net
Owing to genetic alterations and overexpression, the dysregulation of protein kinases plays
a significant role in the pathogenesis of many autoimmune and neoplastic disorders and …

[HTML][HTML] Treatment of autoimmunity: the impact of disease-modifying therapies in multiple sclerosis and comorbid autoimmune disorders

FF Konen, N Möhn, T Witte, M Schefzyk, M Wiestler… - Autoimmunity …, 2023 - Elsevier
More than 10 disease-modifying therapies (DMT) are approved by the European Medicines
Agency (EMA) and the US Food and Drug Administration (FDA) for the treatment of multiple …

Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies

R Roskoski Jr - Pharmacological Research, 2021 - Elsevier
The discovery of the phosphatidylinositol 3-kinase (PI 3-kinase) pathway was a major
advance in understanding eukaryotic signal transduction. The high frequency of PI 3-kinase …