[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 …

[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] A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models

F Ren, A Aliper, J Chen, H Zhao, S Rao, C Kuppe… - Nature …, 2024 - nature.com
Idiopathic pulmonary fibrosis (IPF) is an aggressive interstitial lung disease with a high
mortality rate. Putative drug targets in IPF have failed to translate into effective therapies at …

[HTML][HTML] Protein kinases: drug targets for immunological disorders

L Castelo-Soccio, H Kim, M Gadina… - Nature Reviews …, 2023 - nature.com
Protein kinases play a major role in cellular activation processes, including signal
transduction by diverse immunoreceptors. Given their roles in cell growth and death and in …

[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 …

Targeting the PI3K/AKT/mTOR signaling pathway in the treatment of human diseases: Current status, trends, and solutions

J Huang, L Chen, J Wu, D Ai, JQ Zhang… - Journal of medicinal …, 2022 - ACS Publications
The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …

Janus kinase (JAK) inhibitors in the treatment of neoplastic and inflammatory disorders

R Roskoski Jr - Pharmacological Research, 2022 - Elsevier
The Janus kinase (JAK) family of nonreceptor protein-tyrosine kinases consists of JAK1,
JAK2, JAK3, and TYK2 (Tyrosine Kinase 2). Each of these proteins contains a JAK …

[HTML][HTML] Signaling pathway and small-molecule drug discovery of FGFR: A comprehensive review

J Zheng, W Zhang, L Li, Y He, Y Wei, Y Dang… - Frontiers in …, 2022 - frontiersin.org
The targeted therapy is a groundbreaking innovation in cancer treatment. Among the
receptor tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered enormous …

Harnessing systematic protein–ligand interaction fingerprints for drug discovery

Z Zhao, PE Bourne - Drug Discovery Today, 2022 - Elsevier
Highlights•Review of function-site interaction fingerprints for drug discovery.•Study of the
polypharmacology of kinase inhibitors.•Kinase allosteric and covalent inhibitors.Determining …

[HTML][HTML] Fluorine-a small magic bullet atom in the drug development: perspective to FDA approved and COVID-19 recommended drugs

G Chandra, DV Singh, GK Mahato, S Patel - Chemical Papers, 2023 - Springer
During the last twenty years, organic fluorination chemistry established itself as an important
tool to get a biologically active compound. This belief can be supported by the fact that every …