[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] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Molecular targeted therapy for anticancer treatment

HY Min, HY Lee - Experimental & molecular medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …

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 targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

The role of JAK/STAT signaling pathway and its inhibitors in diseases

P Xin, X Xu, C Deng, S Liu, Y Wang, X Zhou… - International …, 2020 - Elsevier
The JAK/STAT signaling pathway is an universally expressed intracellular signal
transduction pathway and involved in many crucial biological processes, including cell …

Protein tyrosine kinase inhibitor resistance in malignant tumors: molecular mechanisms and future perspective

Y Yang, S Li, Y Wang, Y Zhao, Q Li - Signal transduction and targeted …, 2022 - nature.com
Protein tyrosine kinases (PTKs) are a class of proteins with tyrosine kinase activity that
phosphorylate tyrosine residues of critical molecules in signaling pathways. Their basal …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

R Roskoski Jr - Pharmacological research, 2020 - Elsevier
Because genetic alterations including mutations, overexpression, translocations, and
dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this …

Emerging strategies to overcome resistance to third-generation EGFR inhibitors

K Shi, G Wang, J Pei, J Zhang, J Wang… - Journal of Hematology & …, 2022 - Springer
Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …