[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] Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update

R Roskoski Jr - Pharmacological research, 2024 - 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 …

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] Deucravacitinib is an allosteric TYK2 protein kinase inhibitor FDA-approved for the treatment of psoriasis

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Psoriasis is a heterogeneous, inflammatory, autoimmune skin disease that affects up to 2%
of the world's population. There are many treatment modalities including topical medicines …

[HTML][HTML] The importance of the pyrazole scaffold in the design of protein kinases inhibitors as targeted anticancer therapies

GM Nitulescu, G Stancov, OC Seremet, G Nitulescu… - Molecules, 2023 - mdpi.com
The altered activation or overexpression of protein kinases (PKs) is a major subject of
research in oncology and their inhibition using small molecules, protein kinases inhibitors …

[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 …

Annual review of PROTAC degraders as anticancer agents in 2022

X Wang, ZL Qin, N Li, MQ Jia, QG Liu, YR Bai… - European Journal of …, 2024 - Elsevier
Following nearly two decades of development, significant advancements have been
achieved in PROTAC technology. As of the end of 2022, more than 20 drugs have entered …

[HTML][HTML] Acid-sensing ion channel 1: potential therapeutic target for tumor

Y Wang, H Zhou, Y Sun, Y Huang - Biomedicine & Pharmacotherapy, 2022 - Elsevier
Acidic extracellular pH is a major characteristic of tumor tissue, studies suggest that the local
pH value of malignant tumor tissues is between 6.0 and 6.9. Acid-sensing ion channel 1 …

[HTML][HTML] Cost in the United States of FDA-approved small molecule protein kinase inhibitors used in the treatment of neoplastic and non-neoplastic diseases

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 …

[HTML][HTML] Combination immune checkpoint and targeted protein kinase inhibitors for the treatment of renal cell carcinomas

R Roskoski Jr - Pharmacological Research, 2024 - Elsevier
Kidney cancers comprise about 3% of all new malignancies in the United States. Renal cell
carcinomas (RCCs) are the most common type of renal malignancy making up about 85% of …