Protein kinases as targets for anticancer agents: from inhibitors to useful drugs

D Fabbro, S Ruetz, E Buchdunger… - Pharmacology & …, 2002 - Elsevier
Many components of mitogenic signaling pathways in normal and neoplastic cells have
been identified, including the large family of protein kinases, which function as components …

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 …

FDA-approved small-molecule kinase inhibitors

P Wu, TE Nielsen, MH Clausen - Trends in pharmacological sciences, 2015 - cell.com
Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …

The specificities of protein kinase inhibitors: an update

J Bain, H McLauchlan, M Elliott, P Cohen - Biochemical Journal, 2003 - portlandpress.com
We have previously examined the specificities of 28 commercially available compounds,
reported to be relatively selective inhibitors of particular serine/threonine-specific protein …

Small-molecule inhibitors binding to protein kinases. Part I: exceptions from the traditional pharmacophore approach of type I inhibition

AC Backes, B Zech, B Felber, B Klebl… - Expert Opinion on Drug …, 2008 - Taylor & Francis
Background: Protein kinases are essential enzymes propagating cellular signal transduction
processes and consequently have emerged as central targets for drug discovery against a …

Protein kinase inhibitors: emerging pharmacophores 1997-2000

J Dumas - Expert Opinion on Therapeutic Patents, 2001 - Taylor & Francis
Kinase inhibition is a major area for therapeutic intervention against a variety of diseases
including cancer, inflammatory disorders and diabetes. While this mode of action remains …

Tyrosine kinase inhibitors in cancer therapy

S Madhusudan, TS Ganesan - Clinical biochemistry, 2004 - Elsevier
Cancer is the second leading cause of death in the western world. Despite advances in
diagnosis and treatment, overall survival of patients remains poor. Scientific advances in …

Innovations and patent trends in the development of USFDA approved protein kinase inhibitors in the last two decades

M Imran, SMB Asdaq, SA Khan… - Pharmaceuticals, 2021 - mdpi.com
Protein kinase inhibitors (PKIs) are important therapeutic agents. As of 31 May 2021, the
United States Food and Drug Administration (USFDA) has approved 70 PKIs. Most of the …

Kinase inhibitors in cancer therapy: a look ahead

HH Sedlacek - Drugs, 2000 - Springer
The most essential kinases involved in cell membrane receptor activation, signal
transduction and cell cycle control or programmed cell death and their interconections are …

25 years of small molecular weight kinase inhibitors: potentials and limitations

D Fabbro - Molecular pharmacology, 2015 - ASPET
Deregulation of protein and lipid kinase activities leads to a variety of pathologies, ranging
from cancer inflammatory diseases, diabetes, infectious diseases, and cardiovascular …