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 …
been identified, including the large family of protein kinases, which function as components …
Trends in kinase drug discovery: targets, indications and inhibitor design
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 …
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 …
pharmacological research, especially for cancer, due to their critical roles in cellular …
The specificities of protein kinase inhibitors: an update
We have previously examined the specificities of 28 commercially available compounds,
reported to be relatively selective inhibitors of particular serine/threonine-specific protein …
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 …
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 …
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 …
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
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 …
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 …
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 …
from cancer inflammatory diseases, diabetes, infectious diseases, and cardiovascular …