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 …

Recently targeted kinases and their inhibitors—the path to clinical trials

S Knapp, M Sundström - Current opinion in pharmacology, 2014 - Elsevier
Highlights•Kinases constitute a very successful target area comprising now 28 approved
inhibitors.•Despite this success only few first in class kinase inhibitors entered clinical testing …

Type II kinase inhibitors: an opportunity in cancer for rational design

J Blanc, R Geney, C Menet - Anti-Cancer Agents in Medicinal …, 2013 - ingentaconnect.com
With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against
cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry …

Targeting cancer with small molecule kinase inhibitors

J Zhang, PL Yang, NS Gray - Nature reviews cancer, 2009 - nature.com
Deregulation of kinase activity has emerged as a major mechanism by which cancer cells
evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors …

Small molecule kinase inhibitors as anti-cancer therapeutics

O Chahrour, D Cairns, Z Omran - Mini reviews in medicinal …, 2012 - ingentaconnect.com
Protein kinases have emerged as the most important class of targets in oncology drug
discovery because of their major roles in regulating cellular growth and survival. At least, 11 …

Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

P Wu, TE Nielsen, MH Clausen - Drug discovery today, 2016 - Elsevier
Highlights•A dramatic increase in the approval of small molecule kinase inhibitors
(SMKIs).•The molecular weight of most approved SMKIs is in the range of 400–600.•The …

Targeting cancer with small-molecular-weight kinase inhibitors

D Fabbro, SW Cowan-Jacob, H Möbitz… - … inhibitors: methods and …, 2012 - Springer
Protein and lipid kinases fulfill essential roles in many signaling pathways that regulate
normal cell functions. Deregulation of these kinase activities lead to a variety of pathologies …

[图书][B] Targeting protein kinases for cancer therapy

DJ Matthews, ME Gerritsen - 2011 - books.google.com
An expert guide to targeting protein kinases in cancer therapy Research has shown that
protein kinases can instigate the formation and spread of cancer when they transmit faulty …

Protein kinases as targets for cancer treatment

G Giamas, J Stebbing, CE Vorgias… - …, 2007 - Taylor & Francis
In various types of malignancies, conventional forms of therapy (surgery, radiation and
chemotherapy) are often ineffective, as well as harmful. In the last few years, a convergence …

Kinase inhibitors: the reality behind the success

JY Jeon, A Sparreboom… - Clinical Pharmacology & …, 2017 - Wiley Online Library
Tremendous progress has been made by utilizing kinase inhibitors in oncology, and these
agents continue to pave the way into other areas of medicine. There are, however, many …