New approaches to the treatment of inflammatory disorders small molecule inhibitors of p38 MAP kinase

C Peifer, G Wagner, S Laufer - Current topics in medicinal …, 2006 - ingentaconnect.com
The therapy of chronic inflammatory diseases like rheumatoid arthritis (RA) and
inflammatory bowel disease (IBD) has recently been enriched by the successful launch of …

Biology of Aurora A kinase: implications in cancer manifestation and therapy

D Karthigeyan, SBB Prasad, J Shandilya… - Medicinal research …, 2011 - Wiley Online Library
The Aurora A kinase belongs to serine/threonine group of kinases, well known for its role in
cell cycle, especially in the regulation of mitosis. Numerous substrates of Aurora A kinase …

Rational design of inhibitors that bind to inactive kinase conformations

Y Liu, NS Gray - Nature chemical biology, 2006 - nature.com
The majority of kinase inhibitors that have been developed so far—known as type I inhibitors—
target the ATP binding site of the kinase in its active conformation, in which the activation …

Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring

PD Lyne, ML Lamb, JC Saeh - Journal of medicinal chemistry, 2006 - ACS Publications
The ability of molecular docking, using the program Glide and an MM-GBSA postdocking
scoring protocol, to correctly rank a number of congeneric kinase inhibitors was assessed …

A general strategy for creating “inactive-conformation” abl inhibitors

B Okram, A Nagle, FJ Adrián, C Lee, P Ren, X Wang… - Chemistry & biology, 2006 - cell.com
Kinase inhibitors that bind to the ATP cleft can be broadly classified into two groups: those
that bind exclusively to the ATP site with the kinase assuming a conformation otherwise …

An automated continuous-flow platform for the estimation of multistep reaction kinetics

BJ Reizman, KF Jensen - Organic Process Research & …, 2012 - ACS Publications
Automated continuous flow systems coupled with online analysis and feedback have been
previously demonstrated to model and optimize chemical syntheses with little a priori …

Inhibition of vascular smooth muscle and cancer cell proliferation by new VEGFR inhibitors and their immunomodulator effect: Design, synthesis, and biological …

F Ran, W Li, Y Qin, T Yu, Z Liu, M Zhou… - Oxidative medicine …, 2021 - Wiley Online Library
Abnormal vascular smooth muscle cell (VSMC) proliferation has an important role in the
pathogenesis of both atherosclerosis restenosis and hypertension. Vascular endothelial …

Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III 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 emerged as central targets for drug discovery against a wide …

[HTML][HTML] Novel uracil derivatives depicted potential anticancer agents: in vitro, molecular docking, and ADME study

S El-Kalyoubi, F Agili, I Adel, MA Tantawy - Arabian Journal of Chemistry, 2022 - Elsevier
Using a simple technique to prepare many uracil derivatives as Schiff base of uracil 4, bis 6-
amino [5-(1-(4-aryl) ethylidene) amino)] pyrimidine-2, 4-dione 5–12 by heating of 5, 6 …

[HTML][HTML] Small molecule recognition of c-Src via the Imatinib-binding conformation

AC Dar, MS Lopez, KM Shokat - Chemistry & biology, 2008 - cell.com
The cancer drug, Imatinib, is a selective Abl kinase inhibitor that does not inhibit the closely
related kinase c-Src. This one drug and its ability to selectively inhibit Abl over c-Src has …