New approaches to the treatment of inflammatory disorders small molecule inhibitors of p38 MAP kinase
The therapy of chronic inflammatory diseases like rheumatoid arthritis (RA) and
inflammatory bowel disease (IBD) has recently been enriched by the successful launch of …
inflammatory bowel disease (IBD) has recently been enriched by the successful launch of …
Biology of Aurora A kinase: implications in cancer manifestation and therapy
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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
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 …
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 …
related kinase c-Src. This one drug and its ability to selectively inhibit Abl over c-Src has …