Results 21 to 30 of about 4,627,885 (297)

Fast in-vitro screening of FLT3-ITD inhibitors using silkworm-baculovirus protein expression system.

PLoS ONE, 2022
We report expression and purification of a FLT3 protein with ITD mutation (FLT3-ITD) with a steady tyrosine kinase activity using a silkworm-baculovirus system, and its application as a fast screening system of tyrosine kinase inhibitors.
Naoki Yamamoto, Jiro Kikuchi, Yusuke Furukawa, Naoya Shibayama   +3 more
doaj   +1 more source

From PERK to RIPK1: Design, synthesis and evaluation of novel potent and selective necroptosis inhibitors

Frontiers in Chemistry, 2023
Receptor-Interacting serine/threonine-Protein Kinase 1 (RIPK1) emerged as an important driver of inflammation and, consequently, inflammatory pathologies.
Camilla Scarpellini, Sophie Valembois, Kenneth Goossens, Mike Vadi, Mike Vadi, Caroline Lanthier, Greta Klejborowska, Pieter Van Der Veken, Hans De Winter, Mathieu J. M. Bertrand, Mathieu J. M. Bertrand, Koen Augustyns   +11 more
doaj   +1 more source

Protein Kinase Inhibitors

Folia Biologica, 2006
Since protein kinases have been found to be implicated in many diseases, first of all malignancies, they are considered as promising therapeutic targets. Many protein kinase inhibitors have been designed by now. These molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. Some protein
I, Shchemelinin, L, Sefc, E, Necas
openaire   +2 more sources

Bivalent inhibitors of protein kinases [PDF]

Critical Reviews in Biochemistry and Molecular Biology, 2014
Protein kinases are key players in a large number of cellular signaling pathways. Dysregulated kinase activity has been implicated in a number of diseases, and members of this enzyme family are of therapeutic interest. However, due to the fact that most inhibitors interact with the highly conserved ATP-binding sites of kinases, it is a significant ...
Carrie M, Gower, Matthew E K, Chang, Dustin J, Maly   +2 more
openaire   +2 more sources

High throughput screens yield small molecule inhibitors of Leishmania CRK3:CYC6 cyclin-dependent kinase [PDF]

, 2011
<p><b>Background:</b> <i>Leishmania</i> species are parasitic protozoa that have a tightly controlled cell cycle, regulated by cyclin-dependent kinases (CDKs).
Mottram Jeremy C., Thomson, Graeme, Mottram, JC, Grant Karen M., Turner, N.J., Malcolm D. Walkinshaw, Malone, Kirk, Turner, Nicholas J., Nicholas J Turner, Jeremy C. Mottram, Karen M. Grant, Walker, Roderick G., Kita, K, Graeme Thomson, Malone Kirk, Karen M Grant, Grant, Karen, Nicholas J. Turner, Walker, RG, Nowicki, Matthew W., Thomson Graeme, Walkinshaw, M.D., Walkinshaw Malcolm D., David G. Blake, David G Blake, Walker Roderick G., Brown, Elaine, Brown Elaine, Blake David G., Brown, E, Malone, K, Turner Nicholas J., Walkinshaw, MD, Blake, DG, Matthew W. Nowicki, Walker, R.G., Malone, K., Blake, David G., Elaine Brown, Mottram, J.C., Kirk Malone, Walkinshaw, Malcolm D., Matthew W Nowicki, Nowicki, MW, Brown, E., Nowicki Matthew W., Turner, Nicholas J.; id_orcid, Grant, Karen M., Grant, K.M., Mottram, Jeremy C., Roderick G Walker, Thomson, G, Jeremy C Mottram, Roderick G. Walker, Nowicki, M.W., Grant, KM, Blake, D.G., Malcolm D Walkinshaw, Turner, NJ, Thomson, G.   +59 more
core   +2 more sources

Combinatorial strategy using protein kinase inhibitors and a cytotoxic compound for highly resistant glioblastoma cells : "in vitro studies" [PDF]

, 2007
Glioblastoma multiforme (GBM) is the most frequent and the most aggesssive malignant neoplasm of the human central nervous system (CNS), with a median survival of less than one year. These neoplasms are radio- and chemo-resistant, and are highly invasive,
Failly, Mike
core   +1 more source

Role of protein kinase C in renal vasoconstriction caused by angiotensin II [PDF]

, 1990
In this study we have examined the subcellar pathways along which angiotensin II (ANG II) causes renal vasoconstriction. Using the isolated perfused rat kidney model, we found that renal vasoconstriction produced by ANG II (100 pM) was not altered by the
Kurtz, Armin, Scholz, H., A. Kurtz, H. Scholz   +3 more
core   +1 more source

On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine [PDF]

, 2009
Protein kinases are important regulatory enzymes in signal transduction and in cell regulation. Understanding inhibition mechanisms of kinases is important for the further development of new therapies for cancer and inflammatory diseases.
William R. Pitt, Duangrudee Tanramluk, Tom L. Blundell, Adrian Schreyer   +3 more
core   +2 more sources

Is inhibition of kinase activity the only therapeutic strategy for LRRK2-associated Parkinson's disease?

BMC Medicine, 2012
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are a common cause of familial Parkinson's disease (PD). Variation around the LRRK2 locus also contributes to the risk of sporadic PD.
Rudenko Iakov N, Chia Ruth, Cookson Mark R   +2 more
doaj   +1 more source

Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome. [PDF]

PLoS ONE, 2017
Protein kinases are critical drug targets for treating a large variety of human diseases. Type-III kinase inhibitors have attracted increasing attention as highly selective therapeutics.
Zheng Zhao, Lei Xie, Philip E Bourne
doaj   +1 more source