Sentences with phrase «small molecule inhibitors»
Small molecule inhibitors refer to a class of compounds that can bind to specific target proteins, such as enzymes or receptors, and block their activity. Full definition
An ideal model for the evaluation of small molecule inhibitors in two disease models simultaneously.
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Those features present significant challenges in drug discovery, and in fact, DNA - binding proteins traditionally have been considered to be beyond the reach of even small molecule inhibitors.
Unfortunately, not every gene product can be targeted with conventional small molecule inhibitors.
Vescor, advised by its scientific founders White and Kimmelman, whose research has shown inhibition of autophagy can dramatically impact tumor growth in pre-clinical models, will develop small molecule inhibitors of a number of protein targets at critical nodes of the autophagy cascade, perform investigational new drug (IND) enabling studies, and move these into clinical development.
To this end, we made use of two widely used small molecule inhibitors, PD98059 and SB203580.
CM4620 is a potent and selective small molecule inhibitor of calcium release - activated calcium (CRAC) channels.
Hu and his collaborator Juan R. Del Valle at the University of South Florida are developing novel small molecule inhibitors against IRE - 1 to combat cancers associated with high numbers of MDSCs.
He went on to a postdoctoral position with Dr. Iwao Ojima evaluating anti-tubercular compound series that inhibit the cell division protein FtsZ and screening computationally designed small molecule inhibitors of Botulinum neurotoxin.
His thesis work focused on developing novel small molecule inhibitors against protein targets such as survivin and STAT3 that are essential for progression and survival of cancer.
Professor Olson's lab has focused on characterizing how Rho GTPase signalling pathways contribute to cancer, with the ultimate goal of identifying critical elements that could be targeted with small molecule inhibitors.
Our team is currently developing methods that can be used to screen small molecule inhibitors of EDD1 and also looking into how the regulation of TIP60 levels can be translated into therapeutic advances for the treatment of viral - mediated cancers such as cervical cancer.
«Small molecule inhibitor shows promise in precision cancer targeting.»
By using pharmacological small molecule inhibitors as well as neutrophils from genetically modified mouse strains the team could identify essential receptor and signaling pathways involved in the nicotine - mediated activation of neutrophils.
Direct targeting of FKBP12 / YY1 with in vivo - morpholino approaches or small molecule inhibitors including GPI - 1046 were equally effective to induce ARNT expression with subsequent activation of ALK3 - dependent canonical BMP signaling responses and attenuated chronic organ failure in models of chronic kidney, but also cardiac and liver injuries.
Other major small molecule inhibitors used to study MRP4 activity (including MK - 571, dipyridamole and indomethacin) also target other related ABC transporter family members or inhibit the production, function or degradation of important MRP4 substrates.
Whilst the function of MRP4 has been advanced by MRP4 - / - mice and RNAi, until now the absence of specific small molecule inhibitors of MRP4 has been a major constraint.
«There are currently many exciting therapies including conventional chemotherapies, small molecule inhibitor tyrosine kinase inhibitors and immune modulating therapies under development in follicular lymphoma,» Westin told Cancer Network.
We discovered a potent small molecule inhibitor of furin which has proven useful both in bacterial diseases where furin activation is critical to toxin activation as well as in cancer pathogenesis.
She remained in Sheffield to complete a PhD and short post-doc in the lab of Professor Beining Chen, primarily working to screen and characterise small molecule inhibitors of anthrax toxins as part of a collaboration with the Health Protection Agency at Porton Down.
In more current, but not yet published work, Sattler is also fusing NMR and crystallography in a drug discovery project to find small molecule inhibitors that neutralize trypanosoma, parasites that cause sleeping sickness, by disrupting life - critical protein - protein interactions.
Evaluating the efficacy of repurposed small molecule inhibitors in treating filariasis using preclinical and clinical studies
Such a similarity makes TNFΔARE a unique model of a complex human pathology appropriate for the simoultaneous testing of novel therapeutics and small molecule inhibitors on two different pathologies.
It will provide a framework to design small molecule inhibitors of telomerase that may be of therapeutic value for cancer and other diseases associated with cellular aging.
This lab, in collaboration with the lab of Ruben Shaw at the Salk Institute, recently identified SBI - 0206965, the first potent and selective small molecule inhibitor of ULK1, a serine / threonine kinase that is a critical regulator of autophagy.
The authors also found that a novel small molecule inhibitor of the salvage pathway enzyme deoxycytidine kinase blocked leukemia growth in mice in combination with thymidine (to inhibit the de novo pathway).
Investigated TAM family receptor tyrosine kinase gene expression in response to small molecule inhibitors in glioblastoma multiforme
Our strategy is to identify basic mechanisms of proteins involved in metabolism and DNA repair to gain better understanding in disease and also develop small molecule inhibitors to selectively targeting these proteins as potential therapeutics.
iTeos is now developing EOS200271 which is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1), which has demonstrated the same anti-tumour activity in multiple preclinical tumour models in combination with immune checkpoint inhibitors as competitors, but also has demonstrated superior brain penetration.
The newly crafted molecule is non-toxic, simple to produce, and cost - effective compared to the production of alternate treatment strategies, such as antibodies and small molecule inhibitors.
Prior to the new study, however, no one had identified a small molecule inhibitor of RAD52.
turned into 10 years of systematic research to identify the enzyme PLK4 as a promising therapeutic target and develop a small molecule inhibitor to block it,» says Dr. Mak, Director of The Campbell Family Institute for Breast Cancer Research at the Princess Margaret Cancer Centre, University Health Network.
In a paper published today in Cancer Research, researchers: 1) identify a biomarker enzyme associated with aggressive glioma brain tumors, 2) reveal the regulatory mechanism for that enzyme, and 3) demonstrate potent efficacy, using a mouse model of glioma, for a small molecule inhibitor they have developed.
«If we could design a small molecule inhibitor that would look like heme - iron but would actually clog up a key metabolic pathway in bacteria, we may be able to get around the problem of antibiotic resistance,» suggests Dr. Mason, who adds that he and Dr. Justice plan to use the new five - year NIH grant to further studies of just such an inhibitor.
One possibility is to cut off bacteria's nutrient supply by blocking essential metabolic pathways with a small molecule inhibitor, essentially starving the bacteria to death.
Dr. Levitsky: Other sections under the Oncology Discovery and Translation Area (DTA) focus on anti-angiogenesis, small molecule inhibitors of the p53 pathway, apoptosis, signal transduction, and the tumor microenvironment.
Small Molecule Inhibitors of CXCR4 Bikash Debnath, Shili Xu, Fedora Grande, Antonio Garofalo, Nouri Neamati Theranostics 2013; 3 (1): 47 - 75.
«We are presently testing a number of biological and small molecule inhibitors of Notch3,» he said.
Finally, we show that addition of small molecule inhibitors of eIF2α dephosphorylation to muscle stem cell cultures permits their ex vivo expansion and engraftment into a preclinical mouse model of Duchenne muscular dystrophy.
The drug candidate is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) that also inhibits IDO1 in the tumor micro-environment to trigger immune - modulation.
IDO1 Inhibitor (EOS200271): Synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) to trigger immune - modulation in the tumor micro-environment.
Synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) to trigger immune - modulation in the tumor micro-environment.
The team is taking several approaches to inhibit HIF - 1 activity, including RNA interference, dominant negative constructs, and small molecule inhibitors.
A comprehensive review on Aurora kinase: small molecule inhibitors and clinical trial studies