WNT Signaling in Cardiac and Vascular Disease DOI Creative Commons
Sébastien Foulquier, Evangelos P. Daskalopoulos, Gentian Lluri

et al.

Pharmacological Reviews, Journal Year: 2017, Volume and Issue: 70(1), P. 68 - 141

Published: Dec. 15, 2017

WNT signaling is an elaborate and complex collection of signal transduction pathways mediated by multiple molecules. critically important for developmental processes, including cell proliferation, differentiation tissue patterning. Little activity present in the cardiovascular system healthy adults, but reactivation pathway observed many pathologies heart blood vessels. The high prevalence these their significant contribution to human disease burden has raised interest as a potential target therapeutic intervention. In this review, we first will focus on constituents regulation different routes. Subsequently, role development addressed, followed detailed discussion its involvement vascular cardiac disease. After highlighting crosstalk between WNT, transforming growth factor-β angiotensin II signaling, emerging stem cells, provide overview drugs targeting at levels. From combined studies conclude that, despite sometimes conflicting experimental data, general picture that excessive stimulation adversely affects pathology. rapidly increasing interfering levels allow evaluation interventions relevant animal models diseases eventually patients near future, translating outcomes preclinical into clinically context.

Language: Английский

The selectivity of protein kinase inhibitors: a further update DOI

Jenny Bain,

Lorna Plater,

Matt Elliott

et al.

Biochemical Journal, Journal Year: 2007, Volume and Issue: 408(3), P. 297 - 315

Published: Nov. 28, 2007

The specificities of 65 compounds reported to be relatively specific inhibitors protein kinases have been profiled against a panel 70–80 kinases. On the basis this information, effects that we studied in cells and other data literature, recommend use following small-molecule inhibitors: SB 203580/SB202190 BIRB 0796 used parallel assess physiological roles p38 MAPK (mitogen-activated kinase) isoforms, PI-103 wortmannin inhibit phosphatidylinositol (phosphoinositide) 3-kinases, PP1 or PP2 with Src-I1 (Src inhibitor-1) Src family members; PD 184352 0325901 MKK1 (MAPK kinase-1) plus MKK5, Akt-I-1/2 activation PKB (protein kinase B/Akt), rapamycin TORC1 [mTOR (mammalian target rapamycin)–raptor (regulatory associated mTOR) complex], CT 99021 GSK3 (glycogen synthase 3), BI-D1870 SL0101 FMK (fluoromethylketone) RSK (ribosomal S6 kinase), D4476 CK1 (casein 1), VX680 Aurora kinases, roscovitine as pan-CDK (cyclin-dependent inhibitor. We also identified harmine potent inhibitor DYRK1A (dual-specificity tyrosine-phosphorylated -regulated 1A) vitro. results further emphasized need for considerable caution using these enzymes. Despite being widely, many analysed were too non-specific useful conclusions made, than exclude involvement particular cellular processes.

Language: Английский

Citations

2474
Impact of Natural Products on Developing New Anti-Cancer Agents DOI
Gordon M. Cragg,

Paul G. Grothaus,

David Newman

et al.

Chemical Reviews, Journal Year: 2009, Volume and Issue: 109(7), P. 3012 - 3043

Published: May 7, 2009

ADVERTISEMENT RETURN TO ISSUEPREVReviewNEXTImpact of Natural Products on Developing New Anti-Cancer Agents†Gordon M. Cragg, Paul G. Grothaus, and David J. Newman*View Author Information Branch, Developmental Therapeutics Program, Division Cancer Treatment Diagnosis, NCI−Frederick, Fairview Center, Suite 206, P.O. Box B, Frederick, Maryland 21702-1201* To whom correspondence should be addressed. E-mail: [email protected]†This manuscript reflects the opinion authors, not necessarily those United States Government.Cite this: Chem. Rev. 2009, 109, 7, 3012–3043Publication Date (Web):May 2009Publication History Received16 January 2009Published online7 May inissue 8 July 2009https://pubs.acs.org/doi/10.1021/cr900019jhttps://doi.org/10.1021/cr900019jreview-articleACS PublicationsCopyright © This article subject to U.S. Copyright. Published 2009 by American Chemical SocietyRequest reuse permissionsArticle Views24433Altmetric-Citations991LEARN ABOUT THESE METRICSArticle Views are COUNTER-compliant sum full text downloads since November 2008 (both PDF HTML) across all institutions individuals. These metrics regularly updated reflect usage leading up last few days.Citations number other articles citing this article, calculated Crossref daily. Find more information about citation counts.The Altmetric Attention Score is a quantitative measure attention that research has received online. Clicking donut icon will load page at altmetric.com with additional details score social media presence for given article. how calculated. Share Add toView InAdd Full Text ReferenceAdd Description ExportRISCitationCitation abstractCitation referencesMore Options onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose SUBJECTS:Assays,Inhibitors,Peptides proteins,Pharmaceuticals,Polarization Get e-Alerts

Language: Английский

Citations

1239
The crucial role of protein phosphorylation in cell signaling and its use as targeted therapy (Review) DOI Creative Commons

Fatima Ardito,

Michele Giuliani,

D. Perrone

et al.

International Journal of Molecular Medicine, Journal Year: 2017, Volume and Issue: 40(2), P. 271 - 280

Published: June 22, 2017

Protein phosphorylation is an impo-rtant cellular regulatory mechanism as many enzymes and receptors are activated/deactivated by dephosphorylation events, means of kinases phosph-atases. In particular, the protein responsible for transduction signaling their hyperactivity, malfunction or overexpression can be found in several diseases, mostly tumors. Therefore, it evident that use kinase inhibitors valuable treatment cancer. this review, we discuss action phosphorylation, with particular attention to importance under physiological pathological conditions. We also possibility using

Language: Английский

Citations

1078
Kinase drug discovery 20 years after imatinib: progress and future directions DOI Open Access
Philip Cohen, Darren A.E. Cross, Pasi A. Jänne

et al.

Nature Reviews Drug Discovery, Journal Year: 2021, Volume and Issue: 20(7), P. 551 - 569

Published: May 17, 2021

Language: Английский

Citations

783
Role that phosphorylation of GSK3 plays in insulin and Wnt signalling defined by knockin analysis DOI Open Access

Edward J. McManus,

Kei Sakamoto,

Laura J Armit

et al.

The EMBO Journal, Journal Year: 2005, Volume and Issue: 24(8), P. 1571 - 1583

Published: March 24, 2005

Language: Английский

Citations

587
Pharmacological inhibitors of glycogen synthase kinase 3 DOI
Laurent Meijer,

M FLAJOLET,

Paul Greengard

et al.

Trends in Pharmacological Sciences, Journal Year: 2004, Volume and Issue: 25(9), P. 471 - 480

Published: Aug. 4, 2004

Language: Английский

Citations

580
Tau protein kinases: Involvement in Alzheimer's disease DOI
Ludovic Martin, Xénia Latypova, Cornelia M. Wilson

et al.

Ageing Research Reviews, Journal Year: 2012, Volume and Issue: 12(1), P. 289 - 309

Published: June 26, 2012

Language: Английский

Citations

563
Hyperphosphorylation of Microtubule-Associated Protein Tau: A Promising Therapeutic Target for Alzheimer Disease DOI
Cheng‐Xin Gong, Khalid Iqbal

Current Medicinal Chemistry, Journal Year: 2008, Volume and Issue: 15(23), P. 2321 - 2328

Published: Sept. 29, 2008

Alzheimer disease (AD) is the most common cause of dementia in adults. The current therapy for AD has only moderate efficacy controlling symptoms, and it does not cure disease. Recent studies have suggested that abnormal hyperphosphorylation tau brain plays a vital role molecular pathogenesis neurodegeneration. This article reviews advances understanding protein, regulation phosphorylation, its neurofibrillary degeneration. Furthermore, several therapeutic strategies treating on basis important are described. These include (1) inhibition glycogen synthase kinase-3β (GSK-3β), cyclin-dependent kinase 5 (cdk5), other kinases; (2) restoration PP2A activity; (3) targeting O-GlcNAcylation. Development drugs these likely to lead disease-modifying therapies AD.

Language: Английский

Citations

553
Paths to stemness: building the ultimate antitumour T cell DOI
Luca Gattinoni, Christopher A. Klebanoff, Nicholas P. Restifo

et al.

Nature reviews. Cancer, Journal Year: 2012, Volume and Issue: 12(10), P. 671 - 684

Published: Sept. 21, 2012

Language: Английский

Citations

543
Is Alzheimer's disease a Type 3 Diabetes? A critical appraisal DOI
Ramesh Kandimalla,

Vani Thirumala,

P. Hemachandra Reddy

et al.

Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, Journal Year: 2016, Volume and Issue: 1863(5), P. 1078 - 1089

Published: Aug. 30, 2016

Language: Английский

Citations

536