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Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors

The phosphoinositide 3-kinases (PI3Ks) constitute an important family of lipid kinase enzymes that control a range of cellular processes through their regulation of a network of signal transduction pathways, and have emerged as important therapeutic targets in the context of cancer, inflammation and...

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Autores principales: Shuttleworth, S.J, Silva, F.A, Cecil, A.R.L, Tomassi, C.D, Hill, T.J, Raynaud, F.I, Clarke, P.A, Workman, P
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers Ltd 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3228236/
https://www.ncbi.nlm.nih.gov/pubmed/21649578
http://dx.doi.org/10.2174/092986711796011229
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author Shuttleworth, S.J
Silva, F.A
Cecil, A.R.L
Tomassi, C.D
Hill, T.J
Raynaud, F.I
Clarke, P.A
Workman, P
author_facet Shuttleworth, S.J
Silva, F.A
Cecil, A.R.L
Tomassi, C.D
Hill, T.J
Raynaud, F.I
Clarke, P.A
Workman, P
author_sort Shuttleworth, S.J
collection PubMed
description The phosphoinositide 3-kinases (PI3Ks) constitute an important family of lipid kinase enzymes that control a range of cellular processes through their regulation of a network of signal transduction pathways, and have emerged as important therapeutic targets in the context of cancer, inflammation and cardiovascular diseases. Since the mid-late 1990s, considerable progress has been made in the discovery and development of small molecule ATP-competitive PI3K inhibitors, a number of which have entered early phase human trials over recent years from which key clinical results are now being disclosed. This review summarizes progress made to date, primarily on the discovery and characterization of class I and dual class I/IV subtype inhibitors, together with advances that have been made in translational and clinical research, notably in cancer.
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spelling pubmed-32282362011-12-01 Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors Shuttleworth, S.J Silva, F.A Cecil, A.R.L Tomassi, C.D Hill, T.J Raynaud, F.I Clarke, P.A Workman, P Curr Med Chem Article The phosphoinositide 3-kinases (PI3Ks) constitute an important family of lipid kinase enzymes that control a range of cellular processes through their regulation of a network of signal transduction pathways, and have emerged as important therapeutic targets in the context of cancer, inflammation and cardiovascular diseases. Since the mid-late 1990s, considerable progress has been made in the discovery and development of small molecule ATP-competitive PI3K inhibitors, a number of which have entered early phase human trials over recent years from which key clinical results are now being disclosed. This review summarizes progress made to date, primarily on the discovery and characterization of class I and dual class I/IV subtype inhibitors, together with advances that have been made in translational and clinical research, notably in cancer. Bentham Science Publishers Ltd 2011-06 /pmc/articles/PMC3228236/ /pubmed/21649578 http://dx.doi.org/10.2174/092986711796011229 Text en © 2011 Bentham Science Publishers Ltd. http://creativecommons.org/licenses/by/2.5/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.5/), which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Article
Shuttleworth, S.J
Silva, F.A
Cecil, A.R.L
Tomassi, C.D
Hill, T.J
Raynaud, F.I
Clarke, P.A
Workman, P
Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title_full Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title_fullStr Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title_full_unstemmed Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title_short Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
title_sort progress in the preclinical discovery and clinical development of class i and dual class i/iv phosphoinositide 3-kinase (pi3k) inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3228236/
https://www.ncbi.nlm.nih.gov/pubmed/21649578
http://dx.doi.org/10.2174/092986711796011229
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