-
1
-
-
0037205048
-
The phosphoinositide 3-kinase pathway
-
Cantley, L. C. The phosphoinositide 3-kinase pathway Science 2002, 296, 1655-1657 10.1126/science.296.5573.1655
-
(2002)
Science
, vol.296
, pp. 1655-1657
-
-
Cantley, L.C.1
-
2
-
-
77951621262
-
The emerging mechanisms of isoform-specific PI3K signalling
-
Vanhaesebroeck, B.; Guillermet-Guibert, J.; Graupera, M.; Bilanges, B. The emerging mechanisms of isoform-specific PI3K signalling Nat. Rev. Mol. Cell Biol. 2010, 11, 329-341 10.1038/nrm2882
-
(2010)
Nat. Rev. Mol. Cell Biol.
, vol.11
, pp. 329-341
-
-
Vanhaesebroeck, B.1
Guillermet-Guibert, J.2
Graupera, M.3
Bilanges, B.4
-
3
-
-
84867091296
-
Inhibition of PI3K signaling spurs new therapeutic opportunities in inflammatory/autoimmune diseases and hematological malignancies
-
Foster, J. G.; Blunt, M. D.; Carter, E.; Ward, S. G. Inhibition of PI3K signaling spurs new therapeutic opportunities in inflammatory/autoimmune diseases and hematological malignancies Pharmacol. Rev. 2012, 64, 1027-1054 10.1124/pr.110.004051
-
(2012)
Pharmacol. Rev.
, vol.64
, pp. 1027-1054
-
-
Foster, J.G.1
Blunt, M.D.2
Carter, E.3
Ward, S.G.4
-
4
-
-
33746257209
-
The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism
-
Engelman, J. A.; Luo, J.; Cantley, L. C. The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism Nat. Rev. Genet. 2006, 7, 606-619 10.1038/nrg1879
-
(2006)
Nat. Rev. Genet.
, vol.7
, pp. 606-619
-
-
Engelman, J.A.1
Luo, J.2
Cantley, L.C.3
-
5
-
-
79955577250
-
Small-molecule inhibitors of the PI3K signaling network
-
McNamara, C. R.; Degterev, A. Small-molecule inhibitors of the PI3K signaling network Future Med. Chem. 2011, 3, 549-565 10.4155/fmc.11.12
-
(2011)
Future Med. Chem.
, vol.3
, pp. 549-565
-
-
McNamara, C.R.1
Degterev, A.2
-
6
-
-
84863073430
-
Targeting phosphoinositide 3-kinase δ for allergic asthma
-
Rowan, W. C.; Smith, J. L.; Affleck, K.; Amour, A. Targeting phosphoinositide 3-kinase δ for allergic asthma Biochem. Soc. Trans. 2012, 40, 240-245 10.1042/BST20110665
-
(2012)
Biochem. Soc. Trans.
, vol.40
, pp. 240-245
-
-
Rowan, W.C.1
Smith, J.L.2
Affleck, K.3
Amour, A.4
-
7
-
-
84875644704
-
Targeting phosphoinositide 3-kinase δ for the treatment of respiratory diseases
-
Sriskantharajah, S.; Hamblin, N.; Worsley, S.; Calver, A. R.; Hessel, E. M.; Amour, A. Targeting phosphoinositide 3-kinase δ for the treatment of respiratory diseases Ann. N. Y. Acad. Sci. 2013, 1280, 35-39 10.1111/nyas.12039
-
(2013)
Ann. N. Y. Acad. Sci.
, vol.1280
, pp. 35-39
-
-
Sriskantharajah, S.1
Hamblin, N.2
Worsley, S.3
Calver, A.R.4
Hessel, E.M.5
Amour, A.6
-
8
-
-
84906314487
-
PI3K inhibitors as potential therapeutics for autoimmune disease
-
Ball, J.; Archer, S.; Ward, S. PI3K inhibitors as potential therapeutics for autoimmune disease Drug Discovery Today 2014, 19, 1195-1199 10.1016/j.drudis.2014.04.002
-
(2014)
Drug Discovery Today
, vol.19
, pp. 1195-1199
-
-
Ball, J.1
Archer, S.2
Ward, S.3
-
9
-
-
16244393685
-
Signalling by PI3K isoforms: Insights from gene-targeted mice
-
Vanhaesebroeck, B.; Ali, K.; Bilancio, A.; Geering, B.; Foukas, L. C. Signalling by PI3K isoforms: insights from gene-targeted mice Trends Biochem. Sci. 2005, 30, 194-204 10.1016/j.tibs.2005.02.008
-
(2005)
Trends Biochem. Sci.
, vol.30
, pp. 194-204
-
-
Vanhaesebroeck, B.1
Ali, K.2
Bilancio, A.3
Geering, B.4
Foukas, L.C.5
-
10
-
-
33750525089
-
PI3Kγ inhibition: Towards an 'aspirin of the 21st century'?
-
Rückle, T.; Schwarz, M. K.; Rommel, C. PI3Kγ inhibition: towards an 'aspirin of the 21st century'? Nat. Rev. Drug Discovery 2006, 5, 903-918 10.1038/nrd2145
-
(2006)
Nat. Rev. Drug Discovery
, vol.5
, pp. 903-918
-
-
Rückle, T.1
Schwarz, M.K.2
Rommel, C.3
-
11
-
-
84899850988
-
Picking the point of inhibition: A comparative review of PI3K/AKT/mTOR pathway inhibitors
-
Dienstmann, R.; Rodon, J.; Serra, V.; Tabernero, J. Picking the point of inhibition: A comparative review of PI3K/AKT/mTOR pathway inhibitors Mol. Cancer Ther. 2014, 13, 1021-1031 10.1158/1535-7163.MCT-13-0639
-
(2014)
Mol. Cancer Ther.
, vol.13
, pp. 1021-1031
-
-
Dienstmann, R.1
Rodon, J.2
Serra, V.3
Tabernero, J.4
-
12
-
-
33750796968
-
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase
-
Bamborough, P.; Christopher, J. A.; Cutler, G. J.; Dickson, M. C.; Mellor, G. W.; Morey, J. V.; Patel, C. B.; Shewchuk, L. M. 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase Bioorg. Med. Chem. Lett. 2006, 16, 6236-6240 10.1016/j.bmcl.2006.09.018
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 6236-6240
-
-
Bamborough, P.1
Christopher, J.A.2
Cutler, G.J.3
Dickson, M.C.4
Mellor, G.W.5
Morey, J.V.6
Patel, C.B.7
Shewchuk, L.M.8
-
13
-
-
33846076698
-
Degree of throat deposition can explain the variability in lung deposition of inhaled drugs
-
Borgström, L.; Olsson, B.; Thorsson, L. Degree of throat deposition can explain the variability in lung deposition of inhaled drugs J. Aerosol Med. 2006, 19, 473-483 10.1089/jam.2006.19.473
-
(2006)
J. Aerosol Med.
, vol.19
, pp. 473-483
-
-
Borgström, L.1
Olsson, B.2
Thorsson, L.3
-
14
-
-
33645079631
-
Evaluation of the chemiluminescent nitrogen detector for solubility determinations to support drug discovery
-
Bhattachar, S. N.; Wesley, J. A.; Seadeek, C. Evaluation of the chemiluminescent nitrogen detector for solubility determinations to support drug discovery J. Pharm. Biomed. Anal. 2006, 41, 152-157 10.1016/j.jpba.2005.11.009
-
(2006)
J. Pharm. Biomed. Anal.
, vol.41
, pp. 152-157
-
-
Bhattachar, S.N.1
Wesley, J.A.2
Seadeek, C.3
-
15
-
-
84942240048
-
-
version 4.0; Biobyte Corp. Claremont, CA
-
ClogP, version 4.0; Biobyte Corp.: Claremont, CA; http://www.biobyte.com/index.html.
-
ClogP
-
-
-
16
-
-
84862167093
-
Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
-
Sutherlin, D. P.; Baker, S.; Bisconte, A.; Blaney, P. M.; Brown, A.; Chan, B. K.; Chantry, D.; Castanedo, G.; DePledge, P.; Goldsmith, P.; Goldstein, D. M.; Hancox, T.; Kaur, J.; Knowles, D.; Kondru, R.; Lesnick, J.; Lucas, M. C.; Lewis, C.; Murray, J.; Nadin, A. J.; Nonomiya, J.; Pang, J.; Pegg, N.; Price, S.; Reif, K.; Safina, B. S.; Salphati, L.; Staben, S.; Seward, E. M.; Shuttleworth, S.; Sohal, S.; Sweeney, Z. K.; Ultsch, M.; Waszkowycz, B.; Wei, B. Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf Bioorg. Med. Chem. Lett. 2012, 22, 4296-4302 10.1016/j.bmcl.2012.05.027
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 4296-4302
-
-
Sutherlin, D.P.1
Baker, S.2
Bisconte, A.3
Blaney, P.M.4
Brown, A.5
Chan, B.K.6
Chantry, D.7
Castanedo, G.8
DePledge, P.9
Goldsmith, P.10
Goldstein, D.M.11
Hancox, T.12
Kaur, J.13
Knowles, D.14
Kondru, R.15
Lesnick, J.16
Lucas, M.C.17
Lewis, C.18
Murray, J.19
Nadin, A.J.20
Nonomiya, J.21
Pang, J.22
Pegg, N.23
Price, S.24
Reif, K.25
Safina, B.S.26
Salphati, L.27
Staben, S.28
Seward, E.M.29
Shuttleworth, S.30
Sohal, S.31
Sweeney, Z.K.32
Ultsch, M.33
Waszkowycz, B.34
Wei, B.35
more..
-
18
-
-
84872541214
-
Reactive metabolites in the biotransformation of molecules containing a furan ring
-
Peterson, L. A. Reactive metabolites in the biotransformation of molecules containing a furan ring Chem. Res. Toxicol. 2013, 26, 6-25 10.1021/tx3003824
-
(2013)
Chem. Res. Toxicol.
, vol.26
, pp. 6-25
-
-
Peterson, L.A.1
-
19
-
-
0034730616
-
A novel method for measurement of submembrane ATP concentration
-
Gribble, F. M.; Loussouarn, G.; Tucker, S. J.; Zhao, C.; Nichols, C. G.; Ashcroft, F. M. A novel method for measurement of submembrane ATP concentration J. Biol. Chem. 2000, 275, 30046-30049 10.1074/jbc.M001010200
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 30046-30049
-
-
Gribble, F.M.1
Loussouarn, G.2
Tucker, S.J.3
Zhao, C.4
Nichols, C.G.5
Ashcroft, F.M.6
-
20
-
-
84942261507
-
-
EMD Millipore Corporation
-
EMD Millipore Corporation. http://www.merckmillipore.com.
-
-
-
-
21
-
-
84898048432
-
2 receptor agonist with rapid onset of action
-
2 receptor agonist with rapid onset of action ACS Med. Chem. Lett. 2014, 5, 416-421 10.1021/ml4005232
-
(2014)
ACS Med. Chem. Lett.
, vol.5
, pp. 416-421
-
-
Stocks, M.J.1
Alcaraz, L.2
Bailey, A.3
Bonnert, R.4
Cadogan, E.5
Christie, J.6
Dixon, J.7
Connolly, S.8
Cook, A.9
Fisher, A.10
Flaherty, A.11
Humphries, A.12
Ingall, A.13
Jordan, S.14
Lawson, M.15
Mullen, A.16
Nicholls, D.17
Paine, S.18
Pairaudeau, G.19
Young, A.20
more..
-
22
-
-
33750998518
-
Common pharmacophores for uncharged human ether-a-go-go-related gene (hERG) blockers
-
Aronov, A. M. Common pharmacophores for uncharged human ether-a-go-go-related gene (hERG) blockers J. Med. Chem. 2006, 49, 6917-6921 10.1021/jm060500o
-
(2006)
J. Med. Chem.
, vol.49
, pp. 6917-6921
-
-
Aronov, A.M.1
-
23
-
-
77954638677
-
Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin
-
Knight, S. D.; Adams, N. D.; Burgess, J. L.; Chaudhari, A. M.; Darcy, M. G.; Donatelli, C. A.; Luengo, J. I.; Newlander, K. A.; Parrish, C. A.; Ridgers, L. H.; Sarpong, M. A.; Schmidt, S. J.; Van Aller, G. S.; Carson, J. D.; Diamond, M. A.; Elkins, P. A.; Gardiner, C. M.; Garver, E.; Gilbert, S. A.; Gontarek, R. R.; Jackson, J. R.; Kershner, K. L.; Luo, L.; Raha, K.; Sherk, C. S.; Sung, C.-M.; Sutton, D.; Tummino, P. J.; Wegrzyn, R. J.; Auger, K. R.; Dhanak, D. Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin ACS Med. Chem. Lett. 2010, 1, 39-43 10.1021/ml900028r
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, pp. 39-43
-
-
Knight, S.D.1
Adams, N.D.2
Burgess, J.L.3
Chaudhari, A.M.4
Darcy, M.G.5
Donatelli, C.A.6
Luengo, J.I.7
Newlander, K.A.8
Parrish, C.A.9
Ridgers, L.H.10
Sarpong, M.A.11
Schmidt, S.J.12
Van Aller, G.S.13
Carson, J.D.14
Diamond, M.A.15
Elkins, P.A.16
Gardiner, C.M.17
Garver, E.18
Gilbert, S.A.19
Gontarek, R.R.20
Jackson, J.R.21
Kershner, K.L.22
Luo, L.23
Raha, K.24
Sherk, C.S.25
Sung, C.-M.26
Sutton, D.27
Tummino, P.J.28
Wegrzyn, R.J.29
Auger, K.R.30
Dhanak, D.31
more..
-
24
-
-
75349106113
-
The p110δ structure: Mechanisms for selectivity and potency of new PI(3)K inhibitors
-
Berndt, A.; Miller, S.; Williams, O.; Le, D. D.; Houseman, B. T.; Pacold, J. I.; Gorrec, F.; Hon, W.-C.; Ren, P.; Liu, Y.; Rommel, C.; Gaillard, P.; Rückle, T.; Schwarz, M. K.; Shokat, K. M.; Shaw, J. P.; Williams, R. L. The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors Nat. Chem. Biol. 2010, 6, 117-124 10.1038/nchembio.293
-
(2010)
Nat. Chem. Biol.
, vol.6
, pp. 117-124
-
-
Berndt, A.1
Miller, S.2
Williams, O.3
Le, D.D.4
Houseman, B.T.5
Pacold, J.I.6
Gorrec, F.7
Hon, W.-C.8
Ren, P.9
Liu, Y.10
Rommel, C.11
Gaillard, P.12
Rückle, T.13
Schwarz, M.K.14
Shokat, K.M.15
Shaw, J.P.16
Williams, R.L.17
-
25
-
-
1942453243
-
Ligand efficiency: A useful metric for lead selection
-
Hopkins, A. L.; Groom, C. R.; Alex, A. Ligand efficiency: a useful metric for lead selection Drug Discovery Today 2004, 9, 430-431 10.1016/S1359-6446(04)03069-7
-
(2004)
Drug Discovery Today
, vol.9
, pp. 430-431
-
-
Hopkins, A.L.1
Groom, C.R.2
Alex, A.3
-
26
-
-
84874934753
-
Characterization of selective calcium-release activated calcium channel blockers in mast cells and T-cells from human, rat, mouse and Guinea-pig preparations
-
Rice, L. V.; Bax, H. J.; Russell, L. J.; Barrett, V. J.; Walton, S. E.; Deakin, A. M.; Thomson, S. A.; Lucas, F.; Solari, R.; House, D.; Begg, M. Characterization of selective calcium-release activated calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations Eur. J. Pharmacol. 2013, 704, 49-57 10.1016/j.ejphar.2013.02.022
-
(2013)
Eur. J. Pharmacol.
, vol.704
, pp. 49-57
-
-
Rice, L.V.1
Bax, H.J.2
Russell, L.J.3
Barrett, V.J.4
Walton, S.E.5
Deakin, A.M.6
Thomson, S.A.7
Lucas, F.8
Solari, R.9
House, D.10
Begg, M.11
-
27
-
-
33746294441
-
Blinded validation of the isolated arterially perfused rabbit ventricular wedge in preclinical assessment of drug-induced proarrhythmias
-
Liu, T.; Brown, B. S.; Wu, Y.; Antzelevitch, C.; Kowey, P. R.; Yan, G. X. Blinded validation of the isolated arterially perfused rabbit ventricular wedge in preclinical assessment of drug-induced proarrhythmias Heart Rhythm 2006, 3, 948-956 10.1016/j.hrthm.2006.04.021
-
(2006)
Heart Rhythm
, vol.3
, pp. 948-956
-
-
Liu, T.1
Brown, B.S.2
Wu, Y.3
Antzelevitch, C.4
Kowey, P.R.5
Yan, G.X.6
|