-
1
-
-
33746257209
-
The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism
-
DOI 10.1038/nrg1879, PII NRG1879
-
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 (Pubitemid 44100518)
-
(2006)
Nature Reviews Genetics
, vol.7
, Issue.8
, pp. 606-619
-
-
Engelman, J.A.1
Luo, J.2
Cantley, L.C.3
-
2
-
-
0035190026
-
Cellular function of phosphoinositide 3-Kinase: Implications for development, immunity, homeostasis, and cancer
-
DOI 10.1146/annurev.cellbio.17.1.615
-
Katso, R.; Okkenhaug, K.; Ahmadi, K.; White, S.; Timms, J. Cellular Function of Phosphoinositide 3-Kinases: Implications for Development, Homeostasis and Cancer Annu. Rev. Cell Dev. Biol. 2000, 17, 615-675 (Pubitemid 33096187)
-
(2001)
Annual Review of Cell and Developmental Biology
, vol.17
, pp. 615-675
-
-
Katso, R.1
Okkenhaug, K.2
Ahmadi, K.3
White, S.4
Timms, J.5
Waterfield, M.D.6
-
3
-
-
11144358645
-
High Frequency of Mutations of the PIK3CA Gene in Human Cancers
-
DOI 10.1126/science.1096502
-
Samuels, Y.; Wang, Z.; Bardelli, A.; Silliman, N.; Ptak, J.; Szabo, S.; Yan, H.; Gasdar, A.; Powell, S. M.; Riggins, G. J.; Willson, J. K.; Markowitz, S.; Kinzler, K. W.; Vogelstein, B.; Velculescu, V. E. High Frequency of Mutations of the PIK3CA Gene in Human Cancers Science 2004, 304, 554 (Pubitemid 38541907)
-
(2004)
Science
, vol.304
, Issue.5670
, pp. 554
-
-
Samuels, Y.1
Wang, Z.2
Bardelli, A.3
Silliman, N.4
Ptak, J.5
Szabo, S.6
Yan, H.7
Gazdar, A.8
Powell, S.M.9
Riggins, G.J.10
Willson, J.K.V.11
Markowitz, S.12
Kinzler, K.W.13
Vogelstein, B.14
Velculescu, V.E.15
-
4
-
-
4344684649
-
PTEN function: How normal cells control it and tumour cells lose it
-
DOI 10.1042/BJ20040825
-
Leslie, N. R.; Downes, C. P. PTEN Function: How Normal Cells Control it and Tumour Cells Lose it Biochem. J. 2004, 382, 1-11 (Pubitemid 39141560)
-
(2004)
Biochemical Journal
, vol.382
, Issue.1
, pp. 1-11
-
-
Leslie, N.R.1
Downes, C.P.2
-
5
-
-
68249093818
-
Targeting the Phosphoinositide 3-Kinase Pathway in Cancer
-
Liu, P.; Cheng, H.; Roberts, T. M.; Zhao, J. J. Targeting the Phosphoinositide 3-Kinase Pathway in Cancer Nat. Rev. Drug Discovery 2009, 8, 627-644
-
(2009)
Nat. Rev. Drug Discovery
, vol.8
, pp. 627-644
-
-
Liu, P.1
Cheng, H.2
Roberts, T.M.3
Zhao, J.J.4
-
6
-
-
84861668771
-
Emerging Therapies Based on Inhibitors of Phosphatidyl-Inositol-3-Kinases
-
In; Macor, J. E. Academic Press: Oxford
-
Nuss, J. M.; Tsuhako, A. L.; Anand, N. K. Emerging Therapies Based on Inhibitors of Phosphatidyl-Inositol-3-Kinases. In Annual Reports in Medicinal Chemistry; Macor, J. E., Ed.; Academic Press: Oxford, 2009; Vol. 44, pp 339-351.
-
(2009)
Annual Reports in Medicinal Chemistry
, vol.44
, pp. 339-351
-
-
Nuss, J.M.1
Tsuhako, A.L.2
Anand, N.K.3
-
7
-
-
51049109033
-
Identification and Characterization of NVP-BEZ235, a New Orally Available Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor with Potent in Vivo Antitumor Activity
-
Maira, S.-M.; Stauffer, F.; Brueggen, J.; Furet, P.; Schnell, C.; Fritsch, C.; Brachmann, S.; Chene, P.; De Pover, A.; Schoemaker, K.; Fabbro, D.; Gabriel, D.; Simonen, M.; Murphy, L.; Finan, P.; Sellers, W.; Garcia-Echeverria, C. Identification and Characterization of NVP-BEZ235, a New Orally Available Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor with Potent in Vivo Antitumor Activity Mol. Cancer Ther. 2008, 7, 1851-1863
-
(2008)
Mol. Cancer Ther.
, vol.7
, pp. 1851-1863
-
-
Maira, S.-M.1
Stauffer, F.2
Brueggen, J.3
Furet, P.4
Schnell, C.5
Fritsch, C.6
Brachmann, S.7
Chene, P.8
De Pover, A.9
Schoemaker, K.10
Fabbro, D.11
Gabriel, D.12
Simonen, M.13
Murphy, L.14
Finan, P.15
Sellers, W.16
Garcia-Echeverria, C.17
-
8
-
-
52449106253
-
The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin- 1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class i PI3 Kinase for the Treatment of Cancer
-
Folkes, A. J.; Ahmadi, K.; Alderton, W. K.; Alix, S.; Baker, S. J.; Box, G.; Chuckowree, I. S.; Clarke, P. A.; Depledge, P.; Eccles, S. A.; Friedman, L. S.; Hayes, A.; Hancox, T. C.; Kugendradas, A.; Lensun, L.; Moore, P.; Olivero, A. G.; Pang, J.; Patel, S.; Pergl-Wilson, G. H.; Raynaud, F. I.; Robson, A.; Saghir, N.; Salphati, L.; Sohal, S.; Ultsch, M. H.; Valenti, M.; Wallweber, H. J. A.; Wan, N. C.; Wiesmann, C.; Workman, P.; Zhyvoloup, A.; Zvelebil, M. J.; Shuttleworth, S. J. The Identification of 2-(1H-Indazol-4-yl)-6-(4- methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer J. Med. Chem. 2008, 51, 5522-5532
-
(2008)
J. Med. Chem.
, vol.51
, pp. 5522-5532
-
-
Folkes, A.J.1
Ahmadi, K.2
Alderton, W.K.3
Alix, S.4
Baker, S.J.5
Box, G.6
Chuckowree, I.S.7
Clarke, P.A.8
Depledge, P.9
Eccles, S.A.10
Friedman, L.S.11
Hayes, A.12
Hancox, T.C.13
Kugendradas, A.14
Lensun, L.15
Moore, P.16
Olivero, A.G.17
Pang, J.18
Patel, S.19
Pergl-Wilson, G.H.20
Raynaud, F.I.21
Robson, A.22
Saghir, N.23
Salphati, L.24
Sohal, S.25
Ultsch, M.H.26
Valenti, M.27
Wallweber, H.J.A.28
Wan, N.C.29
Wiesmann, C.30
Workman, P.31
Zhyvoloup, A.32
Zvelebil, M.J.33
Shuttleworth, S.J.34
more..
-
9
-
-
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. E.; 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
-
(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.E.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..
-
10
-
-
77949881462
-
The PI3K Pathway as Drug Target in Human Cancer
-
Courtney, K. D.; Corcoran, R. B.; Engelman, J. A. The PI3K Pathway as Drug Target in Human Cancer J. Clin. Oncol. 2010, 28, 1075-1083
-
(2010)
J. Clin. Oncol.
, vol.28
, pp. 1075-1083
-
-
Courtney, K.D.1
Corcoran, R.B.2
Engelman, J.A.3
-
11
-
-
78149283201
-
Identification and Structure-Activity Relationship of 2-Morpholino 6-(3-hydroxyphenyl)pyrimidines, a Class of Potent and Selective PI3-kinase Inhibitors
-
Pecchi, S.; Renhowe, P. A.; Taylor, C.; Kaufman, S.; Merrit, H.; Wiesmann, M.; Shoemaker, K.; Knapp, M. S.; Hendrickson, T. F.; Fantl, W.; Voliva, C. F. Identification and Structure-Activity Relationship of 2-Morpholino 6-(3-hydroxyphenyl)pyrimidines, a Class of Potent and Selective PI3-kinase Inhibitors Bioorg. Med. Chem. Lett. 2010, 20, 6895-6898
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 6895-6898
-
-
Pecchi, S.1
Renhowe, P.A.2
Taylor, C.3
Kaufman, S.4
Merrit, H.5
Wiesmann, M.6
Shoemaker, K.7
Knapp, M.S.8
Hendrickson, T.F.9
Fantl, W.10
Voliva, C.F.11
-
12
-
-
78651479722
-
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3- kinase Inhibitors
-
Burger, M. T.; Knapp, M.; Wagman, A.; Ni, Z. J.; Hendrickson, T.; Atallah, G.; Zhang, Y.; Frazier, K.; Verhagen, J.; Pfister, K.; Ng, S.; Smith, A.; Bartulis, S.; Merrit, H.; Wiesmann, M.; Xin, X.; Haznedar, J.; Voliva, C. F.; Iwanowicz, E.; Pecchi, S. Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors ACS Med. Chem. Lett. 2011, 2, 34-38
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 34-38
-
-
Burger, M.T.1
Knapp, M.2
Wagman, A.3
Ni, Z.J.4
Hendrickson, T.5
Atallah, G.6
Zhang, Y.7
Frazier, K.8
Verhagen, J.9
Pfister, K.10
Ng, S.11
Smith, A.12
Bartulis, S.13
Merrit, H.14
Wiesmann, M.15
Xin, X.16
Haznedar, J.17
Voliva, C.F.18
Iwanowicz, E.19
Pecchi, S.20
more..
-
13
-
-
0024017498
-
Models for Strong Interactions in Proteins and Enzymes. 1. Enhanced Acidities of Principal Biological Hydrogen Donors
-
By mimicking the electronics and H bond donating capabilities of the aminopyrimidines. see
-
By mimicking the electronics and H bond donating capabilities of the aminopyrimidines. see: Mautner, M. Models for Strong Interactions in Proteins and Enzymes. 1. Enhanced Acidities of Principal Biological Hydrogen Donors J. Am. Chem. Soc. 1988, 110, 3071-3075
-
(1988)
J. Am. Chem. Soc.
, vol.110
, pp. 3071-3075
-
-
Mautner, M.1
-
14
-
-
0033634827
-
Structural Determinants of Phosphoinositide-3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin and Staurosporine
-
Walker, E. H.; Pacold, M. E.; Perisic, O.; Stephens, L.; Hawkins, P. T.; Wymann, M. P.; Roger, L. Structural Determinants of Phosphoinositide-3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin and Staurosporine Mol. Cell 2000, 6, 909-919
-
(2000)
Mol. Cell
, vol.6
, pp. 909-919
-
-
Walker, E.H.1
Pacold, M.E.2
Perisic, O.3
Stephens, L.4
Hawkins, P.T.5
Wymann, M.P.6
Roger, L.7
-
15
-
-
3843135141
-
Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold
-
DOI 10.1016/j.bmc.2004.06.022, PII S0968089604004547
-
Knight, Z. A.; Chiang, G. G.; Alaimo, P. G.; Kenski, D. M.; Ho, C. B.; Coan, K.; Abraham, R. T.; Shokat, K. M. Isoform Specific Phosphoinositide-3- Kinase Inhibitors from an Arylmorpholine Scaffold Bioorg. Med. Chem. 2004, 12, 4749-4759 (Pubitemid 39044362)
-
(2004)
Bioorganic and Medicinal Chemistry
, vol.12
, Issue.17
, pp. 4749-4759
-
-
Knight, Z.A.1
Chiang, G.G.2
Alaimo, P.J.3
Kenski, D.M.4
Ho, C.B.5
Coan, K.6
Abraham, R.T.7
Shokat, K.M.8
-
16
-
-
80054757374
-
NVP-BKM120, a novel inhibitor of phosphoinositide 3-kinase in Phase I/II clinical trials, shows significant antitumor activity in xenograft models
-
Washington, D.C. Abstract 4497
-
"NVP-BKM120, a novel inhibitor of phosphoinositide 3-kinase in Phase I/II clinical trials, shows significant antitumor activity in xenograft models". Maira, M.; Menezes, D.; Pecchi, S.; Shoemaker, K.; Burger, M.; Schnell, C.; Fritsch, C.; Brachmann, S.; Nagel, T.; Sellers, W. R.; Garcia-Echeverria, C.; Wiesmann, M.; Voliva, C. F. 2010 AACR annual meeting, Washington, D.C., Abstract 4497.
-
2010 AACR Annual Meeting
-
-
Maira, M.1
Menezes, D.2
Pecchi, S.3
Shoemaker, K.4
Burger, M.5
Schnell, C.6
Fritsch, C.7
Brachmann, S.8
Nagel, T.9
Sellers, W.R.10
Garcia-Echeverria, C.11
Wiesmann, M.12
Voliva, C.F.13
-
17
-
-
84860888846
-
-
Oral Pan-Class I PI3K Inhibitor BKM120 Monotherapy in Patients with Advanced Solid Tumors: an Update on Safety and Efficacy". 47th ASCO Annual Meeting, June, Chicago, IL, Abstract 3043
-
"Oral Pan-Class I PI3K Inhibitor BKM120 Monotherapy in Patients with Advanced Solid Tumors: an Update on Safety and Efficacy". Graña-Suárez, B.; Burris, H. A.; Anhert, J. R.; Abdul Razak, A. R.; De Jonge, M. J.; Eskens, F.; Siu, L. L.; Ru, Q. C.; Homji, N. F.; Demanse, D.; Di Tomaso, E.; Cosaert, J.; Quadt, C.; Baselga, J.; Bendell, J. C. 47th ASCO Annual Meeting, June 2001, Chicago, IL, Abstract 3043.
-
(2001)
-
-
Graña-Suárez, B.1
Burris, H.A.2
Anhert, J.R.3
Abdul Razak, A.R.4
De Jonge, M.J.5
Eskens, F.6
Siu, L.L.7
Ru, Q.C.8
Homji, N.F.9
Demanse, D.10
Di Tomaso, E.11
Cosaert, J.12
Quadt, C.13
Baselga, J.14
Bendell, J.C.15
-
18
-
-
80054724383
-
-
Novartis internal data
-
Novartis internal data.
-
-
-
-
19
-
-
84860885181
-
-
NVP-BKM120
-
www.clinicaltrials.gov and NVP-BKM120.
-
-
-
|