PI3K/mutant PI3K inhibitors [cytosol]

Stable Identifier
Set [CandidateSet]
Locations in the PathwayBrowser

PI3K inhibitors bind the catalytic subunit of PIK3CA, blocking its phosphoinositide kinase activity.

Literature References
PubMed ID Title Journal Year
21317208 Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide

Weiss, WA, Yang, X, Polley, MY, Haas-Kogan, DA, James, CD, Sottero, T, Prados, MD, Prasad, G, Ozawa, T, Berger, MS, Aftab, DT, Mueller, S

Neuro-oncology 2011
8657148 Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction

Wymann, MP, Bulgarelli-Leva, G, Pirola, L, Waterfield, MD, Vanhaesebroeck, B, Zvelebil, MJ, Panayotou, G

Mol. Cell. Biol. 1996
19411071 Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941

Junttila, TT, Fields, C, Sliwkowski, MX, Lewis Phillips, GD, Sampath, D, Friedman, LS, Parsons, K, Akita, RW

Cancer Cell 2009
19644473 Targeting the phosphoinositide 3-kinase pathway in cancer

Roberts, TM, Cheng, H, Liu, P, Zhao, JJ

Nat Rev Drug Discov 2009
22188813 Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor

De Pover, A, Hofmann, F, Brachmann, S, Chène, P, Fabbro, D, Guthy, D, García-Echeverría, C, Martiny-Baron, G, Menezes, D, Shoemaker, K, Pecchi, S, Fritsch, C, Huang, A, Sellers, WR, Wiesmann, M, Voliva, CF, Dorsch, M, Maira, SM, Schnell, C, Sterker, D, Nagel, T, Wilson, CJ, Knapp, M, Burger, M, Schlegel, R

Mol. Cancer Ther. 2012
21976531 Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo

Chuang, BF, Tsai, SY, Chang, KY, Chang, JY, Yen, CJ, Wu, CM

Clin. Cancer Res. 2011
18606717 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

Furet, P, De Pover, A, Brachmann, S, Finan, P, Chène, P, Fabbro, D, García-Echeverría, C, Maira, SM, Murphy, L, Gabriel, D, Schnell, C, Schoemaker, K, Fritsch, C, Brueggen, J, Simonen, M, Sellers, W, Stauffer, F

Mol. Cancer Ther. 2008
18829560 NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations

Arribas, J, Maira, M, Baselga, J, Guzman, M, Parra, JL, Eichhorn, PJ, Atzori, F, Botero, ML, Serra, V, Valero, V, Markman, B, Di Cosimo, S, Llonch, E, Garcia-Echeverria, C, Scaltriti, M

Cancer Res. 2008
18754654 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

Valenti, M, Workman, P, Depledge, P, Alix, S, Hancox, TC, Kugendradas, A, Baker, SJ, Box, G, Chuckowree, IS, Eccles, SA, Alderton, WK, Ultsch, MH, Pang, J, Clarke, PA, Saghir, N, Patel, S, Zhyvoloup, A, Wiesmann, C, Wan, NC, Moore, P, Wallweber, HJ, Zvelebil, MJ, Pergl-Wilson, GH, Raynaud, FI, Ahmadi, K, Lensun, L, Hayes, A, Salphati, L, Robson, A, Olivero, AG, Shuttleworth, SJ, Sohal, S, Friedman, LS, Folkes, AJ

J. Med. Chem. 2008
21368164 Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors

Kuba, MG, Arteaga, CL, Rinehart, C, Sánchez, V, Chakrabarty, A

Proc. Natl. Acad. Sci. U.S.A. 2012
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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