Beta-testing of PI3-kinase inhibitors: Is beta better?

Cancer Discovery

Volumn 2, Issue 5, 2012, Pages 393-394

  Shepherd, Peter R ^a   Denny, William A ^b  

^a UNIVERSITY OF AUCKLAND   (New Zealand)

^b UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; ENZYME INHIBITOR; G PROTEIN COUPLED RECEPTOR; ISOPROTEIN; KIN 193; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3, 4, 5 TRISPHOSPHATE 3 PHOSPHATASE; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE 3 KINASE; PROTEIN KINASE B; PROTEIN P110; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; CELL GROWTH; DRUG ANTAGONISM; FEMALE; GENE SILENCING; HUMAN; MALE; MUTATION; NEOPLASM; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; CLASS IA PHOSPHATIDYLINOSITOL 3-KINASE; ENZYME INHIBITORS; FEMALE; HUMANS; MALE; NEOPLASMS;

EID: 84866326235     PISSN: 21598274     EISSN: 21598290     Source Type: Journal    
DOI: 10.1158/2159-8290.CD-12-0122     Document Type: Article

References (11)

1. Vanhaesebroeck B, Stephens L, Hawkins P. PI3K signalling: the path to discovery and understanding. Nat Rev Mol Cell Biol 2012;113:195-203.
2. Samuels Y, Wang Z, Bardelli A, Silliman N, Ptak J, Szabo S, et al. High frequency of mutations of the PIK3CA gene in human cancers. Science 2004;304:554.
3. Jamieson S, Flanagan JU, Kolekar S, Buchanan C, Kendall JD, Lee WJ, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J 2011;438:53-62.
4. So L, Fruman DA. PI3K signalling in B-and T-lymphocytes: new developments and therapeutic advances. Biochem J 2012;442:465-81.
5. Kang S, Denley A, Vanhaesebroeck B, Vogt PK. Oncogenic transformation induced by the p110beta,-gamma, and-delta isoforms of class I phosphoinositide 3-kinase. Proc Natl Acad Sci U S A 2006;103:1289-94.
6. Chen H, Mei L, Zhou L, Shen X, Guo C, Zheng Y, et al. PTEN restoration and PIK3CB knockdown synergistically suppress glioblastoma growth in vitro and in xenografts. J Neuro-Oncol 2011;104:155-67.
7. Kim J, Hong S, Hong S. Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kβ) inhibitors with selectivity over PI3Kα. Bioorg Med Chem Lett 2012;54:6977-81.
8. Edgar KA, Wallin JJ, Berry M, Lee LB, Prior WW, Sampath D, et al. Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors. Cancer Res 2010;70:1164-72.
9. Ni J, Liu Q, Xie S, Carlson CB, Von T, Vogel KW, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov 2012;2:425-33.
10. Smith GC, Ong WK, Rewcastle GW, Kendall JD, Han W, Shepherd PR. Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo. Biochem J 2012;442:161-9.
11. Berenjeno IM, Guillermet-Guibert J, Pearce W, Gray A, Fleming S, Vanhaesebroeck B. Both p110α and p110β isoforms of PI3K can modulate the impact of loss-of-function of the PTEN tumour suppressor. Biochem J 2012;442:151-9.