Isoform-Specific Phosphoinositide 3-Kinase Inhibitors Exert Distinct Effects in Solid Tumors

• Published in: Cancer research (Chicago, Ill.) Vol. 70; no. 3; pp. 1164 - 1172
• Main Authors: EDGAR, Kyle A, WALLIN, Jeffrey J, BERRY, Megan, LEE, Leslie B, PRIOR, Wei Wei, SAMPATH, Deepak, FRIEDMAN, Lori S, BELVIN, Marcia
• Format: Journal Article
• Language: English
• Published: Philadelphia, PA American Association for Cancer Research 01.02.2010
• Subjects: Animals; Antineoplastic agents; Biological and medical sciences; Blotting, Western; Cell Cycle - drug effects; Cell Line, Tumor; Cell Survival - drug effects; Dose-Response Relationship, Drug; Female; Flow Cytometry; Humans; Indazoles - chemistry; Indazoles - pharmacology; Isoenzymes - antagonists & inhibitors; Isoenzymes - metabolism; Male; Medical sciences; Mice; Mice, Nude; Molecular Structure; Multiple tumors. Solid tumors. Tumors in childhood (general aspects); Mutation; Oncogene Protein v-akt - metabolism; Pharmacology. Drug treatments; Phosphatidylinositol 3-Kinases - antagonists & inhibitors; Phosphatidylinositol 3-Kinases - genetics; Phosphatidylinositol 3-Kinases - metabolism; Phosphorylation; Prostatic Neoplasms - drug therapy; Prostatic Neoplasms - metabolism; Prostatic Neoplasms - pathology; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - pharmacology; PTEN Phosphohydrolase - genetics; PTEN Phosphohydrolase - metabolism; Sulfonamides - chemistry; Sulfonamides - pharmacology; Tumors; Xenograft Model Antitumor Assays; Solid tumor; Molecular form; Enzyme; Transferases; Inhibitor; Malignant tumor; Cancer; 1-Phosphatidylinositol 3-kinase

Therapeutic inhibitors are being developed against the phosphoinositide 3-kinase (PI3K) pathway, the deregulation of which drives tumor growth and survival in many cancers. There are eight PI3Ks in mammals divided into three classes. Class IA PI3Ks (p110alpha, p110beta, and p110delta) are critical f...