Journal: Oncology letters

Article Title: TCN, an AKT inhibitor, exhibits potent antitumor activity and enhances radiosensitivity in hypoxic esophageal squamous cell carcinoma in vitro and in vivo .

doi: 10.3892/ol.2016.5515

Figure Lengend Snippet: Figure 3. Upregulation of AKT and HIF‑1α by hypoxia can be attenuated by TCN in ESCC cells and xenografts in vivo. (A) Accumulation of HIF‑1α, VEGF and p‑AKT was observed upon 6 h of hypoxic incubation, and reached a maximum at 24 h in ESCC cells and nude mice. (B) For further experiments, the 24 h time point was selected. The hypoxia‑stimulated accumulation of p‑AKT, HIF‑1α and VEGF was significantly decreased by TCN. HIF, hypoxia-inducible factor; VEGF, vascular endothelial growth factor; ESCC, esophageal squamous cell carcinoma; TCN, triciribine; p, phosphorylated.

Article Snippet: The AKT inhibitor TCN (>99%) was purchased from Selleck Chemicals (Houston, TX, USA), while RPMI-1640 medium and fetal bovine serum (FBS) were obtained from Gibco (Thermo Fisher Scientific, Inc., Waltham, MA, USA).

Techniques: In Vivo, Incubation

Journal: Expert opinion on emerging drugs

Article Title: Emerging serine-threonine kinase inhibitors for treating ovarian cancer

doi: 10.1080/14728214.2019.1696773

Figure Lengend Snippet: Terms used for PubMed and ClinicalTrials.gov search.

Article Snippet: Triciribine phosphate , Prescient Therapeutics , CN1C2 = NC = NC3 = C2C(= CN3C4C (C(C(O4)COP(= O)(O)O)O)O)C(= N1)N , Combination with Carboplatin (C) , Recurrent, platinum resistant , Not specified , Phase II , AKT inhibitor.

Techniques:

Journal: Expert opinion on emerging drugs

Article Title: Emerging serine-threonine kinase inhibitors for treating ovarian cancer

doi: 10.1080/14728214.2019.1696773

Figure Lengend Snippet: Competitive environment characteristics of drugs with confirmed phase II/III activity for ovarian cancer are described in the table.

Article Snippet: Triciribine phosphate , Prescient Therapeutics , CN1C2 = NC = NC3 = C2C(= CN3C4C (C(C(O4)COP(= O)(O)O)O)O)C(= N1)N , Combination with Carboplatin (C) , Recurrent, platinum resistant , Not specified , Phase II , AKT inhibitor.

Techniques: Activity Assay, Mutagenesis

Journal: Expert opinion on emerging drugs

Article Title: Emerging serine-threonine kinase inhibitors for treating ovarian cancer

doi: 10.1080/14728214.2019.1696773

Figure Lengend Snippet: Clinical trials of STK inhibitors in active development for ovarian cancer active and completed clinical trials for drugs discussed in this review.

Article Snippet: Triciribine phosphate , Prescient Therapeutics , CN1C2 = NC = NC3 = C2C(= CN3C4C (C(C(O4)COP(= O)(O)O)O)O)C(= N1)N , Combination with Carboplatin (C) , Recurrent, platinum resistant , Not specified , Phase II , AKT inhibitor.

Techniques: Clinical Proteomics

Journal: The Journal of Clinical Investigation

Article Title: Stiff stroma increases breast cancer risk by inducing the oncogene ZNF217

doi: 10.1172/JCI129249

Figure Lengend Snippet: (A) Immunohistochemical (IHC) staining of paraffin sections from the mammary glands of heterozygous Col1a1tm1Jae (COL+/–; n = 3) and WT (n = 3) mice using a phospho–histone H3–specific antibody. Selected mice were treated with the ZNF217/Akt inhibitor triciribine (TRIC; n = 3 each for WT and COL+/– mice). Scale bar: 50 μm. (B) Quantification of positive phospho–histone H3 staining from A expressed as the percentage of highly positive nuclei area per total epithelial area (n = 14–16). (C) qRT-PCR analysis for miR-203 using RNA isolated from the mammary glands of 10-week-old COL+/– mice and age-matched WT counterparts. Results are normalized to U6 RNA levels and plotted relative to WT (n = 4). (D) IHC staining of paraffin sections as in A using a ZNF217-specific antibody. Scale bar: 50 μm. (E) Quantification of positive ZNF217 staining from D expressed as the percentage of high positive staining in MECs (n = 15). (F) IHC staining of paraffin sections as in A using a phosphorylated Akt substrate–specific antibody. Selected mice were treated with triciribine as in A. Scale bar: 50 μm. (G) Quantification of positive phosphorylated Akt substrate staining from F expressed as the percentage of high positive staining in MECs (n = 12–15). Data are represented as mean ± SEM. *P < 0.05; **P < 0.01; ***P < 0.001 by 2-tailed unpaired Student’s t test (C and E) or Kruskal-Wallis test followed by Dunn’s multiple-comparison test (B and G).

Article Snippet: Triciribine (APExBIO, catalog A8541) was diluted in DMSO and administered by intraperitoneal injection to 8-week-old Col1a1 tm1Jae mice at a dosage of 1 mg/kg, 5 times per week, for a total of 2 weeks.

Techniques: Immunohistochemical staining, Immunohistochemistry, Staining, Quantitative RT-PCR, Isolation, Comparison

Journal: British Journal of Clinical Pharmacology

Article Title: AKT in cancer: new molecular insights and advances in drug development

doi: 10.1111/bcp.13021

Figure Lengend Snippet: Ongoing clinical trials involving AKT inhibitors as registered on clinicaltrials.gov as of October 2015

Article Snippet: PTX‐200 , Prescient Therapeutics , Triciribine , PH domain (AKT) inhibitor , I/II , Advanced or metastatic HER2‐negative BC with paclitaxel, doxorubicin and cyclophosphamide.

Techniques: Protease Inhibitor