Dual Inhibitor
The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models
... XL388 is a mTORC1/2 dual inhibitor [14]. Therefore, we studied the mTORC1/2 activation in XL388-treated OS cells. Phosphorylated- (p-) S6K1 (Thr-389) and p-4E-BP1 (Ser 65) were tested as indicators of ...
12
<p>Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of α-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity</p>
... results revealed that the three substituted methoxy deriva- tives 7c, 7g and 7j experienced greater anticancer activity than that of CA-4; particularly the trimethoxy derivative 7j which experienced the most potent ...
20
Inulanolide A as a new dual inhibitor of NFAT1-MDM2 pathway for breast cancer therapy
... Of note, our in vitro and in vivo results showed a favorable safety profile of InuA in the preclinical breast cancer models in the present study. In the cell cytotoxicity assays, we found that the normal cell lines were ...
13
MLN-8237: A dual inhibitor of aurora A and B in soft tissue sarcomas
... Aurora kinases have become an attractive target in cancer therapy due to their deregulated expression in human tumors. Liposarcoma, a type of soft tissue sarcoma in adults, account for approximately 20% of all adult soft ...
11
Lapatinib, a TKI Dual Inhibitor of Her1 and Her2 Receptors: Review of the Literature
... In conclusion, lapatinib is an active and well tolerated oral dual TK inhibitor for the treatment of breast cancer. Clinical efficacy of lapatinib is limited only to the treat- ment of ErbB-2 overexpressing ...
8
Design and development of ICCA as a dual inhibitor of GPIIb/IIIa and P-selectin receptors
... Methods: For this reason, the structural characteristics and the CDOCKER interaction energies of 12 carbolines were analyzed. This led to the design of 1-(4-isopropyl-phenyl)-β-carboline-3- carboxylic acid (ICCA) as a ...
14
Efficacy of the dual PI3K and mTOR inhibitor NVP-BEZ235 in combination with imatinib mesylate against chronic myelogenous leukemia cell lines
... single inhibitor of mTOR, we chose NVP-BEZ235, the dual inhibitor of PI3K and mTOR, as investigational drug to study its effect on the PI3K/Akt/mTOR pathway of K562 and KBM7R ...
12
In silico design and biological evaluation of a dual specificity kinase inhibitor targeting cell cycle progression and angiogenesis
... a dual inhibitor of VEGFR and FGFR kinases) have proven effective in combating redundancy in signaling pathways ...similarly, dual inhibition of the Aurora A and CDK1 kinases targets multiple ...
16
A dose-ranging study of the inhaled dual phosphodiesterase 3 and 4 inhibitor ensifentrine in COPD
... Background: Many patients with chronic obstructive pulmonary disease (COPD) still experience daily symptoms, exacerbations, and accelerated lung function decline, even when receiving maximal combined treatment with ...
11
<p>Dual SGLT1/SGLT2 Inhibitor Phlorizin Ameliorates Non-Alcoholic Fatty Liver Disease and Hepatic Glucose Production in Type 2 Diabetic Mice</p>
... a dual SGLT1/2 inhibitor was used in the present study while selective SGLT2 inhibitors were used in the studies in T2D subjects; 2) the pyruvate tolerance test used here re fl ects gluconeogen- esis ...
13
The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression
... kinase inhibitor with an mTOR inhibitor might have complementary growth- inhibitory effects against ...PIM inhibitor AZD1208 and of mTOR by selective mTORC1/2 dual inhibitor AZD2014 ...
18
Noni Seed Oil Topical Safety, Efficacy, and Potential Mechanisms of Action
... selective inhibitor of COX-2 enzymes ...a dual inhibitor of COX-2 and 5-LOX enzymes [23]. This dual inhibition may explain the pain- reducing and anti-inflammatory effect of noni juice, as ...
5
<p>Dual PI3K/mTOR Inhibitor, XL765, suppresses glioblastoma growth by inducing ER stress-dependent apoptosis</p>
... XL765 (SAR245409) is a potent class I dual inhibitor of PI3Ks and mTOR. In cellular assays, treatment with XL765 suppresses phosphorylation of PI3K and mTOR downstream effectors in multiple tumor cell ...
10
Original Article Targeting the VEGF and PDGF signaling pathway in glioblastoma treatment
... mTOR inhibitor rapamycin and its analogs did not have a significant therapeutic effect on cancer diseases ...The dual inhibi- tion of both pathways seems to be more effec- tive in GB ...the dual ...
13
PubMedCentral-PMC5022787.pdf
... BRAF inhibitor, vemurafenib, was FDA-approved for the first-line treatment of BRAF V600E-positive melanoma after interim review of a phase 3 randomized controlled trial that demonstrated improved OS (84% ...BRAF ...
33
The novel dual PI3K/mTOR inhibitor NVP-BGT226 displays cytotoxic activity in both normoxic and hypoxic hepatocarcinoma cells
... bioavailable dual PI3K/mTOR inhibitor, NVP-BGT226, on a panel of HCC cell lines, since hyperactivated PI3K/Akt/mTOR signaling pathway could represent a biomolecular target for Small Inhibitor ...
14
Seronegative autoimmune autonomic ganglionopathy from dual immune checkpoint inhibition in a patient with metastatic melanoma
... Careful thought has to be given to re-inducing patients with ICI who have had prior irAEs. In this case, our pa- tient made a significant, albeit partial recovery of his AAG and the risk of his melanoma progression was ...
6
Phase 2 study evaluating intermittent and continuous linsitinib and weekly paclitaxel in patients with recurrent platinum resistant ovarian epithelial cancer.
... Linsitinib (OSI-906) is an orally active, dual IGF1R and insulin recep- tor (IR) inhibitor, with anti-proliferative effects in tumor cell lines and in vivo xenograft tumor models [18,19]. By inhibiting both ...
8
Pediatric and adult glioblastoma radiosensitization induced by PI3K/mTOR inhibition causes early metabolic alterations detected by nuclear magnetic resonance spectroscopy.
... a dual blockade of IGFR1 and PDGFR [9] or mTOR and AKT ...the dual PI3K/mTOR inhibitor NVP-BEZ235 has been shown to be active against ATM serine/threonine kinase (ATM), ATR serine/ threonine kinase ...
15
A Chemical Biology Platform to Develop Small Molecule Probes for Bromodomains
... XMD11-50 (19) to define the binding modes and to predict how these scaffolds further direct the medicinal chemistry effort around modifying the dual kinase-bromodomain inhibitory activity against either kinases or ...
109