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- PI3K/Akt/mTOR
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Archives
IDO/TDO
Pharmacokinetics of S-epacadostat, an indoleamine 2,3-dioxygenase 1 inhibitor, in dog plasma and identification of its metabolites in vivo and in vitro
54 views | Sep 24 2021
Yumu Zhang et al. thought that substituting the nitrogen with sulfur affected the metabolism of the adjacent alkyl side chain. [Read the Full Post]
Overcoming Chemoimmunotherapy-Induced Immunosuppression by Assemblable and Depot Forming Immune Modulating Nanosuspension
58 views | Sep 24 2021
Seung Mo Jin et al. found that local administration of AIMS increased T cell infiltration in both local and distant tumors and significantly inhibited the metastasis of tumors to the lung. [Read the Full Post]
Synergistic Utilization of Necrostatin-1 and Z-VAD-FMK Efficiently Promotes the Survival of Compression-Induced Nucleus Pulposus Cells via Alleviating Mitochondrial Dysfunction
165 views | Jan 03 2021
Songfeng Chen et al. found that the synergistic utilization of Necrostatin-1 and Z-VAD-FMK was a very worthwhile solution in preventing compression-mediated NP cells death, which might be largely attributed to restored mitochondrial function. [Read the Full Post]
Peptide vaccination directed against IDO1-expressing immune cells elicits CD8 + and CD4 + T-cell-mediated antitumor immunity and enhanced anti-PD1 responses
133 views | Sep 17 2020
Souvik Dey et al. found that the in vivo antitumor effects demonstrated with IDO1-based vaccines via targeting of the tumor microenvironment highlighted the utility of mouse models for further exploration and refinement of this novel vaccine-based approach to IDO1-directed cancer therapy and its potential to improve patient response rates to anti-PD1 therapy. [Read the Full Post]
Clinical Significance of Program Death Ligand-1 and Indoleamine-2,3-Dioxygenase Expression in Colorectal Carcinoma
139 views | Sep 17 2020
Sean Hacking et al. supported the theoretical foundation for targeting PD-L1 and IDO-1 in CRC, which now needed verification in well-designed robust clinical trials. [Read the Full Post]
MYC promotes tryptophan uptake and metabolism by the kynurenine pathway in colon cancer
293 views | Jan 17 2020
Venkateswaran N et al. proposed that limiting cellular kynurenine or its downstream targets could present a new strategy to reduce the proliferation of MYC-dependent cancer cells. [Read the Full Post]
First-in-Human Phase I Study of the Oral Inhibitor of Indoleamine 2,3-Dioxygenase-1 Epacadostat (INCB024360) in Patients with Advanced Solid Malignancies
294 views | Nov 25 2019
Beatty GL et al. showed that epacadostat was generally well tolerated, effectively normalized kynurenine levels, and produced maximal inhibition of IDO1 activity at doses of ≥100 mg BID. Studies investigating epacadostat in combination with other immunomodulatory drugs are ongoing. [Read the Full Post]
Updates in the Clinical Development of Epacadostat and Other Indoleamine 2,3-Dioxygenase 1 Inhibitors (IDO1) for Human Cancers
296 views | Nov 24 2019
Komiya T et al. indicated that IDO1 is a promising target that can improve the treatment outcome in the field of Immuno-oncology. Several orally available IDO1 inhibitors including Epacadostat have entered human clinical trials over the last few years without a major safety concern. Although there is no objective response in single-agent trials, combination regimens with PD-1 inhibitors appear to exceed the activity of PD-1 inhibitors alone. Recent phase III ECHO 301 trial testing the combination of Epacadostat with Pembrolizumab in melanoma did not show superior outcome compared to Pembrolizumab alone. This lead to halting of other phase III trials using IDO1 inhibitors. In this minireview, we will discuss the recent clinical development of Epacadostat and other IDO1 inhibitors. [Read the Full Post]
Effects of EF-24, RAD001, and paclitaxel on the expression profiles of apoptotic and anti-apoptotic genes
527 views | May 15 2019
Alp E et al. showed that response of these cells to paclitaxel, EF-24, and RAD001 was found different at the transcriptional level of apoptotic and antiapoptotic genes. [Read the Full Post]
Effects of Epacadostat on Brain Extracellular Fluid Concentrations of Serotonin -- An Intracerebral Microdialysis Study in Sprague-Dawley Rats
440 views | May 14 2019
Zhang Y et al. suggested that serotonin syndrome is unlikely following treatment with either epacadostat alone or with combination with MAOIs such as linezolid. [Read the Full Post]
