Results 1 to 10 of about 4,006,149 (207)

Abrine, an IDO1 inhibitor, suppresses the immune escape and enhances the immunotherapy of anti-PD-1 antibody in hepatocellular carcinoma [PDF]

Frontiers in Immunology, 2023
BackgroundIndoleamine-2,3-dioxygenase 1 (IDO1) is responsible for tumor immune escape by regulating T cell-associated immune responses and promoting the activation of immunosuppressive.
Xiaowei Liang, Xiaowei Liang, Hongwei Gao, Hongwei Gao, Jian Xiao, Shan Han, Shan Han, Jia He, Jia He, Renyikun Yuan, Renyikun Yuan, Shilin Yang, Shilin Yang, Chun Yao   +13 more
doaj   +7 more sources

IDO1 Inhibitor RY103 Suppresses Trp-GCN2-Mediated Angiogenesis and Counters Immunosuppression in Glioblastoma [PDF]

Pharmaceutics
Glioma is characterized by strong immunosuppression and excessive angiogenesis. Based on existing reports, it can be speculated that the resistance to anti-angiogenic drug vascular endothelial growth factor A (VEGFA) antibody correlates to the induction ...
Zikang Xing, Xuewen Li, Zhen Ning Tony He, Xin Fang, Heng Liang, Chunxiang Kuang, Aiying Li, Qing Yang   +7 more
doaj   +4 more sources

Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype. [PDF]

Angew Chem Int Ed Engl, 2022
Natural product (NP)‐inspired design principles provide invaluable guidance for bioactive compound discovery. Pseudo‐natural products (PNPs) are de novo combinations of NP fragments to target biologically relevant chemical space not covered by NPs.
Davies C, Dötsch L, Ciulla MG, Hennes E, Yoshida K, Gasper R, Scheel R, Sievers S, Strohmann C, Kumar K, Ziegler S, Waldmann H.   +11 more
europepmc   +6 more sources

Sphingomyelin-derived nanovesicles for the delivery of the IDO1 inhibitor epacadostat enhance metastatic and post-surgical melanoma immunotherapy. [PDF]

Nat Commun, 2023
Epacadostat (EPA), the most advanced IDO1 inhibitor, in combination with PD-1 checkpoint inhibitor, has failed in a recent Phase III clinical trial for treating metastatic melanoma. Here we report an EPA nanovesicle therapeutic platform (Epacasome) based
Wang Z, Li W, Jiang Y, Tran TB, Cordova LE, Chung J, Kim M, Wondrak G, Erdrich J, Lu J.   +9 more
europepmc   +3 more sources

Amyloid β neurotoxicity is IDO1–Kyn–AhR dependent and blocked by IDO1 inhibitor [PDF]

Signal Transduction and Targeted Therapy, 2020
Dear Editor, Alzheimer’s disease (AD), the most common neurodegenerative disorder and a leading cause of dementia is characterized by progressive memory deficits, cognitive impairment and personality changes.
Chunxiang Kuang, Qing Yang, Osamu Takikawa   +2 more
exaly   +3 more sources

Metabolic adaptation of ovarian tumors in patients treated with an IDO1 inhibitor constrains antitumor immune responses. [PDF]

Sci Transl Med, 2022
To uncover underlying mechanisms associated with failure of indoleamine 2,3-dioxygenase 1 (IDO1) blockade in clinical trials, we conducted a pilot, window-of-opportunity clinical study in 17 patients with newly diagnosed advanced high-grade serous ...
Odunsi K, Qian F, Lugade AA, Yu H, Geller MA, Fling SP, Kaiser JC, Lacroix AM, D'Amico L, Ramchurren N, Morishima C, Disis ML, Dennis L, Danaher P, Warren S, Nguyen VA, Ravi S, Tsuji T, Rosario S, Zha W, Hutson A, Liu S, Lele S, Zsiros E, McGray AJR, Chiello J, Koya R, Chodon T, Morrison CD, Putluri V, Putluri N, Mager DE, Gunawan R, Cheever MA, Battaglia S, Matsuzaki J.   +35 more
europepmc   +2 more sources

IDO1 inhibitor enhances the effectiveness of PD-1 blockade in microsatellite stable colorectal cancer by promoting macrophage pro-inflammatory phenotype polarization. [PDF]

Cancer Immunol Immunother
Microsatellite stable (MSS) colorectal cancer (CRC) is a subtype of CRC that generally exhibits resistance to immunotherapy, particularly immune checkpoint inhibitors such as PD-1 blockade. This study investigates the effects and underlying mechanisms of
Guangzhao L, Xin W, Miaoqing W, Wenjuan M, Ranyi L, Zhizhong P, Rongxin Z, Gong C.   +7 more
europepmc   +2 more sources

Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor. [PDF]

Br J Clin Pharmacol, 2019
Navoximod (GDC‐0919, NLG‐919) is a small molecule inhibitor of indoleamine‐2,3‐dioxygenase 1 (IDO1), developed to treat the acquired immune tolerance associated with cancer.
Ma S, Suchomel J, Yanez E, Yost E, Liang X, Zhu R, Le H, Siebers N, Joas L, Morley R, Royer-Joo S, Pirzkall A, Salphati L, Ware JA, Morrissey KM.   +14 more
europepmc   +2 more sources

Discovery of novel IDO1 inhibitors targeting the protein’s apo form through scaffold hopping from holo-IDO1 inhibitor

Bioorganic and Medicinal Chemistry Letters, 2021
Immunomodulating enzyme IDO1 plays an important role in tumor immune resistance. Inhibiting IDO1 by small molecules with new mechanism of action is a potential strategy in IDO1 inhibitor development.
Yungen Xu, Yi Zou, Qihua Zhu
exaly   +2 more sources

Cell based functional assays for IDO1 inhibitor screening and characterization. [PDF]

Oncotarget, 2018
Indoleamine 2,3-dioxygenase 1 (IDO1) is a new immune-oncology target and its inhibitors have shown promise in the clinic especially in combination with other immune-stimulating agents.
Richards T, Brin E.
europepmc   +2 more sources