Targeting the IDO1/TDO2-KYN-AhR Pathway for Cancer Immunotherapy - Challenges and Opportunities.
Sign Up to like & getrecommendations! Published in 2018 at "Trends in pharmacological sciences"
DOI: 10.1016/j.tips.2017.11.007
Abstract: Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase 2 (TDO2) catalyze the commitment step of the kynurenine (KYN) metabolic pathway. Traditionally the immunosuppressive effect of IDO1 has been attributed mainly to reduced levels of tryptophan, which… read more here.
Keywords: tdo2; tdo2 kyn; targeting ido1; cancer ... See more keywords
Discovery of novel IDO1/TDO2 dual inhibitors: a consensus Virtual screening approach with molecular dynamics simulations, and binding free energy analysis
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2024.2329302
Abstract: Abstract The pursuit of effective cancer immunotherapy drugs remains challenging, with overexpression of indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase 2 (TDO2) allowing cancer cells to evade immune attacks. While several IDO1 inhibitors have undergone… read more here.
Keywords: ido1; dual inhibitors; binding free; tdo2 dual ... See more keywords
Abstract 1701: EPL-1410, a novel fused heterocycle based orally active dual inhibitor of IDO1/TDO2, as a potential immune-oncology therapeutic
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1701
Abstract: Many tumors use tryptophan (Trp)-catabolizing enzymes such as Indoleamine/Tryptophan-2,3-dioxygenases (IDO1/TDO2) to induce an immunosuppressive environment by depleting Trp, resulting in excessive generation of kynurenine (Kyn) pathway metabolites. IDO1 inhibitors in combination with immune-checkpoint inhibitors are… read more here.
Keywords: oncology; 1410 novel; ido1 tdo2; epl 1410 ... See more keywords
Abstract 5886: Targeting IDO1 and TDO2 is crucial for the modulation of immune effector in platinum resistant non-small cell lung cancer
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-5886
Abstract: The impact of non-small cell lung cancer (NSCLC) tumor metabolism on the immune microenvironment is not well understood in the context of platinum resistance. We have identified and characterized crucial metabolic differences between cisplatin-resistant (CR)… read more here.
Keywords: lung cancer; cell; cancer; ido1 tdo2 ... See more keywords
Abstract PR-010: Dual targeting of IDO1/TDO2 inhibits tumor progression and attenuates the immune suppressive tumor microenvironment
Sign Up to like & getrecommendations! Published in 2024 at "Cancer Research"
DOI: 10.1158/1538-7445.ovarian23-pr-010
Abstract: Introduction: High-grade serous carcinoma (HGSC) tumors of the ovary, fallopian tube, or peritoneum are predicted to be immunogenic since the presence of tumor-infiltrating lymphocytes conveys a better prognosis. However, the efficacy of immunotherapies has been… read more here.
Keywords: ido1 tdo2; tdo2; tumor; immune suppressive ... See more keywords
AT-0174, a novel dual IDO1/TDO2 enzyme inhibitor, synergises with temozolomide to improve survival in an orthotopic mouse model of glioblastoma
Sign Up to like & getrecommendations! Published in 2024 at "BMC Cancer"
DOI: 10.1186/s12885-024-12631-w
Abstract: Glioblastoma is an aggressive brain cancer, usually of unknown etiology, and with a very poor prognosis. Survival from diagnosis averages only 3 months if left untreated and this only increases to 12–15 months upon treatment.… read more here.
Keywords: treatment; survival; glioblastoma; tdo2 ... See more keywords
Discovery and Characterisation of Dual Inhibitors of Tryptophan 2,3-Dioxygenase (TDO2) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Using Virtual Screening
Sign Up to like & getrecommendations! Published in 2019 at "Molecules"
DOI: 10.3390/molecules24234346
Abstract: Cancers express tryptophan catabolising enzymes indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) to produce immunosuppressive tryptophan metabolites that undermine patients’ immune systems, leading to poor disease outcomes. Both enzymes are validated targets for cancer… read more here.
Keywords: ido1; tdo2; dioxygenase ido1; indoleamine dioxygenase ... See more keywords
Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15091090
Abstract: Indoleamine 2, 3-dioxygenase 1 (IDO1) is commonly expressed by cancers as a mechanism for evading the immune system. Preclinical and clinical studies have indicated the potential of combining IDO1 inhibitors with immune therapies for the… read more here.
Keywords: human ido1; ido1; ido1 tdo2; selectivity ... See more keywords
In silico discovery and therapeutic potential of IDO1 and TDO2 inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2017-0070
Abstract: The war on cancer has traditionally been fought by deploying ever-powerful tactics of killing cancer cells by irradiation, chemoand targeted-therapies. Many hard-fought battles have been won but novel strategies are necessary to declare ultimate victory… read more here.
Keywords: discovery therapeutic; potential ido1; cancer; therapeutic potential ... See more keywords