2019
DOI: 10.1039/c9md00208a
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Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

Abstract: This review summarizes the recent development of IDO1 inhibitors, focusing on structures, enzymatic inhibitory activity, selectivity and other biological activities.

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Cited by 26 publications
(16 citation statements)
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“…18 Although various compounds of tryptophan or indole analogues were studied as IDO1 inhibitors, the carbazole class has not reported any inhibitory activity against IDO1 yet. 23,39 The computational docking data between compounds 1-3 and apo-IDO1 enzyme (PDB id: 6AZV) were in good accordance with the results of IDO1 inhibition assay. Docking analysis proposed that compounds 1-3 interact with both the A-pocket and abandoned heme pocket of the IDO1 apoenzyme by hydrogen bonds and hydrophobic interactions.…”
Section: Resultssupporting
confidence: 64%
“…18 Although various compounds of tryptophan or indole analogues were studied as IDO1 inhibitors, the carbazole class has not reported any inhibitory activity against IDO1 yet. 23,39 The computational docking data between compounds 1-3 and apo-IDO1 enzyme (PDB id: 6AZV) were in good accordance with the results of IDO1 inhibition assay. Docking analysis proposed that compounds 1-3 interact with both the A-pocket and abandoned heme pocket of the IDO1 apoenzyme by hydrogen bonds and hydrophobic interactions.…”
Section: Resultssupporting
confidence: 64%
“…It recently underwent the phase I/II clinical trials and is currently during phase III trials in combination with checkpoint blockade. However, the latest results from one of the phase III clinical studies indicate that it does not improve the effectiveness of pembrolizumab in patients with unresectable or metastatic melanoma [ 74 , 155 , 156 , 157 ].…”
Section: Modulation Of Kynurenine Pathway Activity In the Management Of Neoplastic Diseasesmentioning
confidence: 99%
“…[ 43 , 44 , 45 , 46 , 47 , 181 ]. Additionally, recent preclinical evidence indicates that the IDO1 inhibitors synergize the effects of tumor immuno- and chemotherapies and help to solve the problem of tumor resistance against them [ 83 , 93 , 105 , 106 , 107 , 108 , 112 , 113 , 119 , 120 , 129 , 132 , 133 , 136 , 137 , 143 , 146 , 151 , 154 , 155 , 156 , 157 , 171 ]. In turn, the discoveries concerning the role of IDO1 in tumor angiogenesis suggest that inhibiting its activity may effectively suppress this process, providing a potentially effective solution in the prevention of tumor development and metastasis.…”
Section: Summary and Future Directionsmentioning
confidence: 99%
“…Since IDO1 plays an important role in cancer immunotherapy and neurological diseases, searching for highly active inhibitors is now a focus of research and development efforts by pharmaceutical companies and academic research institutions [8–30] . Various molecular scaffolds with inhibitory activity against IDO1 have been documented in the academic and patent literature [8–30] . To date, several IDO1 inhibitors such as Epacadostat, PF‐06840003, NLG‐919 and BMS‐986205 have advanced to clinical trials (Figure 1).…”
Section: Introductionmentioning
confidence: 99%