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Future Medicinal ChemistryVol. 9, No. 12 EditorialSmall-molecule antagonists of the immune checkpoint pathways: concept to clinicPottayil G Sasikumar & Murali RamachandraPottayil G Sasikumar Aurigene Discovery Technologies Limited, Bangalore, India & Murali Ramachandra*Author for correspondence: E-mail Address: murali_r@aurigene.com Aurigene Discovery Technologies Limited, Bangalore, IndiaPublished Online:3 Aug 2017https://doi.org/10.4155/fmc-2017-0107AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: antagonistcheckpoint inhibitorimmunomodulatorimmuno-oncologyimmunotherapyorally bioavailablePD-1 pathwayprotein–protein interactionsmall moleculeVISTAReferences1 Greil R, Hutterer E, Hartmann TN, Pleyer L. Reactivation of dormant anti-tumor immunity – a clinical perspective of therapeutic immune checkpoint modulation. Cell Commun. 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Cancer Res. 76, 4861–4861 (2016).Crossref, Medline, Google Scholar23 Clinical Trials Database: NCT02812875. https://clinicaltrials.gov/ct2/show/study/NCT02812875.Google ScholarFiguresReferencesRelatedDetailsCited ByNear Infrared Photoimmunotherapy: A Review of Recent Progress and Their Target Molecules for Cancer Therapy31 January 2023 | International Journal of Molecular Sciences, Vol. 24, No. 3Leveraging structural and 2D-QSAR to investigate the role of functional group substitutions, conserved surface residues and desolvation in triggering the small molecule-induced dimerization of hPD-L127 June 2022 | BMC Chemistry, Vol. 16, No. 1Discovery of Anti-PD-L1 Human Domain Antibodies for Cancer Immunotherapy4 April 2022 | Frontiers in Immunology, Vol. 13SAR study of small molecule inhibitors of the programmed cell death‐1/programmed cell death‐ligand 1 interaction23 September 2021 | Chemical Biology & Drug Design, Vol. 98, No. 5Combining Oncolytic Viruses and Small Molecule Therapeutics: Mutual Benefits6 July 2021 | Cancers, Vol. 13, No. 14Discovery of a new inhibitor targeting PD-L1 for cancer immunotherapyNeoplasia, Vol. 23, No. 3Discovery of low-molecular weight anti-PD-L1 peptides for cancer immunotherapy22 October 2019 | Journal for ImmunoTherapy of Cancer, Vol. 7, No. 1The Characteristics of PD-L1 Inhibitors, from Peptides to Small Molecules20 May 2019 | Molecules, Vol. 24, No. 10Immunotherapy… a pursuit race to tomorrow's medicinesAntonio Macchiarulo3 August 2017 | Future Medicinal Chemistry, Vol. 9, No. 12 Vol. 9, No. 12 Follow us on social media for the latest updates Metrics Downloaded 307 times History Published online 3 August 2017 Published in print August 2017 Information© 2017 Future Science LtdKeywordsantagonistcheckpoint inhibitorimmunomodulatorimmuno-oncologyimmunotherapyorally bioavailablePD-1 pathwayprotein–protein interactionsmall moleculeVISTAAcknowledgementsWe thank David Tuck and Tim Wyant (both from Curis, Inc.) for their comments on this manuscript.Financial & competing interests disclosureThe authors are full-time employees of Aurigene Discovery Technologies Limited, which holds multiple patents in the immuno-oncology space. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.No writing assistance was utilized in the production of this manuscript.PDF download