http://purl.uniprot.org/citations/33797901 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/33797901 | http://www.w3.org/2000/01/rdf-schema#comment | "The approvals of idelalisib and duvelisib have validated PI3Kδ inhibitors for the treatment for hematological malignancies driven by the PI3K/AKT pathway. Our program led to the identification of structurally distinct heterocycloalkyl purine inhibitors with excellent isoform and kinome selectivity; however, they had high projected human doses. Improved ligand contacts gave potency enhancements, while replacement of metabolic liabilities led to extended half-lives in preclinical species, affording PI3Kδ inhibitors with low once-daily predicted human doses. Treatment of C57BL/6-Foxp3-GDL reporter mice with 30 and 100 mg/kg/day of 3c (MSD-496486311) led to a 70% reduction in Foxp3-expressing regulatory T cells as observed through bioluminescence imaging with luciferin, consistent with the role of PI3K/AKT signaling in Treg cell proliferation. As a model for allergic rhinitis and asthma, treatment of ovalbumin-challenged Brown Norway rats with 0.3 to 30 mg/kg/day of 3c gave a dose-dependent reduction in pulmonary bronchoalveolar lavage inflammation eosinophil cell count."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.1c00237"xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Chen D."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Li C."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Lee H.H."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Hill A."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Shah S."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Zhou H."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Yu H."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Jain R."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Alves S."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Lesburg C.A."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Shaffer L."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Garcia Y."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Altman M.D."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "McLeod R.L."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Christopher M."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Anthony N.J."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Katz J.D."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Fradera X."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Chappell C.P."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Tong V."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Trotter B.W."xsd:string |
http://purl.uniprot.org/citations/33797901 | http://purl.uniprot.org/core/author | "Methot J.L."xsd:string |