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Analysis of PI3K pathway inhibition by Wormannin-Leu (Wn-L) and intact Wortmannin (Wn) showed that attachment of Leu at C-20 decreased potency of PI3K pathway inhibition 10-fold compared to intact wortmannin, yet exceeded the potency of a competitive PI3K inhibitor LY294002.</jats:p>","journal":"Molecules","year":2018,"id":647920,"datarank":0.5334288069418921,"base_score":2.302585092994046,"endowment":2.302585092994046,"self_citation_contribution":0.3453877639491069,"citation_network_contribution":0.18804104299278515,"self_endowment_contribution":0.3453877639491069,"citer_contribution":0.18804104299278515,"corpus_percentile":null,"corpus_rank":null,"citation_count":9,"citer_count":9,"citers_with_citation_signal":8,"citers_with_endowment":8,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":282832,"name":"Yue Huang","orcid":"0000-0002-3913-9400","position":1,"is_corresponding":false},{"id":1688246,"name":"Antonio A. 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To test this approach, a wortmannin derivative with a leucine linker attached to C20 has been synthesized and tested for inhibition of PI3K activity in prostate cancer cells. Analysis of PI3K pathway inhibition by Wormannin-Leu (Wn-L) and intact Wortmannin (Wn) showed that attachment of Leu at C-20 decreased potency of PI3K pathway inhibition 10-fold compared to intact wortmannin, yet exceeded the potency of a competitive PI3K inhibitor LY294002.</jats:p>","is_dataset_classified":null,"base_score":2.302585092994046,"endowment":2.302585092994046,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"30036994","pmcid":"PMC6100554","openalex_id":"https://openalex.org/W2883502622","authors":[],"funders":[{"funder_name":"National Cancer Institute","grant_id":"R21CA182248","title":null},{"funder_name":"National Institutes of Health","grant_id":"5R21CA182248-02","title":"A novel mechanism of AKT activation regulated by YY1 binding"}],"total_grants":2,"fwci":0.2475,"citation_percentile":0.52360324,"influential_citations":0,"citation_trend":[{"year":2019,"count":1},{"year":2021,"count":2},{"year":2022,"count":3},{"year":2023,"count":1},{"year":2025,"count":1},{"year":2026,"count":1}],"oa_status":"gold","license":"cc-by","oa_locations":[{"url":"https://www.mdpi.com/1420-3049/23/7/1791/pdf?version=1532079359","host_type":"journal"},{"url":"https://www.mdpi.com/1420-3049/23/7/1791/pdf?version=1532079359","host_type":"publisher"},{"url":"https://www.mdpi.com/1420-3049/23/7/1791/pdf","host_type":"publisher"},{"url":"https://doi.org/10.3390/molecules23071791","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/30036994","host_type":"repository"},{"url":"https://doaj.org/article/b9ff3dd12f214e6197c9271b7679b6b9","host_type":"repository"},{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/6100554","host_type":"repository"},{"url":"http://dx.doi.org/10.3390/molecules23071791","host_type":"repository"},{"url":"http://hdl.handle.net/10339/96049","host_type":"repository"},{"url":"https://europepmc.org/articles/PMC6100554","host_type":"Europe_PMC"},{"url":"https://europepmc.org/articles/PMC6100554?pdf=render","host_type":"Europe_PMC"},{"url":"https://dx.doi.org/10.3390/molecules23071791","host_type":""}],"fields_of_study":["PI3K/AKT/mTOR signaling in cancer","Protein Degradation and Inhibitors","Histone Deacetylase Inhibitors Research","0301 basic medicine","03 medical and health sciences"],"mesh_terms":["Wortmannin","Phosphoinositide-3 Kinase Inhibitors","Androstadienes","Calorimetry, Differential Scanning","Enzyme Inhibitors","Humans","Magnetic Resonance Spectroscopy","Phosphorylation","Molecular Structure","Phosphatidylinositol 3-Kinases"],"keywords":["Wortmannin","LY294002","PI3K/AKT/mTOR pathway","Chemistry","In vivo","Potency","Pharmacology","Toxicity","Kinase","Biochemistry","In vitro","Signal transduction","Biology","prostate cancer","Pi3k Inhibitor","Wortmanin Synthesis","Magnetic Resonance Spectroscopy","Calorimetry, Differential Scanning","Molecular Structure","Organic chemistry","Article","Androstadienes","Phosphatidylinositol 3-Kinases","QD241-441","Humans","Enzyme Inhibitors","Phosphorylation","Phosphoinositide-3 Kinase Inhibitors"],"sdg_mappings":[{"sdg_number":2,"sdg_label":"2. 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