{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,28]],"date-time":"2026-09-28T03:57:11Z","timestamp":1790567831750,"version":"4.1.0"},"reference-count":55,"publisher":"Wiley","issue":"18","license":[{"start":{"date-parts":[[2026,9,20]],"date-time":"2026-09-20T00:00:00Z","timestamp":1789862400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"},{"start":{"date-parts":[[2026,9,20]],"date-time":"2026-09-20T00:00:00Z","timestamp":1789862400000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/doi.wiley.com\/10.1002\/tdm_license_1.1"}],"funder":[{"DOI":"10.13039\/501100004704","name":"National Research Council of Thailand","doi-asserted-by":"publisher","award":["N42A661000"],"award-info":[{"award-number":["N42A661000"]}],"id":[{"id":"10.13039\/501100004704","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2026,9,28]]},"abstract":"<jats:p>\n                    Caspase\u20101 is a key marker in pyroptosis and inflammation, playing a central role in the pathogenesis of various acute and chronic inflammatory diseases. While some caspase\u20101 sensing and inhibition studies have been reported, the use of DHPs for these applications remains unexplored. To address this challenge, a novel fluorescent compound,\n                    <jats:bold>zWEHD\u2010NH\u2010DHP<\/jats:bold>\n                    , was synthesized and subsequently developed as a real\u2010time caspase\u20101 detection in vitro and in cells. Furthermore, a new class of potential caspase\u20101 inhibitors was investigated through the screening of a series of nonfluorogenic DHPs, utilizing our established caspase\u20101 fluorescent sensing system. Among the tested compounds,\n                    <jats:bold>THD<\/jats:bold>\n                    and\n                    <jats:bold>FD<\/jats:bold>\n                    showed caspase\u20101 inhibition with IC\n                    <jats:sub>50<\/jats:sub>\n                    values of 2.8\u2009\u00b1\u20090.1\u2009nM and 3.2\u2009\u00b1\u20090.1\u2009\u00b5M, respectively.\n                    <jats:bold>THD<\/jats:bold>\n                    , which exhibited comparable potency to the well\u2010known inhibitor VX\u2010765 (3.68\u2009nM), was selected for further investigation. Moreover, a competitive inhibition mechanism of\n                    <jats:bold>THD<\/jats:bold>\n                    at the enzyme's active site was supported by molecular docking and MD simulations. Western blot analysis of PMA\u2010differentiated THP\u20101 cells further supported this observation by showing reduced cleaved IL\u20101\u03b2 levels in the presence of\n                    <jats:bold>THD<\/jats:bold>\n                    . This inhibitory effect of\n                    <jats:bold>THD<\/jats:bold>\n                    on caspase\u20101 activity in a complex cell system was further confirmed by the concentration\u2010dependent morphological changes in BMDMs.\n                  <\/jats:p>","DOI":"10.1002\/cmdc.70496","type":"journal-article","created":{"date-parts":[[2026,9,21]],"date-time":"2026-09-21T02:32:07Z","timestamp":1789957927000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Potent Caspase\u20101 Antagonists From Dihydropyridine Derivatives: In Vitro Fluorescence Assays and Cell Imaging"],"prefix":"10.1002","volume":"21","author":[{"ORCID":"https:\/\/orcid.org\/0009-0006-5180-4924","authenticated-orcid":false,"given":"Kittiporn","family":"Nakprasit","sequence":"first","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Thitiporn","family":"Pattarakankul","sequence":"additional","affiliation":[{"name":"Department of Microbiology Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8734-6626","authenticated-orcid":false,"given":"Tanapat","family":"Palaga","sequence":"additional","affiliation":[{"name":"Department of Microbiology Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9322-0261","authenticated-orcid":false,"given":"Thanapon","family":"Charoenwongpaiboon","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Silpakorn University  Nakhon Pathom Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0005-0550-9791","authenticated-orcid":false,"given":"Waroton","family":"Paisuwan","sequence":"additional","affiliation":[{"name":"Futuristic Science Research Center School of Science Walailak University  Nakhon Si Thammarat Thailand"},{"name":"Functional Materials and Nanotechnology Center of Excellence School of Science Walailak University  Nakhon Si Thammarat Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kavisara","family":"Srithadindang","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0007-5691-8303","authenticated-orcid":false,"given":"Rachanon","family":"Eakprachasin","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Islah","family":"Muttaqin","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pattraporn","family":"Chobpradit","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sucharat","family":"Sanongkiet","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Silpakorn University  Nakhon Pathom Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mongkol","family":"Sukwattanasinitt","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chanakan","family":"Tongsook","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Silpakorn University  Nakhon Pathom Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1837-6669","authenticated-orcid":false,"given":"Anawat","family":"Ajavakom","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science Chulalongkorn University  Bangkok Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2026,9,20]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1582\u20104934.2008.00292.x"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1038\/nri1997"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1038\/nri.2015.7"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/S1097\u20102765(02)00599\u20103"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1083\/jcb.201602089"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41577\u2010019\u20100215\u20107"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1038\/nature10759"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41421\u2010020\u20100167\u2010x"},{"key":"e_1_2_8_10_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41590\u2010021\u201000886\u20105"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.abe1707"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2018.09.047"},{"key":"e_1_2_8_13_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41586\u2010021\u201003341\u20105"},{"key":"e_1_2_8_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.phymed.2023.155019"},{"key":"e_1_2_8_15_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41583\u2010018\u20100055\u20107"},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.intimp.2023.110293"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.3390\/biom9120850"},{"key":"e_1_2_8_18_1","doi-asserted-by":"publisher","DOI":"10.1002\/mco2.249"},{"key":"e_1_2_8_19_1","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.106.111344"},{"issue":"4","key":"e_1_2_8_20_1","first-page":"473","article-title":"Pharmacological Caspase Inhibitors: Research Towards Therapeutic Perspectives","volume":"66","author":"Kudelova J.","year":"2015","journal-title":"Journal of Physiology and Pharmacology"},{"key":"e_1_2_8_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.biopha.2021.111442"},{"key":"e_1_2_8_22_1","doi-asserted-by":"publisher","DOI":"10.1007\/s10495\u2010026\u201002307\u20100"},{"key":"e_1_2_8_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.imlet.2022.03.003"},{"key":"e_1_2_8_24_1","doi-asserted-by":"publisher","DOI":"10.1038\/nm.3806"},{"key":"e_1_2_8_25_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.4c01558"},{"key":"e_1_2_8_26_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm501072b"},{"key":"e_1_2_8_27_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jim.2017.03.004"},{"key":"e_1_2_8_28_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.snb.2015.05.077"},{"key":"e_1_2_8_29_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.chembiol.2010.07.011"},{"key":"e_1_2_8_30_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bios.2022.114812"},{"key":"e_1_2_8_31_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsami.7b14845"},{"key":"e_1_2_8_32_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.biomaterials.2019.119543"},{"key":"e_1_2_8_33_1","doi-asserted-by":"publisher","DOI":"10.1593\/neo.03214"},{"key":"e_1_2_8_34_1","doi-asserted-by":"publisher","DOI":"10.1039\/D5SC07690K"},{"key":"e_1_2_8_35_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.drudis.2009.08.004"},{"key":"e_1_2_8_36_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2017.03.005"},{"key":"e_1_2_8_37_1","doi-asserted-by":"publisher","DOI":"10.1155\/2016\/1892412"},{"key":"e_1_2_8_38_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmcr.2026.100339"},{"key":"e_1_2_8_39_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tet.2010.04.102"},{"key":"e_1_2_8_40_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.joc.3c01455"},{"key":"e_1_2_8_41_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tet.2012.11.094"},{"key":"e_1_2_8_42_1","unstructured":"W. P.Islah Muttaqin T.Pattarakankul andT.Palaga M.Sukwattanasinitt andA.Ajavakom \u201cThiocarbonyl 1 4\u2010Dihydropyridine\u2010Based Fluorescent Chemosensor Candidate for Heavy Metal Ions Detection in Aqueous Solution and Its Potential Application in Living Cells \u201d in16th Eurasia Conference on Chemical Science 2023(The Berkeley Hotel Pratunam 2023) 206\u2013211."},{"key":"e_1_2_8_43_1","doi-asserted-by":"publisher","DOI":"10.3390\/s23010436"},{"key":"e_1_2_8_44_1","doi-asserted-by":"publisher","DOI":"10.1039\/C4AN01843E"},{"key":"e_1_2_8_45_1","doi-asserted-by":"publisher","DOI":"10.1038\/cdd.2017.44"},{"key":"e_1_2_8_46_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.abb.2021.108753"},{"key":"e_1_2_8_47_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.sintl.2025.100349"},{"key":"e_1_2_8_48_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ab.2017.11.023"},{"key":"e_1_2_8_49_1","doi-asserted-by":"publisher","DOI":"10.1159\/000517855"},{"key":"e_1_2_8_50_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.sbsr.2021.100470"},{"key":"e_1_2_8_51_1","first-page":"12","article-title":"1,4\u2010Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family","volume":"4","author":"Cataldi M.","year":"2012","journal-title":"Translational Medicine @ Unisa"},{"key":"e_1_2_8_52_1","doi-asserted-by":"publisher","DOI":"10.1002\/jhet.5570450316"},{"key":"e_1_2_8_53_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsmedchemlett.5c00677"},{"key":"e_1_2_8_54_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41467\u2010018\u201006449\u2010x"},{"key":"e_1_2_8_55_1","doi-asserted-by":"publisher","DOI":"10.3389\/fimmu.2016.00597"},{"key":"e_1_2_8_56_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jim.2016.01.012"}],"container-title":["ChemMedChem"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/cmdc.70496","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/full-xml\/10.1002\/cmdc.70496","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/cmdc.70496","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,9,28]],"date-time":"2026-09-28T03:40:27Z","timestamp":1790566827000},"score":1,"resource":{"primary":{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/10.1002\/cmdc.70496"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,9,20]]},"references-count":55,"journal-issue":{"issue":"18","published-print":{"date-parts":[[2026,9,28]]}},"alternative-id":["10.1002\/cmdc.70496"],"URL":"https:\/\/doi.org\/10.1002\/cmdc.70496","archive":["Portico"],"relation":{},"ISSN":["1860-7179","1860-7187"],"issn-type":[{"value":"1860-7179","type":"print"},{"value":"1860-7187","type":"electronic"}],"subject":[],"published":{"date-parts":[[2026,9,20]]},"assertion":[{"value":"2026-01-30","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2026-08-25","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2026-09-20","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e70496"}}