{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,2,25]],"date-time":"2025-02-25T06:10:02Z","timestamp":1740463802639,"version":"3.37.3"},"reference-count":98,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic &amp; Medicinal Chemistry"],"published-print":{"date-parts":[[2025,3]]},"DOI":"10.1016\/j.bmc.2024.118059","type":"journal-article","created":{"date-parts":[[2025,1,5]],"date-time":"2025-01-05T02:53:43Z","timestamp":1736045623000},"page":"118059","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":0,"special_numbering":"C","title":["Modeling, synthesis and cell-based evaluation of pyridine-substituted analogs of CD3254 and fluorinated analogs of CBt-PMN as novel therapeutics"],"prefix":"10.1016","volume":"119","author":[{"given":"Peter W.","family":"Jurutka","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zainab","family":"Khan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ichiro","family":"Kaneko","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michael A.","family":"Sausedo","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pritika H.","family":"Shahani","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mairi","family":"MacNeill","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aleksandra","family":"Grozic","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jaskaran","family":"Bhogal","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Johnathon","family":"Swierski","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michael R.","family":"Wentzel","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christine","family":"Chhun","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michael T.","family":"Applegate","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"San","family":"Raban","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Samir","family":"Ibrahim","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Karar","family":"Alwaeli","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tracie L.","family":"Feldman","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kayla J.","family":"Pomeroy","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Joseph T.","family":"Sarnowski","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Natalia","family":"Nguyen","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Joseph W.","family":"Ziller","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ning","family":"Ma","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Arjan","family":"van der Vaart","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jennifer F.","family":"Hackney","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pamela A.","family":"Marshall","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0380-4656","authenticated-orcid":false,"given":"Carl E.","family":"Wagner","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmc.2024.118059_b0005","series-title":"The retinoids","first-page":"319","author":"Mangelsdorf","year":"1994"},{"key":"10.1016\/j.bmc.2024.118059_b0010","doi-asserted-by":"crossref","first-page":"427","DOI":"10.1016\/0968-0004(92)90014-Z","article-title":"Multiplicity generates diversity in the retinoic acid signalling pathways","volume":"17","author":"Leid","year":"1992","journal-title":"Trends Biochem Sci"},{"key":"10.1016\/j.bmc.2024.118059_b0015","doi-asserted-by":"crossref","DOI":"10.3390\/foods12234205","article-title":"Dietary phenolic compounds exert some of their health-promoting bioactivities by targeting liver X receptor (LXR) and retinoid X receptor (RXR)","volume":"12","author":"Dom\u00ednguez-Avila","year":"2023","journal-title":"Foods"},{"key":"10.1016\/j.bmc.2024.118059_b0020","doi-asserted-by":"crossref","DOI":"10.3390\/cells12081201","article-title":"Steatosis and metabolic disorders associated with synergistic activation of the CAR\/RXR heterodimer by pesticides","volume":"12","author":"Dauwe","year":"2023","journal-title":"Cells"},{"key":"10.1016\/j.bmc.2024.118059_b0025","doi-asserted-by":"crossref","first-page":"51","DOI":"10.1016\/j.mce.2017.07.033","article-title":"RXR heterodimers orchestrate transcriptional control of neurogenesis and cell fate specification","volume":"471","author":"Simandi","year":"2018","journal-title":"Mol Cell Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0030","doi-asserted-by":"crossref","first-page":"1224","DOI":"10.1080\/21655979.2021.2020468","article-title":"Interleukin-17 promotes proliferation, migration, and invasion of trophoblasts via regulating PPAR-\u03b3\/RXR-\u03b1\/Wnt signaling","volume":"13","author":"Zhang","year":"2022","journal-title":"Bioengineered"},{"key":"10.1016\/j.bmc.2024.118059_b0035","doi-asserted-by":"crossref","first-page":"157","DOI":"10.1016\/j.biochi.2020.09.027","article-title":"Natural and synthetic retinoid X receptor ligands and their role in selected nuclear receptor action","volume":"179","author":"Brtko","year":"2020","journal-title":"Biochimie"},{"key":"10.1016\/j.bmc.2024.118059_b0040","doi-asserted-by":"crossref","first-page":"363","DOI":"10.1038\/s41574-020-0349-5","article-title":"Nuclear receptor crosstalk - defining the mechanisms for therapeutic innovation","volume":"16","author":"De Bosscher","year":"2020","journal-title":"Nat Rev Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0045","doi-asserted-by":"crossref","DOI":"10.1002\/jbm4.10432","article-title":"Vitamin D receptor mediates a myriad of biological actions dependent on its 1,25-dihydroxyvitamin D ligand: distinct regulatory themes revealed by induction of klotho and fibroblast growth factor-23","volume":"5","author":"Haussler","year":"2021","journal-title":"JBMR Plus"},{"key":"10.1016\/j.bmc.2024.118059_b0050","doi-asserted-by":"crossref","first-page":"36863","DOI":"10.1074\/jbc.R100047200","article-title":"Nuclear receptor minireview series","volume":"276","author":"Olefsky","year":"2001","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0055","doi-asserted-by":"crossref","first-page":"1610","DOI":"10.1210\/mend-3-10-1610","article-title":"A domain containing leucine-zipper-like motifs mediate novel in vivo interactions between the thyroid hormone and retinoic acid receptors","volume":"3","author":"Forman","year":"1989","journal-title":"Mol Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0060","doi-asserted-by":"crossref","first-page":"841","DOI":"10.1016\/0092-8674(95)90200-7","article-title":"The RXR heterodimers and orphan receptors","volume":"83","author":"Mangelsdorf","year":"1995","journal-title":"Cell"},{"key":"10.1016\/j.bmc.2024.118059_b0065","doi-asserted-by":"crossref","first-page":"587","DOI":"10.1038\/358587a0","article-title":"Homodimer formation of retinoid X receptor induced by 9-cis retinoic acid","volume":"358","author":"Zhang","year":"1992","journal-title":"Nature"},{"key":"10.1016\/j.bmc.2024.118059_b0070","doi-asserted-by":"crossref","first-page":"211","DOI":"10.1677\/jme.0.0270211","article-title":"Distinct retinoid X receptor activation function-2 residues mediate transactivation in homodimeric and vitamin D receptor heterodimeric contexts","volume":"27","author":"Thompson","year":"2001","journal-title":"J Mol Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0075","doi-asserted-by":"crossref","DOI":"10.1016\/j.jbc.2023.102896","article-title":"Agonist-controlled competition of RAR and VDR nuclear receptors for heterodimerization with RXR is manifested in their DNA binding","volume":"299","author":"Reh\u00f3","year":"2023","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0080","doi-asserted-by":"crossref","first-page":"4625","DOI":"10.1093\/emboj\/cdg456","article-title":"Crystal structure of the heterodimeric complex of LXR\u03b1 and RXR\u03b2 ligand\u2010binding domains in a fully agonistic conformation","volume":"22","author":"Svensson","year":"2003","journal-title":"EMBO J"},{"key":"10.1016\/j.bmc.2024.118059_b0085","doi-asserted-by":"crossref","first-page":"1227","DOI":"10.4155\/fmc-2020-0069","article-title":"Identifying new liver X receptor alpha modulators and distinguishing between agonists and antagonists by crystal ligand pocket screening","volume":"12","author":"Lee","year":"2020","journal-title":"Fut Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0090","doi-asserted-by":"crossref","first-page":"17323","DOI":"10.1073\/pnas.0705356104","article-title":"Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function","volume":"104","author":"Nahoum","year":"2007","journal-title":"PNAS USA"},{"key":"10.1016\/j.bmc.2024.118059_b0095","doi-asserted-by":"crossref","first-page":"2218","DOI":"10.1210\/me.2010-0215","article-title":"Research resource: transcriptome profiling of genes regulated by RXR and its permissive and nonpermissive partners in differentiating monocyte-derived dendritic cells","volume":"24","author":"Sz\u00e9les","year":"2010","journal-title":"Mol Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0100","doi-asserted-by":"crossref","first-page":"105","DOI":"10.1016\/j.abb.2008.02.003","article-title":"Corepressor interaction differentiates the permissive and non-permissive retinoid X receptor heterodimers","volume":"472","author":"Lammi","year":"2008","journal-title":"Arch Biochem Biophys"},{"key":"10.1016\/j.bmc.2024.118059_b0105","doi-asserted-by":"crossref","first-page":"541","DOI":"10.1016\/0092-8674(95)90075-6","article-title":"Unique response pathways are established by allosteric interactions among nuclear hormone receptors","volume":"81","author":"Forman","year":"1995","journal-title":"Cell"},{"key":"10.1016\/j.bmc.2024.118059_b0110","doi-asserted-by":"crossref","first-page":"57","DOI":"10.1016\/j.bbalip.2011.04.003","article-title":"Modulation of RXR function through ligand design","volume":"1821","author":"P\u00e9rez","year":"2012","journal-title":"Biochim Biophys Acta"},{"key":"10.1016\/j.bmc.2024.118059_b0115","doi-asserted-by":"crossref","first-page":"450","DOI":"10.1038\/383450a0","article-title":"Activation of specific RXR heterodimers by an antagonist of RXR homodimers","volume":"383","author":"Lala","year":"1996","journal-title":"Nature"},{"key":"10.1016\/j.bmc.2024.118059_b0120","doi-asserted-by":"crossref","first-page":"1006","DOI":"10.1128\/MCB.16.3.1006","article-title":"Selective effects of ligands on vitamin D3 receptor- and retinoid X receptor-mediated gene activation in vivo","volume":"16","author":"Lemon","year":"1996","journal-title":"Mol Cell Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0125","first-page":"5907","article-title":"Retinoid X receptors stimulate and 9-cis retinoic acid inhibits 1,25-dihydroxyvitamin D3-activated expression of the rat osteocalcin gene","volume":"13","author":"MacDonald","year":"1993","journal-title":"Mol Cell Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0130","doi-asserted-by":"crossref","first-page":"8483","DOI":"10.1074\/jbc.273.14.8483","article-title":"Heterodimeric DNA binding by the vitamin D receptor and retinoid X receptors is enhanced by 1,25-dihydroxyvitamin D3 and inhibited by 9-cis-retinoic acid: evidence for allosteric receptor interactions","volume":"273","author":"Thompson","year":"1998","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0135","first-page":"7698","article-title":"Formation of retinoid X receptor homodimers leads to repression of T3 response: hormonal cross talk by ligand-induced squelching","volume":"13","author":"Lehmann","year":"1993","journal-title":"Mol Cell Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0140","doi-asserted-by":"crossref","first-page":"13060","DOI":"10.1074\/jbc.272.20.13060","article-title":"Thyroid hormone-mediated enhancement of heterodimer formation between thyroid hormone receptor beta and retinoid X receptor","volume":"272","author":"Collingwood","year":"1997","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0145","doi-asserted-by":"crossref","first-page":"1367","DOI":"10.1210\/mend.12.9.0165","article-title":"Thyroid hormone receptor does not heterodimerize with the vitamin D receptor but represses vitamin D receptor-mediated transactivation","volume":"12","author":"Raval-Pandya","year":"1998","journal-title":"Mol Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0150","doi-asserted-by":"crossref","first-page":"462","DOI":"10.1002\/(SICI)1097-4644(19991201)75:3<462::AID-JCB11>3.0.CO;2-D","article-title":"Vitamin D receptor displays DNA binding and transactivation as a heterodimer with the retinoid X receptor, but not with the thyroid hormone receptor","volume":"75","author":"Thompson","year":"1999","journal-title":"J Cell Biochem"},{"key":"10.1016\/j.bmc.2024.118059_b0155","doi-asserted-by":"crossref","first-page":"10910","DOI":"10.1074\/jbc.271.18.10910","article-title":"Vitamin D receptors repress basal transcription and exert dominant negative activity on triiodothyronine-mediated transcriptional activity","volume":"271","author":"Yen","year":"1996","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0160","doi-asserted-by":"crossref","first-page":"793","DOI":"10.1038\/nrd2397","article-title":"RAR and RXR modulation in cancer and metabolic disease","volume":"6","author":"Altucci","year":"2007","journal-title":"Nat Rev Drug Discov"},{"key":"10.1016\/j.bmc.2024.118059_b0165","doi-asserted-by":"crossref","first-page":"1944","DOI":"10.1126\/science.1335166","article-title":"Retinoids selective for retinoid X receptor response pathways","volume":"258","author":"Lehmann","year":"1992","journal-title":"Science"},{"key":"10.1016\/j.bmc.2024.118059_b0170","doi-asserted-by":"crossref","first-page":"2605","DOI":"10.1021\/jm00070a003","article-title":"Conformational effects on retinoid receptor selectivity. 1. Effect of 9-double bond geometry on retinoid X receptor activity","volume":"36","author":"Jong","year":"1993","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0175","doi-asserted-by":"crossref","first-page":"3368","DOI":"10.1021\/jm00017a021","article-title":"Conformational effects on retinoid receptor selectivity. 2. Effects of retinoid bridging group on retinoid X receptor activity and selectivity","volume":"38","author":"Dawson","year":"1995","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0180","doi-asserted-by":"crossref","first-page":"2930","DOI":"10.1021\/jm00044a014","article-title":"Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids","volume":"37","author":"Boehm","year":"1994","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0185","doi-asserted-by":"crossref","first-page":"3192","DOI":"10.1021\/om040143k","article-title":"Synthesis, crystal structure analysis, and pharmacological characterization of disila-bexarotene, a disila-analogue of the RXR-selective retinoid agonist bexarotene","volume":"24","author":"Daiss","year":"2005","journal-title":"Organometallics"},{"key":"10.1016\/j.bmc.2024.118059_b0190","doi-asserted-by":"crossref","first-page":"225","DOI":"10.1016\/j.canlet.2005.09.010","article-title":"Differentiation and growth inhibition mediated via the RXR:PPAR\u03b3 heterodimer in colon cancer","volume":"240","author":"Cesario","year":"2006","journal-title":"Cancer Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0195","doi-asserted-by":"crossref","first-page":"141","DOI":"10.1007\/s10549-004-1426-5","article-title":"Synergistic effect of a retinoid X receptor-selective ligand bexarotene (LGD1069, Targretin) and paclitaxel (Taxol) in mammary carcinoma","volume":"88","author":"Yen","year":"2004","journal-title":"Breast Cancer Res Treat"},{"key":"10.1016\/j.bmc.2024.118059_b0200","doi-asserted-by":"crossref","first-page":"838","DOI":"10.1093\/jnci\/djad062","article-title":"Inverse agonists of retinoic acid receptor\/retinoid X receptor signaling as lineage-specific antitumor agents against human adenoid cystic carcinoma","volume":"115","author":"Viragova","year":"2023","journal-title":"J Natl Cancer Inst"},{"key":"10.1016\/j.bmc.2024.118059_b0205","doi-asserted-by":"crossref","first-page":"8656","DOI":"10.1158\/1078-0432.CCR-04-0979","article-title":"A selective retinoid X receptor agonist bexarotene (targretin) prevents and overcomes acquired paclitaxel (taxol) resistance in human non\u2013small cell lung cancer","volume":"10","author":"Yen","year":"2004","journal-title":"Clin Cancer Res"},{"key":"10.1016\/j.bmc.2024.118059_b0210","doi-asserted-by":"crossref","first-page":"1794","DOI":"10.1158\/1078-0432.CCR-06-1836","article-title":"A proof-of-principle clinical trial of bexarotene in patients with non\u2013small cell lung cancer","volume":"13","author":"Dragnev","year":"2007","journal-title":"Clin Cancer Res"},{"key":"10.1016\/j.bmc.2024.118059_b0215","doi-asserted-by":"crossref","first-page":"407","DOI":"10.1038\/386407a0","article-title":"Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists","volume":"386","author":"Mukherjee","year":"1997","journal-title":"Nature"},{"key":"10.1016\/j.bmc.2024.118059_b0220","doi-asserted-by":"crossref","first-page":"1075","DOI":"10.1056\/NEJM199904083401404","article-title":"Central hypothyroidism associated with retinoid X receptor\u2013selective ligands","volume":"340","author":"Sherman","year":"1999","journal-title":"N Engl J Med"},{"key":"10.1016\/j.bmc.2024.118059_b0225","doi-asserted-by":"crossref","first-page":"5782","DOI":"10.1128\/MCB.22.16.5782-5792.2002","article-title":"Functional evidence for retinoid X receptor (RXR) as a nonsilent partner in the thyroid hormone receptor\/RXR heterodimer","volume":"22","author":"Li","year":"2002","journal-title":"Mol Cell Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0230","doi-asserted-by":"crossref","first-page":"1054","DOI":"10.1194\/jlr.M100358-JLR200","article-title":"LXR\/RXR activation enhances basolateral efflux of cholesterol in CaCo-2 cells","volume":"43","author":"Murthy","year":"2002","journal-title":"J Lipid Res"},{"key":"10.1016\/j.bmc.2024.118059_b0235","doi-asserted-by":"crossref","first-page":"905","DOI":"10.1194\/jlr.M300473-JLR200","article-title":"LXR\/RXR ligand activation enhances basolateral efflux of beta-sitosterol in CaCo-2 cells","volume":"45","author":"Field","year":"2004","journal-title":"J Lipid Res"},{"key":"10.1016\/j.bmc.2024.118059_b0240","doi-asserted-by":"crossref","first-page":"528","DOI":"10.1016\/S0022-3565(24)36898-3","article-title":"Receptor specificity of retinoid-induced epidermal hyperplasia: effect of RXR-selective agonists and correlation with topical irritation","volume":"282","author":"Thacher","year":"1997","journal-title":"J Pharmacol Exp Ther"},{"key":"10.1016\/j.bmc.2024.118059_b0245","doi-asserted-by":"crossref","first-page":"1430","DOI":"10.1021\/cn400100f","article-title":"Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson\u2019s disease","volume":"4","author":"McFarland","year":"2013","journal-title":"ACS Chem Nerosci"},{"key":"10.1016\/j.bmc.2024.118059_b0250","doi-asserted-by":"crossref","DOI":"10.1126\/science.1217697","article-title":"ApoE-directed therapeutics rapidly clear \u03b2-amyloid and reverse deficits in AD mouse models","volume":"335","author":"Cramer","year":"2012","journal-title":"Science"},{"key":"10.1016\/j.bmc.2024.118059_b0255","doi-asserted-by":"crossref","first-page":"924","DOI":"10.1126\/science.1234114","article-title":"Response to comments on \u201cApoE-directed therapeutics rapidly clear \u03b2-amyloid and reverse deficits in AD mouse models\u201d","volume":"340","author":"Landreth","year":"2013","journal-title":"Science"},{"key":"10.1016\/j.bmc.2024.118059_b0260","doi-asserted-by":"crossref","first-page":"4","DOI":"10.1186\/s13195-016-0173-2","article-title":"Double-blind, placebo-controlled, proof-of-concept trial of bexarotene Xin moderate Alzheimer\u2019s disease","volume":"8","author":"Cummings","year":"2016","journal-title":"Alzheimer's Res Ther"},{"key":"10.1016\/j.bmc.2024.118059_b0265","doi-asserted-by":"crossref","DOI":"10.1080\/14728214.2023.2296079","article-title":"Cancer drugs with high repositioning potential for Alzheimer\u2019s disease","author":"Majeed","year":"2023","journal-title":"Expert Opin Emerg Drugs"},{"key":"10.1016\/j.bmc.2024.118059_b0270","doi-asserted-by":"crossref","first-page":"2298","DOI":"10.1021\/jm0100584","article-title":"Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes","volume":"44","author":"Vuligonda","year":"2001","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0275","doi-asserted-by":"crossref","first-page":"1679","DOI":"10.1021\/jm970635h","article-title":"Conformationally defined retinoic acid analogues. 4. Potential new agents for acute promyelocytic and juvenile myelomonocytic leukemias","volume":"41","author":"Muccio","year":"1998","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0280","doi-asserted-by":"crossref","first-page":"3766","DOI":"10.1021\/jm030095q","article-title":"Conformationally defined retinoic acid analogues. 5. Large-scale synthesis and mammary cancer chemopreventive activity for (2E,4E,6Z,8E)-8-(3\u2032,4\u2032-Dihydro-1\u2032(2\u2032H)-naphthalen-1\u2032-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acid (9cUAB30)","volume":"46","author":"Atigadda","year":"2003","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0285","doi-asserted-by":"crossref","first-page":"1565","DOI":"10.1158\/1940-6207.CAPR-10-0149","article-title":"A pilot, first-in-human, pharmacokinetic study of 9cUAB30 in healthy volunteers","volume":"3","author":"Kolesar","year":"2010","journal-title":"Cancer Prev Res"},{"key":"10.1016\/j.bmc.2024.118059_b0290","first-page":"641","article-title":"The low-toxicity 9-cis UAB30 novel retinoid down-regulates the DNA methyltransferases and has anti-telomerase activity in human breast cancer cells","volume":"30","author":"Hansen","year":"2007","journal-title":"Int J Oncol"},{"key":"10.1016\/j.bmc.2024.118059_b0295","doi-asserted-by":"crossref","first-page":"5370","DOI":"10.1021\/jm5004792","article-title":"Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity","volume":"57","author":"Atigadda","year":"2014","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0300","doi-asserted-by":"crossref","first-page":"178","DOI":"10.1016\/j.bmc.2013.11.039","article-title":"Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention","volume":"22","author":"Desphande","year":"2014","journal-title":"Bioorg Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0305","doi-asserted-by":"crossref","first-page":"2152","DOI":"10.1021\/acs.jmedchem.3c02095","article-title":"Structure-guided design of a highly potent partial RXR agonist with superior physicochemical properties","volume":"67","author":"Lewandowski","year":"2024","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0310","doi-asserted-by":"crossref","first-page":"16762","DOI":"10.1021\/acs.jmedchem.3c01435","article-title":"Structural fusion of natural and synthetic ligand features boosts RXR agonist potency","volume":"66","author":"Adouvi","year":"2023","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0315","doi-asserted-by":"crossref","first-page":"2683","DOI":"10.1021\/jm020340q","article-title":"Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes","volume":"46","author":"Michellys","year":"2003","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0320","doi-asserted-by":"crossref","first-page":"4087","DOI":"10.1021\/jm020401k","article-title":"Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids","volume":"46","author":"Michellys","year":"2003","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0325","doi-asserted-by":"crossref","first-page":"1593","DOI":"10.1016\/j.bmcl.2003.12.089","article-title":"Design, synthesis and structure-activity relationship of novel RXR-selective modulators","volume":"14","author":"Michellys","year":"2004","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0330","doi-asserted-by":"crossref","first-page":"5950","DOI":"10.1021\/jm900496b","article-title":"Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene)","volume":"52","author":"Wagner","year":"2009","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0335","doi-asserted-by":"crossref","first-page":"3146","DOI":"10.1021\/jm00016a018","article-title":"Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells","volume":"38","author":"Boehm","year":"1995","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0340","doi-asserted-by":"crossref","first-page":"701","DOI":"10.1002\/jlcr.2580360712","article-title":"Syntheses of isotopically labeled 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethenyl]benzoic acid (LGD1069), a potent retinoid x receptor-selective ligand","volume":"36","author":"Zhang","year":"1995","journal-title":"J. Labelled Comp. Radiopharm."},{"key":"10.1016\/j.bmc.2024.118059_b0345","doi-asserted-by":"crossref","first-page":"5772","DOI":"10.1021\/jo0103064","article-title":"Synthesis of novel retinoid X receptor-selective retinoids","volume":"66","author":"Faul","year":"2001","journal-title":"J Org Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0350","doi-asserted-by":"crossref","first-page":"3150","DOI":"10.1021\/jm900096q","article-title":"Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers","volume":"52","author":"Sant\u00edn","year":"2009","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0355","doi-asserted-by":"crossref","first-page":"447","DOI":"10.1038\/sj.cdd.4400673","article-title":"Retinoid-dependent growth inhibition, differentiation and apoptosis in acute promyelocytic leukemia cells. Expression and activation of caspases","volume":"7","author":"Gianni","year":"2000","journal-title":"Cell Death Differ"},{"key":"10.1016\/j.bmc.2024.118059_b0360","doi-asserted-by":"crossref","DOI":"10.1002\/prp2.122","article-title":"Analysis of differential secondary effects of novel rexinoids: select rexinoid X receptor ligands demonstrate differentiated side effect profiles","volume":"3","author":"Marshall","year":"2015","journal-title":"Pharmacol Res Perspect"},{"key":"10.1016\/j.bmc.2024.118059_b0365","doi-asserted-by":"crossref","first-page":"5139","DOI":"10.1016\/j.bmcl.2010.07.012","article-title":"Modification at the acidic domain of RXR agonists has little effect on permissive RXR-heterodimer activation","volume":"20","author":"Fujii","year":"2010","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0370","doi-asserted-by":"crossref","first-page":"521","DOI":"10.1021\/ml100184k","article-title":"Modification at the lipophilic domain of RXR agonists differentially influences activation of RXR heterodimers","volume":"1","author":"Ohsawa","year":"2010","journal-title":"ACS Med Chem Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0375","doi-asserted-by":"crossref","first-page":"427","DOI":"10.1021\/ml300055n","article-title":"RXR partial agonist CBt-PMN exerts therapeutic effects on type 2 diabetes without the side effects of RXR full agonists","volume":"3","author":"Kakuta","year":"2012","journal-title":"ACS Med Chem Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0380","doi-asserted-by":"crossref","first-page":"629","DOI":"10.1248\/bpb.35.629","article-title":"Feasibility of structural modification of retinoid X receptor agonists to separate blood glucose-lowering action from adverse effects: studies in KKA<sup>y<\/sup> type 2 diabetes model mice","volume":"35","author":"Kakuta","year":"2012","journal-title":"Biol Pharm Bull"},{"key":"10.1016\/j.bmc.2024.118059_b0385","doi-asserted-by":"crossref","first-page":"1865","DOI":"10.1021\/jm400033f","article-title":"Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency","volume":"56","author":"Ohsawa","year":"2013","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0390","doi-asserted-by":"crossref","first-page":"544","DOI":"10.1248\/bpb.21.544","article-title":"Potent retinoid synergists with a diphenylamine skeleton","volume":"21","author":"Ohta","year":"1998","journal-title":"Biol Pharm Bull"},{"key":"10.1016\/j.bmc.2024.118059_b0395","first-page":"15","article-title":"Retinoid Activity Regulators","author":"Kagechika","year":"1998","journal-title":"European Patent WO9845242A1"},{"key":"10.1016\/j.bmc.2024.118059_b0400","doi-asserted-by":"crossref","first-page":"2501","DOI":"10.1016\/j.bmc.2011.03.026","article-title":"Diphenylamine-based retinoid antagonists: regulation of RAR and RXR function depending on the N-substituent","volume":"19","author":"Ohta","year":"2011","journal-title":"Bioorg Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0405","doi-asserted-by":"crossref","first-page":"8924","DOI":"10.1021\/acs.jmedchem.6b00812","volume":"59","author":"Heck","year":"2016","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0410","doi-asserted-by":"crossref","DOI":"10.3390\/ijms232416213","article-title":"An isochroman analog of CD3254 and allyl-, isochroman-analogs of NEt-TMN prove to be more potent retinoid-X-receptor (RXR) selective agonists than bexarotene","volume":"23","author":"Jurutka","year":"2022","journal-title":"Int J Mol Sci"},{"key":"10.1016\/j.bmc.2024.118059_b0415","doi-asserted-by":"crossref","first-page":"987","DOI":"10.1210\/mend.16.5.0823","article-title":"Molecular recognition of agonist ligands by RXRs","volume":"16","author":"Egea","year":"2002","journal-title":"Mol Endocrinol"},{"key":"10.1016\/j.bmc.2024.118059_b0420","doi-asserted-by":"crossref","first-page":"2010","DOI":"10.1021\/jm030565g","article-title":"Structure-based design of potent retinoid X receptor alpha agonists","volume":"47","author":"Haffner","year":"2004","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0425","doi-asserted-by":"crossref","first-page":"1143","DOI":"10.1002\/cmdc.200900090","article-title":"Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology","volume":"4","author":"Lippert","year":"2009","journal-title":"ChemMedChem"},{"key":"10.1016\/j.bmc.2024.118059_b0430","doi-asserted-by":"crossref","first-page":"350","DOI":"10.1038\/nature07413","article-title":"Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA","volume":"456","author":"Chandra","year":"2008","journal-title":"Nature"},{"key":"10.1016\/j.bmc.2024.118059_b0435","doi-asserted-by":"crossref","first-page":"3550","DOI":"10.1016\/j.bmcl.2009.04.151","article-title":"Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma","volume":"19","author":"Connors","year":"2009","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmc.2024.118059_b0440","article-title":"(+)-Rutamarin as a dual inducer of both GLUT4 translocation and expression efficiently ameliorates glucose homeostasis in insulin-resistant mice","volume":"7","author":"Zhang","year":"2012","journal-title":"PLoS One"},{"key":"10.1016\/j.bmc.2024.118059_b0445","doi-asserted-by":"crossref","first-page":"11385","DOI":"10.1074\/jbc.M110869200","article-title":"The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12","volume":"277","author":"Love","year":"2002","journal-title":"J Biol Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0450","doi-asserted-by":"crossref","first-page":"120","DOI":"10.1016\/j.jmb.2010.04.005","article-title":"X-ray structures of the LXR\u03b1 LBD in its homodimeric form and implications for heterodimer signaling","volume":"399","author":"Fradera","year":"2010","journal-title":"J Mol Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0455","doi-asserted-by":"crossref","first-page":"801","DOI":"10.1038\/nsmb.1855","article-title":"A unique secondary-structure switch controls constitutive gene repression by retinoic acid receptor","volume":"17","author":"le Maire","year":"2010","journal-title":"Nat Struct Mol Biol"},{"key":"10.1016\/j.bmc.2024.118059_b0460","doi-asserted-by":"crossref","first-page":"2785","DOI":"10.1002\/jcc.21256","article-title":"AutoDock4 and AutoDockTools4: automated docking with selective receptor flexibility","volume":"30","author":"Morris","year":"2009","journal-title":"J Comput Chem"},{"key":"10.1016\/j.bmc.2024.118059_b0465","doi-asserted-by":"crossref","first-page":"460","DOI":"10.1021\/ci500588j","article-title":"DataWarrior: an open-source program for chemistry aware data visualization and analysis","volume":"55","author":"Sander","year":"2015","journal-title":"J Chem Inf Model"},{"key":"10.1016\/j.bmc.2024.118059_b0470","doi-asserted-by":"crossref","DOI":"10.1038\/srep42717","article-title":"SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules","volume":"7","author":"Daina","year":"2017","journal-title":"Sci Rep"},{"key":"10.1016\/j.bmc.2024.118059_b0475","doi-asserted-by":"crossref","first-page":"767","DOI":"10.1021\/acschemneuro.6b00029","article-title":"Central nervous system multiparameter optimization desirability: application in drug discovery","volume":"7","author":"Wager","year":"2016","journal-title":"ACS Chem Nerosci"},{"key":"10.1016\/j.bmc.2024.118059_b0480","doi-asserted-by":"crossref","first-page":"235","DOI":"10.1016\/S1056-8719(00)00107-6","article-title":"Drug-like properties and the causes of poor solubility and poor permeability","volume":"44","author":"Lipinski","year":"2000","journal-title":"J Pharmacol Toxicol Methods"},{"key":"10.1016\/j.bmc.2024.118059_b0485","doi-asserted-by":"crossref","first-page":"W566","DOI":"10.1093\/nar\/gkv468","article-title":"ClustVis: a web tool for visualizing clustering of multivariate data using Principal Component Analysis and heatmap","volume":"43","author":"Metsalu","year":"2015","journal-title":"Nucleic Acids Res"},{"key":"10.1016\/j.bmc.2024.118059_b0490","doi-asserted-by":"crossref","first-page":"8432","DOI":"10.1021\/jm4008517","volume":"56","author":"Jurutka","year":"2013","journal-title":"J Med Chem"}],"container-title":["Bioorganic &amp; Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089624004735?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089624004735?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,2,25]],"date-time":"2025-02-25T05:21:59Z","timestamp":1740460919000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0968089624004735"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,3]]},"references-count":98,"alternative-id":["S0968089624004735"],"URL":"https:\/\/doi.org\/10.1016\/j.bmc.2024.118059","relation":{},"ISSN":["0968-0896"],"issn-type":[{"type":"print","value":"0968-0896"}],"subject":[],"published":{"date-parts":[[2025,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Modeling, synthesis and cell-based evaluation of pyridine-substituted analogs of CD3254 and fluorinated analogs of CBt-PMN as novel therapeutics","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmc.2024.118059","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2024 Published by Elsevier Ltd.","name":"copyright","label":"Copyright"}],"article-number":"118059"}}