{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,4]],"date-time":"2026-09-04T09:15:59Z","timestamp":1788513359024,"version":"build-2803163510"},"reference-count":51,"publisher":"Oxford University Press (OUP)","issue":"16","license":[{"start":{"date-parts":[[2026,9,4]],"date-time":"2026-09-04T00:00:00Z","timestamp":1788480000000},"content-version":"vor","delay-in-days":11,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","award":["R01CA177585"],"award-info":[{"award-number":["R01CA177585"]}],"id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Purdue Institute for Cancer Research"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2026,8,24]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>Overexpression of PDGFR-\u03b2 (platelet-derived growth factor receptor beta) kinase contributes to diverse human diseases, including cancers, cardiovascular disorders, and fibrosis. G-quadruplexes (G4s) formed in the PDGFR-\u03b2 promoter act as transcriptional repressors and represent attractive therapeutic targets. We previously reported that the major G4-forming region of the PDGFR-\u03b2 promoter adopts a unique broken-strand G4, whereas truncation of this sequence generates a vacancy G4 (vG4) that can be filled-in by external guanine analogs or metabolites and further stabilized by small molecules, suggesting a potential regulatory mechanism and opportunity for selective drug targeting. However, the relationship between broken-strand G4s and vG4s remains unclear. Here, we demonstrate that the PDGFR-\u03b2 promoter sequence forms a dynamic equilibrium between two broken-strand G4 conformations that interconvert on the millisecond timescale, with vG4 serving as an intermediate. We determined the high-resolution NMR structures of these interconverting G4s, which share a conserved vG4 core but differ in their intramolecular guanine \u201cfill-in.\u201d Both conformations feature a stabilizing G\u2013G capping base pair unique to the PDGFR-\u03b2 promoter. These findings elucidate the structural details of broken-strand PDGFR-\u03b2 promoter G4s and the mechanism of vG4 formation, providing critical insights for selective drug targeting and establishing a framework for rational design of small molecules to modulate PDGFR-\u03b2 transcription.<\/jats:p>","DOI":"10.1093\/nar\/gkag843","type":"journal-article","created":{"date-parts":[[2026,9,4]],"date-time":"2026-09-04T08:41:17Z","timestamp":1788511277000},"source":"Crossref","is-referenced-by-count":0,"title":["Structures and dynamics of the major G-quadruplex in the human PDGFR-\u03b2 gene promoter: insights into vacancy G-quadruplex formation"],"prefix":"10.1093","volume":"54","author":[{"given":"Yichen","family":"Han","sequence":"first","affiliation":[{"name":"Borch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University , West Lafayette, IN 47906 ,","place":["United 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