{"database":"GEO","file_versions":[{"headers":{"Content-Type":["application/json"]},"body":{"files":{"Other":["ftp://ftp.ncbi.nlm.nih.gov/geo/series/GSE279nnn/GSE279011/"]},"type":"primary"},"statusCode":"OK","statusCodeValue":200}],"scores":null,"additional":{"omics_type":["Transcriptomics"],"species":["Homo sapiens"],"gds_type":["Expression profiling by high throughput sequencing"],"full_dataset_link":["https://www.ncbi.nlm.nih.gov/geo/query/acc.cgi?acc=GSE279011"],"repository":["GEO"],"entry_type":["GSE"],"additional_accession":[]},"is_claimable":false,"name":"Targeted Delivery of Selective BET Inhibitors","description":"The circumvention of tissue-specific toxicity while improving selectivity remains a significant challenge in cancer therapy. Antibody-assisted delivery of chemotypes aims to address this, leading to several approved therapies; however, non-specific payload release and poor solid tumour penetration necessitate alternative approaches. To this end, we engineered a ligand-targeted drug conjugate, exploiting the over-expression of the prostate-specific membrane antigen (PSMA) in prostate cancer to selectively deliver and conditionally release RT53, a highly specific epigenetic inhibitor of the bromo and extra-terminal (BET) proteins. RT53 phenocopies the effects of the well characterized IBET pan-BET inhibitor in vitro and in vivo, arresting cellular growth and downregulating solute carriers, while exhibiting antitumor activity in subcutaneous ectopic prostate cancer mouse models. Importantly, PSMA-targeted delivery and conditional release of RT53 achieves superior efficacy in vivo ameliorating on-target, off-tissue toxicity, and establishing proof-of-concept for the targeted delivery of small molecule epigenetic chemotherapeutics.","dates":{"publication":"2026/08/27"},"accession":"GSE279011","cross_references":{"GSM":["GSM8559619","GSM8559626","GSM8559637","GSM8559627","GSM8559638","GSM8559639","GSM8559628","GSM8559629","GSM8559633","GSM8559622","GSM8559634","GSM8559623","GSM8559624","GSM8559635","GSM8559636","GSM8559625","GSM8559640","GSM8559630","GSM8559641","GSM8559642","GSM8559631","GSM8559620","GSM8559621","GSM8559632"],"GPL":["18573"],"GSE":["279011"],"taxon":["Homo sapiens"]}}