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However, in contrast to well-established drug targets such as kinases and G protein-coupled receptors, RBPs remain largely underexploited owing to their intrinsic structural heterogeneity, dynamic RNA interactions, and paucity of canonical ligand-binding pockets. In this review, we synthesize current knowledge on the roles of RBPs in disease, outline recent advances in the design of small-molecule modulators, and highlight innovative applications of high-throughput screening and chemical biology approaches for target identification and validation. We further discuss emerging concepts and challenges in translating RBP modulators into therapeutics, providing a forward-looking perspective on how these efforts may reshape small-molecule drug discovery in this evolving field.","is_dataset_classified":null,"base_score":0.0,"endowment":0.0,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"41909745","pmcid":"PMC13031079","openalex_id":null,"authors":[],"funders":[{"funder_name":"Fundamental Research Funds for the Central Universities","grant_id":"2632025TD01","title":null},{"funder_name":"National Natural Science Foundation of China","grant_id":"82574253","title":null},{"funder_name":"Natural Science Foundation of Jiangsu Province","grant_id":"BK20231483","title":null}],"total_grants":3,"fwci":null,"citation_percentile":null,"influential_citations":0,"citation_trend":[],"oa_status":null,"license":"http://creativecommons.org/licenses/by-nc-nd/4.0/","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S2211383525008172?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S2211383525008172?httpAccept=text/plain","host_type":"publisher"},{"url":"https://europepmc.org/articles/PMC13031079","host_type":"Europe_PMC"},{"url":"https://europepmc.org/articles/PMC13031079?pdf=render","host_type":"Europe_PMC"}],"fields_of_study":[],"mesh_terms":[],"keywords":["Disease","High-throughput screening","drug discovery","Target Identification","Rna Binding Proteins","Post-transcriptional Gene Expression","Small-molecule Modulators","Chemical Biology Approaches"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-08T00:40:46.969285Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}