{"doi":"10.1002/anie.202204567","title":"A pH‐Driven Small‐Molecule Nanotransformer Hijacks Lysosomes and Overcomes Autophagy‐Induced Resistance in Cancer","abstract":"Smart conversion of supramolecular structures in vivo is an attractive strategy in cancer nanomedicine, which is usually achieved via specific peptide sequences. Here we developed a lysosomal targeting small-molecule conjugate, PBC, which self-assembles into nanoparticles at physiological pH and smartly converts to nanofibrils in lysosomes of tumor cells. Such a transformation mechanically leads to lysosomal dysfunction, autophagy inhibition, and unusual cytoplasmic vacuolation, thus granting PBC a unique anticancer activity as a monotherapy. Importantly, the photo-activated PBC elicits significant phototoxicity to lysosomes and shows enormous advantages in overcoming autophagy-caused treatment resistance frequently occurring in conventional phototherapy. This improved phototherapy achieves a complete cure of oral cancer xenografts upon limited administration. Our work provides a new paradigm for the construction of nonpeptide nanotransformers with biomedical activities.","journal":"Angewandte Chemie International Edition","year":2022,"id":248541,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":30,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9451,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2022-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":315455,"name":"Kai Lin","orcid":"0000-0003-4445-4939","position":1,"is_corresponding":false},{"id":316273,"name":"Menghuan Tang","orcid":null,"position":2,"is_corresponding":false},{"id":315458,"name":"Mythili Ramachandran","orcid":"0000-0001-8529-1545","position":3,"is_corresponding":false},{"id":888650,"name":"Reng Qiu","orcid":null,"position":4,"is_corresponding":false},{"id":887988,"name":"Jin Li","orcid":"0000-0002-4672-6806","position":5,"is_corresponding":false},{"id":324722,"name":"Lucas N. Solano","orcid":null,"position":6,"is_corresponding":false},{"id":832175,"name":"Yanyu Huang","orcid":"0000-0002-4134-944X","position":7,"is_corresponding":false},{"id":323397,"name":"Cristabelle De Souza","orcid":"0000-0001-9734-9492","position":8,"is_corresponding":false},{"id":888651,"name":"Sara Abou‐Adas","orcid":null,"position":9,"is_corresponding":false},{"id":888652,"name":"Bai Xiang","orcid":null,"position":10,"is_corresponding":false},{"id":315460,"name":"Lanwei Zhang","orcid":"0000-0003-3459-2975","position":11,"is_corresponding":false},{"id":139032,"name":"Minyong Li","orcid":"0000-0003-3276-4921","position":12,"is_corresponding":false},{"id":237446,"name":"Yuanpei Li","orcid":"0000-0002-4015-646X","position":13,"is_corresponding":false},{"id":315456,"name":"Zhao Ma","orcid":"0000-0002-8000-5324","position":0,"is_corresponding":true}],"reference_count":42,"raw_metadata":null,"created_at":"2026-07-19T00:24:14.794521Z","pmid":"35791769","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":[]}