{"doi":"10.1002/cbic.202000532","title":"Chemical Translational Biology: Redefining Druggability of Protein‐Protein Interactions","abstract":"<jats:title>Abstract</jats:title><jats:p>Chemical biologists use chemical tools to answer biological questions. The translational application of these principles has led to an explosion in the discovery and druggability of new protein targets, including protein‐protein interactions (PPIs). <jats:italic>Proteins</jats:italic> tend to interact with other macromolecules using relatively large and featureless binding surfaces, which has hampered traditional drug discovery efforts, particularly for interactions with weaker affinity. In this article, I discuss several emerging strategies for targeting PPIs, including computational and structural methods and novel screening approaches. In particular, I focus on hijacking intrinsic protein allosteric pathways for the discovery and design of small‐molecule and peptide ligands.</jats:p>","journal":"ChemBioChem","year":2021,"id":667053,"datarank":0.20794415416798362,"base_score":1.3862943611198906,"endowment":1.3862943611198906,"self_citation_contribution":0.20794415416798362,"citation_network_contribution":0.0,"self_endowment_contribution":0.20794415416798362,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":3,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1741994,"name":"Laura C. Cesa","orcid":"0000-0002-8367-3790","position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Chemical Translational Biology: Redefining Druggability of Protein‐Protein Interactions","abstract":"<jats:title>Abstract</jats:title><jats:p>Chemical biologists use chemical tools to answer biological questions. The translational application of these principles has led to an explosion in the discovery and druggability of new protein targets, including protein‐protein interactions (PPIs). <jats:italic>Proteins</jats:italic> tend to interact with other macromolecules using relatively large and featureless binding surfaces, which has hampered traditional drug discovery efforts, particularly for interactions with weaker affinity. In this article, I discuss several emerging strategies for targeting PPIs, including computational and structural methods and novel screening approaches. In particular, I focus on hijacking intrinsic protein allosteric pathways for the discovery and design of small‐molecule and peptide ligands.</jats:p>","is_dataset_classified":null,"base_score":1.3862943611198906,"endowment":1.3862943611198906,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"33205588","pmcid":null,"openalex_id":"https://openalex.org/W3099865896","authors":[],"funders":[{"funder_name":"Lundbeck Foundation Postdoctoral Fellowship","grant_id":"R322-2019-2349","title":null}],"total_grants":1,"fwci":0.2536,"citation_percentile":0.6266518,"influential_citations":0,"citation_trend":[{"year":2021,"count":1},{"year":2023,"count":1},{"year":2026,"count":1}],"oa_status":"closed","license":"http://onlinelibrary.wiley.com/termsAndConditions#vor","oa_locations":[{"url":"https://onlinelibrary.wiley.com/doi/pdf/10.1002/cbic.202000532","host_type":"publisher"},{"url":"https://onlinelibrary.wiley.com/doi/full-xml/10.1002/cbic.202000532","host_type":"publisher"},{"url":"https://chemistry-europe.onlinelibrary.wiley.com/doi/pdf/10.1002/cbic.202000532","host_type":"publisher"},{"url":"https://doi.org/10.1002/cbic.202000532","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/33205588","host_type":"repository"},{"url":"https://researchprofiles.ku.dk/da/publications/dfed61d1-91d5-41a9-aeee-fdf01b30ad21","host_type":"repository"}],"fields_of_study":["Computational Drug Discovery Methods","Click Chemistry and Applications","Microbial Natural Products and Biosynthesis"],"mesh_terms":["Allosteric Regulation","Biphenyl Compounds","Ligands","Nitrophenols","Piperazines","Protein Binding","Proteins","Sulfonamides","Proto-Oncogene Proteins c-bcl-2","bcl-X Protein","Drug Discovery","Protein Interaction Maps"],"keywords":["Druggability","Drug discovery","Chemical biology","Computational biology","Allosteric regulation","Protein–protein interaction","Small molecule","Structural biology","Biology","Chemistry","Bioinformatics","Biochemistry","Enzyme","Allostery","protein-protein interactions"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-13T16:27:57.337698Z","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":[]}