dc.contributor.author | Bery, N | |
dc.contributor.author | Bataille, CJR | |
dc.contributor.author | Russell, A | |
dc.contributor.author | Hayes, A | |
dc.contributor.author | Raynaud, F | |
dc.contributor.author | Milhas, S | |
dc.contributor.author | Anand, S | |
dc.contributor.author | Tulmin, H | |
dc.contributor.author | Miller, A | |
dc.contributor.author | Rabbitts, TH | |
dc.date.accessioned | 2021-05-19T14:00:06Z | |
dc.date.available | 2021-05-19T14:00:06Z | |
dc.date.issued | 2021-04-01 | |
dc.identifier.citation | Science advances, 2021, 7 (15) | |
dc.identifier.issn | 2375-2548 | |
dc.identifier.uri | https://repository.icr.ac.uk/handle/internal/4562 | |
dc.identifier.eissn | 2375-2548 | |
dc.identifier.doi | 10.1126/sciadv.abg1950 | |
dc.description.abstract | Intracellular antibodies are tools that can be used directly for target validation by interfering with properties like protein-protein interactions. An alternative use of intracellular antibodies in drug discovery is developing small-molecule surrogates using antibody-derived (Abd) technology. We previously used this strategy with an in vitro competitive surface plasmon resonance method that relied on high-affinity antibody fragments to obtain RAS-binding compounds. We now describe a novel implementation of the Abd method with a cell-based intracellular antibody-guided screening method that we have applied to the chromosomal translocation protein LMO2. We have identified a chemical series of anti-LMO2 Abd compounds that bind at the same LMO2 location as the inhibitory anti-LMO2 intracellular antibody combining site. Intracellular antibodies could therefore be used in cell-based screens to identify chemical surrogates of their binding sites and potentially be applied to any challenging proteins, such as transcription factors that have been considered undruggable. | |
dc.format | Print-Electronic | |
dc.language | eng | |
dc.language.iso | eng | |
dc.publisher | AMER ASSOC ADVANCEMENT SCIENCE | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0 | |
dc.title | A cell-based screening method using an intracellular antibody for discovering small molecules targeting the translocation protein LMO2. | |
dc.type | Journal Article | |
dcterms.dateAccepted | 2021-02-19 | |
rioxxterms.version | VoR | |
rioxxterms.versionofrecord | 10.1126/sciadv.abg1950 | |
rioxxterms.licenseref.uri | https://creativecommons.org/licenses/by/4.0 | |
rioxxterms.licenseref.startdate | 2021-04-09 | |
rioxxterms.type | Journal Article/Review | |
dc.relation.isPartOf | Science advances | |
pubs.issue | 15 | |
pubs.notes | Not known | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Chromosomal Translocations and Intracellular Antibody Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Chromosomal Translocations and Intracellular Antibody Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
pubs.publication-status | Published | |
pubs.volume | 7 | |
pubs.embargo.terms | Not known | |
icr.researchteam | Chromosomal Translocations and Intracellular Antibody Therapeutics | |
icr.researchteam | Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
icr.researchteam | Chromosomal Translocations and Intracellular Antibody Therapeutics | |
icr.researchteam | Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
dc.contributor.icrauthor | Raynaud, Florence | |
dc.contributor.icrauthor | Rabbitts, Terence | |