Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
27 10 2022
Historique:
pubmed: 7 10 2022
medline: 29 10 2022
entrez: 6 10 2022
Statut: ppublish

Résumé

Human DNA polymerase theta (Polθ), which is essential for microhomology-mediated DNA double strand break repair, has been proposed as an attractive target for the treatment of BRCA deficient and other DNA repair pathway defective cancers. As previously reported, we recently identified the first selective small molecule Polθ in vitro probe,

Identifiants

pubmed: 36200480
doi: 10.1021/acs.jmedchem.2c01142
doi:

Substances chimiques

Ligands 0
Poly(ADP-ribose) Polymerase Inhibitors 0
DNA 9007-49-2

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

13879-13891

Commentaires et corrections

Type : ErratumIn

Auteurs

Martin L Stockley (ML)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Amanda Ferdinand (A)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Giovanni Benedetti (G)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Peter Blencowe (P)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Susan M Boyd (SM)

CompChem Solutions Ltd, St John's Innovation Centre, Cowley Rd, CambridgeCB4 0WS, U. K.

Mat Calder (M)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Mark D Charles (MD)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Lucy V Edwardes (LV)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Tennyson Ekwuru (T)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Harry Finch (H)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Alessandro Galbiati (A)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Lerin Geo (L)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Diego Grande (D)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Vera Grinkevich (V)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Nicholas D Holliday (ND)

Excellerate Bioscience Ltd., BioCity, Pennyfoot Street, NottinghamNG1 1GF, U. K.

Wojciech W Krajewski (WW)

Cancer Research Horizons Therapeutic Innovation, The Francis Crick Institute, 1 Midland Road, LondonNW1 1AT, U. K.

Ellen MacDonald (E)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Jayesh B Majithiya (JB)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Hollie McCarron (H)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Claire L McWhirter (CL)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Viral Patel (V)

Excellerate Bioscience Ltd., BioCity, Pennyfoot Street, NottinghamNG1 1GF, U. K.

Chris Pedder (C)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Eeson Rajendra (E)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Marco Ranzani (M)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Laurent J M Rigoreau (LJM)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Helen M R Robinson (HMR)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Theresia Schaedler (T)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Julija Sirina (J)

Excellerate Bioscience Ltd., BioCity, Pennyfoot Street, NottinghamNG1 1GF, U. K.

Graeme C M Smith (GCM)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

Martin E Swarbrick (ME)

Cancer Research Horizons Therapeutic Innovation, Jonas Webb Building, Babraham Research Campus, CambridgeCB22 3AT, U. K.

Andrew P Turnbull (AP)

Cancer Research Horizons Therapeutic Innovation, The Francis Crick Institute, 1 Midland Road, LondonNW1 1AT, U. K.

Simon Willis (S)

Cancer Research Horizons Therapeutic Innovation, The Francis Crick Institute, 1 Midland Road, LondonNW1 1AT, U. K.

Robert A Heald (RA)

Artios Pharma Ltd., B940, Babraham Research Campus, CambridgeCB22 3FH, U. K.

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Classifications MeSH