K
Krystyna J. Dillon
Publications - 6
Citations - 6436
Krystyna J. Dillon is an academic researcher. The author has contributed to research in topics: Poly ADP ribose polymerase & Enzyme inhibitor. The author has an hindex of 6, co-authored 6 publications receiving 5670 citations.
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Journal ArticleDOI
Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy
Hannah Farmer,Nuala McCabe,Christopher J. Lord,Andrew Tutt,Andrew Tutt,Damian A. Johnson,Tobias B. Richardson,Manuela Santarosa,Krystyna J. Dillon,Ian Hickson,Charlotte Knights,Niall M. B. Martin,Stephen P. Jackson,Graeme C. M. Smith,Alan Ashworth +14 more
TL;DR: BRCA1 or BRCA2 dysfunction unexpectedly and profoundly sensitizes cells to the inhibition of PARP enzymatic activity, resulting in chromosomal instability, cell cycle arrest and subsequent apoptosis, illustrating how different pathways cooperate to repair damage.
Journal ArticleDOI
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Keith Allan Menear,Claire Adcock,Robert Boulter,Xiao-Ling Fan Cockcroft,Louise Copsey,Aaron Cranston,Krystyna J. Dillon,Jan Drzewiecki,Sheila Garman,Sylvie Gomez,Hashim Javaid,Frank Kerrigan,Charlotte Knights,Alan Lau,Vincent Junior Ming-Lai Loh,Ian Timothy William Matthews,Stephen Moore,Mark J. O'Connor,Graeme C. M. Smith,Niall M. B. Martin +19 more
TL;DR: A novel series of substituted 4-benzyl-2 H-phthalazin-1-ones that possess high inhibitory enzyme and cellular potency for both PARP-1 andPARP-2 are disclosed and shows standalone activity against BRCA1-deficient breast cancer cell lines.
Journal ArticleDOI
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Vincent M. Loh,Xiao-Ling Fan Cockcroft,Krystyna J. Dillon,Lesley Dixon,Jan Drzewiecki,Penny Jane Eversley,Sylvie Gomez,Janet Hoare,Frank Kerrigan,Ian Timothy William Matthews,Keith Allan Menear,Niall M. B. Martin,Roger F. Newton,Jane Paul,Graeme C. M. Smith,Julia Vile,Alan Whittle +16 more
TL;DR: A novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity as PARP-1 inhibitors and promising metabolic stability in vitro are presented.
Journal ArticleDOI
Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Xiao-Ling Fan Cockcroft,Krystyna J. Dillon,Lesley Dixon,Jan Drzewiecki,Frank Kerrigan,Vincent M. Loh,Niall M. B. Martin,Keith Allan Menear,Graeme C. M. Smith +8 more
TL;DR: A novel series of meta-substituted 4-benzyl-2H-phthalazin-1-one PARP-1 inhibitors which retain low nM cellular activity and show good stability in vivo and efficacy in cell based models are presented.
Journal ArticleDOI
A FlashPlate assay for the identification of PARP-1 inhibitors.
TL;DR: The developed assay is a robust and reproducible method of screening for PARP-1 inhibitors that is low maintenance and cost-effective and can easily be automated.