K
Kathryn L. Chapman
Researcher at Imperial College London
Publications - 8
Citations - 298
Kathryn L. Chapman is an academic researcher from Imperial College London. The author has contributed to research in topics: Pharmacophore & Virtual screening. The author has an hindex of 5, co-authored 8 publications receiving 223 citations. Previous affiliations of Kathryn L. Chapman include Francis Crick Institute.
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Journal ArticleDOI
Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases.
TL;DR: It is concluded that chaetocin, or related natural products, are not fit for application as selective chemical probes of HKMT function, and the disulfide bridge of the ETP unit is central to chaetOCin’s HKMT inhibitory activity by a nonspecific mechanism.
Journal ArticleDOI
MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo
Lorna R. Fiedler,Kathryn L. Chapman,Min Xie,Evie Maifoshie,Micaela Jenkins,Pelin Arabacilar Golforoush,Mohamed Bellahcene,Michela Noseda,Dörte Faust,Ashley Jarvis,Gary Newton,Marta Abreu Paiva,Mutsuo Harada,Daniel J. Stuckey,Weihua Song,Josef Habib,Priyanka Narasimhan,Rehan Aqil,Devika Sanmugalingam,Robert Yan,Lorenzo Pavanello,Motoaki Sano,Sam C. Wang,Robert D. Sampson,Sunthar Kanayaganam,George E. Taffet,Lloyd H. Michael,Mark L. Entman,Tse-Hua Tan,Tse-Hua Tan,Sian E. Harding,Caroline M. R. Low,Catherine Tralau-Stewart,Trevor Perrior,Michael D. Schneider,Michael D. Schneider +35 more
TL;DR: A small-molecule inhibitor is devised, DMX-5804, that rescues cell survival, mitochondrial function, and calcium cycling in hiPSC-CMs and implicates MAP4K4 as a well-posed target toward suppressing human cardiac cell death and highlights the utility of hiPSCs in drug discovery to enhance cardiomyocyte survival.
Journal ArticleDOI
The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model.
Paolo Di Fruscia,Emmanouil Zacharioudakis,Chang Liu,Sébastien Moniot,Sasiwan Laohasinnarong,Mattaka Khongkow,Ian F. Harrison,Konstantina Koltsida,Christopher R. Reynolds,Karin Schmidtkunz,Manfred Jung,Kathryn L. Chapman,Clemens Steegborn,David T. Dexter,Michael J.E. Sternberg,Eric Lam,Matthew J. Fuchter +16 more
TL;DR: In concordance with the recent reports that suggest SIRT2 inhibition is a potential strategy for the treatment of Parkinson’s disease, compound ICL‐SIRT078 has a significant neuroprotective effect in a lactacystin‐induced model of Parkinsonian neuronal cell death in the N27 cell line.
Journal ArticleDOI
On the histone lysine methyltransferase activity of fungal metabolite chaetocin.
Fanny L. Cherblanc,Kathryn L. Chapman,Jim Reid,Aaron J. Borg,Sandeep Sundriyal,Laura Alcazar-Fuoli,Elaine Bignell,Marina Demetriades,Christopher J. Schofield,Peter A. DiMaggio,Robert S. Brown,Matthew J. Fuchter +11 more
TL;DR: It is revealed that only the structurally unique ETP core is required for inhibition, and such inhibition is time-dependent and irreversible (in the absence of DTT), ultimately resulting in protein denaturation.
Journal ArticleDOI
Repurposed floxacins targeting RSK4 prevent chemoresistance and metastasis in lung and bladder cancer.
Stelios Chrysostomou,Rajat Roy,Filippo Prischi,Filippo Prischi,Lucksamon Thamlikitkul,Lucksamon Thamlikitkul,Kathryn L. Chapman,Uwais Mufti,Robert L. Peach,Laifeng Ding,David C. Hancock,Christopher I. Moore,Miriam Molina-Arcas,Francesco Mauri,David J. Pinato,Joel Abrahams,Silvia Ottaviani,Leandro Castellano,Georgios Giamas,Jennifer Pascoe,Devmini Moonamale,Sarah Pirrie,Claire Gaunt,Lucinda Billingham,Neil Steven,Michael Cullen,David Hrouda,Mathias Winkler,John Post,Philip Cohen,Seth J. Salpeter,Vered Bar,Adi Zundelevich,Shay Golan,Dan Leibovici,Romain Lara,Romain Lara,David R. Klug,Sophia N. Yaliraki,Mauricio Barahona,Yulan Wang,Julian Downward,J. Mark Skehel,Maruf M.U. Ali,Michael J. Seckl,Olivier E. Pardo +45 more
TL;DR: In this article, the authors identified RSK4 as a promoter of drug resistance and metastasis in lung and bladder cancer cells, and they suggested that inhibition of this kinase may represent an effective therapeutic strategy.