H
H. Rachel Lagiakos
Researcher at Monash University
Publications - 4
Citations - 168
H. Rachel Lagiakos is an academic researcher from Monash University. The author has contributed to research in topics: Chemistry & Medicine. The author has an hindex of 2, co-authored 2 publications receiving 101 citations.
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Journal ArticleDOI
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth
Jonathan B. Baell,Jonathan B. Baell,David J. Leaver,S.J. Hermans,Gemma L. Kelly,Gemma L. Kelly,Margs S. Brennan,Margs S. Brennan,Natalie L. Downer,Nghi H. Nguyen,Johannes Wichmann,Johannes Wichmann,Helen M. McRae,Helen M. McRae,Yuquing Yang,Yuquing Yang,Benjamin Cleary,H. Rachel Lagiakos,Stephen Mieruszynski,Stephen Mieruszynski,Guido Pacini,Hannah K. Vanyai,Hannah K. Vanyai,Maria I. Bergamasco,Maria I. Bergamasco,Rose E. May,Bethany K. Davey,Kimberly J. Morgan,Kimberly J. Morgan,Andrew J. Sealey,Andrew J. Sealey,Beinan Wang,Beinan Wang,Beinan Wang,Natasha Zamudio,Natasha Zamudio,Stephen Wilcox,Stephen Wilcox,Alexandra L. Garnham,Alexandra L. Garnham,Bilal N. Sheikh,Bilal N. Sheikh,Brandon J. Aubrey,Brandon J. Aubrey,Karen Doggett,Karen Doggett,M.C. Chung,Melanie de Silva,John D. Bentley,Pat Pilling,Meghan Hattarki,Olan Dolezal,Matthew L. Dennis,Hendrik Falk,Hendrik Falk,Bin Ren,Susan A. Charman,Karen L. White,Jai Rautela,Jai Rautela,Andrea Newbold,Edwin D. Hawkins,Edwin D. Hawkins,Ricky W. Johnstone,Nicholas D. Huntington,Nicholas D. Huntington,Thomas S. Peat,Joan K. Heath,Joan K. Heath,Andreas Strasser,Andreas Strasser,Michael W. Parker,Michael W. Parker,Gordon K. Smyth,Gordon K. Smyth,Ian P. Street,Ian P. Street,Brendon J. Monahan,Brendon J. Monahan,Anne K. Voss,Anne K. Voss,Tim Thomas,Tim Thomas +82 more
TL;DR: Biochemical and structural studies demonstrate that these compounds are reversible competitors of acetyl coenzyme A and inhibit MYST-catalysed histone acetylation, induce cell cycle exit and cellular senescence without causing DNA damage, and arrest lymphoma progression in mouse models.
Journal ArticleDOI
In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas
Samantha A Ottavi,Sarah M. Scarry,John W. Mosior,Yan-Lan Ling,Julia Roberts,Amrita Saxena H B Singh,David T Zhang,Laurent Goullieux,Christine Roubert,Eric Bacqué,H. Rachel Lagiakos,Jeremie Vendome,Francesca Maria Moraca,Kenli Li,Andrew J. Perkowski,Remya Ramesh,Matthew M. Bowler,William Woodbridge Tracy,Victoria A. Feher,James C. Sacchettini,Ben Gold,Carl Nathan,Jeffrey Aubé +22 more
TL;DR: Studying the structure–activity relationships of a recently disclosed inhibitor, amidinourea (AU) 8918, showed that the AU moiety in AU 8918 is largely optimized and that potency enhancements are obtained in analogues containing a para-substituted aromatic ring.
Journal ArticleDOI
Discovery of acylsulfonohydrazide-derived inhibitors of the lysine acetyltransferase, kat6a, as potent senescence-inducing anti-cancer agents
Daniel L. Priebbenow,David J. Leaver,Nghi Nguyen,Benjamin Cleary,H. Rachel Lagiakos,Julie Sanchez,Julie Sanchez,Lian Xue,Fei Huang,Yuxin Sun,Prashant Mujumdar,Ramesh Mudududdla,Swapna Varghese,Silvia Teguh,Susan A. Charman,Karen L. White,David M. Shackleford,Kasiram Katneni,Matthew E. Cuellar,Jessica M. Strasser,Jayme L. Dahlin,Michael A. Walters,Ian P. Street,Ian P. Street,Brendon J. Monahan,Brendon J. Monahan,Kate E. Jarman,Kate E. Jarman,Helene Jousset Sabroux,Helene Jousset Sabroux,Hendrik Falk,Hendrik Falk,M.C. Chung,S.J. Hermans,Natalie L. Downer,Michael W. Parker,Anne K. Voss,Anne K. Voss,Tim Thomas,Tim Thomas,Jonathan B. Baell,Jonathan B. Baell +41 more
TL;DR: Aryl acylsulfonohydrazide with an IC50 of 1.0 μM was used as a template for a high-throughput screen designed to discover new inhibitors of histone acetyltransferase KAT6A as mentioned in this paper.
Journal ArticleDOI
A Computational Physics-based Approach to Predict Unbound Brain-to-Plasma Partition Coefficient, Kp,uu
Morgan Lawrenz,Mats Svensson,Mitsunori Kato,Karen H. Dingley,Jackson Chief Elk,Zhe Nie,Yefen Zou,H. Rachel Lagiakos,Hideyuki Igawa,Eric Therrien +9 more
TL;DR: In this article , a physics-based computational approach, a quantum mechanics (QM)-based energy of solvation (E-sol), was described to predict the optimal brain penetration of small-molecule central nervous system drugs.