[HTML][HTML] CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition

…, J Bowlan, N Chaudhary, J Desjardins, E Dietrich… - Nature, 2022 - nature.com
Amplification of the CCNE1 locus on chromosome 19q12 is prevalent in multiple tumour
types, particularly in high-grade serous ovarian cancer, uterine tumours and gastro-…

Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus

…, L Cegelski, D Stueber, M Singh, E Dietrich… - Journal of molecular …, 2008 - Elsevier
Solid-state NMR measurements performed on intact whole cells of Staphylococcus aureus
labeled selectively in vivo have established that des-N-methylleucyl oritavancin (which has …

Vancomycin and oritavancin have different modes of action in Enterococcus faecium

GJ Patti, SJ Kim, TY Yu, E Dietrich, KSE Tanaka… - Journal of molecular …, 2009 - Elsevier
The increasing frequency of Enterococcus faecium isolates with multidrug resistance is a
serious clinical problem given the severely limited number of therapeutic options available to …

Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis

…, KSE Tanaka, T Kang, E Dietrich… - Journal of medicinal …, 2008 - ACS Publications
Osteomyelitis is an infection located in bone and a notoriously difficult disease to manage,
requiring frequent and heavy doses of systemically administered antibiotics. Targeting …

Discovery of an orally bioavailable and selective PKMYT1 inhibitor, RP-6306

J Szychowski, R Papp, E Dietrich, B Liu… - Journal of medicinal …, 2022 - ACS Publications
PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for
the treatment of certain types of DNA damage response cancers due to its established …

Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis

KSE Tanaka, TJ Houghton, T Kang, E Dietrich… - Bioorganic & medicinal …, 2008 - Elsevier
Osteomyelitis is a difficult to treat bacterial infection of the bone. Delivering antibacterial
agents to the bone may overcome the difficulties in treating this illness by effectively …

A new class of small molecule RNA polymerase inhibitors with activity against rifampicin-resistant Staphylococcus aureus

…, S Ciblat, M Dehbi, D Delorme, E Dietrich… - Bioorganic & medicinal …, 2006 - Elsevier
The RNA polymerase holoenzyme is a proven target for antibacterial agents. A high-throughput
screening program based on this enzyme from Staphylococcus aureus had previously …

Locations of the Hydrophobic Side Chains of Lipoglycopeptides Bound to the Peptidoglycan of Staphylococcus aureus

SJ Kim, KSE Tanaka, E Dietrich, A Rafai Far… - Biochemistry, 2013 - ACS Publications
Glycopeptides whose aminosugars have been modified by attachment of hydrophobic side
chains are frequently active against vancomycin-resistant microorganisms. We have …

Efficient synthesis of enantiopure pyrrolizidinone amino acid

E Dietrich, WD Lubell - The Journal of Organic Chemistry, 2003 - ACS Publications
Enantiopure (3S,5R,8S)-3-[N-(Boc)amino]-1-azabicyclo[3.3.0]octan-2-one 8-carboxylic acid
(1) was synthesized in nine steps and 16% overall yield from aspartate β-aldehyde 7. …

Synthesis and in vitro evaluation of bisphosphonated glycopeptide prodrugs for the treatment of osteomyelitis

KSE Tanaka, E Dietrich, S Ciblat, C Métayer… - Bioorganic & Medicinal …, 2010 - Elsevier
As therapeutic agents of choice in the treatment of complicated infections, glycopeptide
antibiotics are often preferentially used in cases of osteomyelitis, an infection located in bone …