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PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti‐tumour activity
BACKGROUND AND PURPOSE PM01183 is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumours. In this study we haveExpand
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Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition
Significance Safer and more effective oral drugs are urgently required to treat visceral leishmaniasis (VL), a neglected parasitic disease that kills 20,000–40,000 people each year in parts of Asia,Expand
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Temperature-induced melting of double-stranded DNA in the absence and presence of covalently bonded antitumour drugs: insight from molecular dynamics simulations
The difference in melting temperature of a double-stranded (ds) DNA molecule in the absence and presence of bound ligands can provide experimental information about the stabilization brought about byExpand
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XPF-dependent DNA breaks and RNA polymerase II arrest induced by antitumor DNA interstrand crosslinking-mimetic alkaloids.
Trabectedin and Zalypsis are two potent anticancer tetrahydroisoquinoline alkaloids that can form a covalent bond with the amino group of a guanine in selected triplets of DNA duplexes and eventuallyExpand
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Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis
Significance Malaria and cryptosporidiosis are major burdens to both global health and economic development in many countries. Malaria caused >400,000 deaths in 2017, and cryptosporidiosis isExpand
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Impact of Ser17 Phosphorylation on the Conformational Dynamics of the Oncoprotein MDM2.
MDM2 is an important oncoprotein that downregulates the activity of the tumor suppressor protein p53 via binding of its N-terminal domain to the p53 transactivation domain. The first 24 residues ofExpand
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A structural study of the complex between neuroepithelial cell transforming gene 1 (Net1) and RhoA reveals a potential anticancer drug hot spot
The GTPase RhoA is a major player in many different regulatory pathways. RhoA catalyzes GTP hydrolysis, and its catalysis is accelerated when RhoA forms heterodimers with proteins of the guanineExpand
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Molecular basis of RNA guanine-7 methyltransferase (RNMT) activation by RAM
Maturation and translation of mRNA in eukaryotes requires the addition of the 7-methylguanosine cap. In vertebrates, the cap methyltransferase, RNA guanine-7 methyltransferase (RNMT), has anExpand
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Rationale for the opposite stereochemistry of the major monoadducts and interstrand crosslinks formed by mitomycin C and its decarbamoylated analogue at CpG steps in DNA and the effect of cytosine
Mitomycin C (MMC) is a potent antitumour agent that forms a covalent bond with the 2-amino group of selected guanines in the minor groove of double-stranded DNA following intracellular reduction ofExpand
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Mechanistic Insight into the Catalytic Activity of ββα‐Metallonucleases from Computer Simulations: Vibrio vulnificus Periplasmic Nuclease as a Test Case
Using information from wild‐type and mutant Vibrio vulnificus nuclease (Vvn) and I‐PpoI homing endonuclease co‐crystallized with different oligodeoxynucleotides, we have built the complex of Vvn withExpand
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