Synthesis and Structure–Activity Relationship Studies of Benzo[ b ][1,4]oxazin‐3(4 H )‐one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X

Autor: Michiel Vanmeert, Hannu Myllykallio, Rania Abu El‐Asrar, Jiahong Li, Eveline Lescrinier, Anastasia Parchina, Lia Margamuljana, Hubert F. Becker, Shrinivas Dumbre, Jakub Modranka, Hoai Nguyen, Roeland Vanhoutte, Mayla Salman, Jef Rozenski, Steven De Jonghe, Piet André Maurits Maria Herdewijn

Publikováno v: ChemMedChem
ChemMedChem, Wiley-VCH Verlag, 2019, 14 (6), pp.645-662. ⟨10.1002/cmdc.201800739⟩

Since the discovery of a flavin‐dependent thymidylate synthase (ThyX or FDTS) that is absent in humans but crucial for DNA biosynthesis in a diverse group of pathogens, the enzyme has been pursued for the development of new antibacterial agents aga

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bad860f52246e3df6dbc18d33e50352
https://doi.org/10.1002/cmdc.201800739

Highly stable hexitol based XNA aptamers targeting the vascular endothelial growth factor

Autor: Elena Eremeeva, Dominique Schols, Elisabetta Groaz, Lia Margamuljana, Antonios Fikatas, Piet Herdewijn, Mikhail Abramov

Publikováno v: Nucleic Acids Research

Biomedical applications of nucleic acid aptamers are limited by their rapid degradation in biological fluids and generally demand tedious post-selection modifications that might compromise binding. One possible solution to warrant biostability is to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4732eed5ed690be0b7b4e3653e53b6df
http://hdl.handle.net/11577/3369256

Discovery of a new Mycobacterium tuberculosis thymidylate synthase X inhibitor with a unique inhibition profile

Autor: Piet Herdewijn, Hugo Klaassen, Steven De Jonghe, Patrick Chaltin, Arnaud Marchand, Hannu Myllykallio, Eveline Lescrinier, Marnik Nijs, Lia Margamuljana, Rania Abou El Asrar, Hubert F. Becker

Publikováno v: Biochemical Pharmacology
Biochemical Pharmacology, 2017, 135, pp.69-78. ⟨10.1016/j.bcp.2017.03.017⟩
Biochemical Pharmacology, Elsevier, 2017, 135, pp.69-78. ⟨10.1016/j.bcp.2017.03.017⟩

Tuberculosis (TB), mainly caused by Mycobacterium tuberculosis (Mtb), is an infection that is responsible for roughly 1.5 million deaths per year. The situation is further complicated by the wide-spread resistance to the existing first- and second-li

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60ab62fe7757dd83ab6ea98b2785d7f9
https://polytechnique.hal.science/hal-01613159

Glypican-3–mediated inhibition of CD26 by TFPI: a novel mechanism in hematopoietic stem cell homing and maintenance

Autor: Sarah Schouteden, Shannon Buckley, Lia Margamuljana, Satish Khurana, Chacko Joseph, Catherine M. Verfaillie

Publikováno v: Blood. 121:2587-2595

Directional migration determines hematopoietic stem/progenitor cell (HSPC) homing, which depends upon the interaction between the chemokine CXCL12 and its receptor CXCR4. CD26 is a widely expressed membrane-bound ectopeptidase that cleaves CXCL12 the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aec53391f8a9ec559627583061dbccad
https://doi.org/10.1182/blood-2012-09-456715

Syntheses of 5'-Nucleoside Monophosphate Derivatives with Unique Aminal, Hemiaminal, and Hemithioaminal Functionalities: A New Class of 5'-Peptidyl Nucleotides

Autor: Piet Herdewijn, Elisabetta Groaz, Lia Margamuljana, Swarup De

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany). 22(24)

A number of synthetically useful transformations have been developed to generate novel 5'-peptidyl nucleoside monophosphate analogues that incorporate sensitive phosphoaminal, -hemiaminal or -hemithioaminal functionalities. The strategies adopted ent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b20f6d6b89b8521aa1de08ed0abc818
https://pubmed.ncbi.nlm.nih.gov/27136602