Cargando…

Structure-Based Design of Potent and Selective LeishmaniaN-Myristoyltransferase Inhibitors

[Image: see text] Inhibitors of LeishmaniaN-myristoyltransferase (NMT), a potential target for the treatment of leishmaniasis, obtained from a high-throughput screen, were resynthesized to validate activity. Crystal structures bound to Leishmania major NMT were obtained, and the active diastereoisom...

Descripción completa

Detalles Bibliográficos
Autores principales:	Hutton, Jennie A., Goncalves, Victor, Brannigan, James A., Paape, Daniel, Wright, Megan H., Waugh, Thomas M., Roberts, Shirley M., Bell, Andrew S., Wilkinson, Anthony J., Smith, Deborah F., Leatherbarrow, Robin J., Tate, Edward W.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2014
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4211304/ https://www.ncbi.nlm.nih.gov/pubmed/25238611 http://dx.doi.org/10.1021/jm5011397

Ejemplares similares

Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes
por: Bell, Andrew S., et al.
Publicado: (2020)

Diverse modes of binding in structures of Leishmania major N-myristoyltransferase with selective inhibitors
por: Brannigan, James A., et al.
Publicado: (2014)

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase
por: Rackham, Mark D., et al.
Publicado: (2015)

Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase
por: Goncalves, Victor, et al.
Publicado: (2016)

Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites
por: Olaleye, Tayo O., et al.
Publicado: (2014)

N-Myristoyltransferase from Leishmania donovani: Structural and Functional Characterisation of a Potential Drug Target for Visceral Leishmaniasis
por: Brannigan, James A., et al.
Publicado: (2010)

Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase
por: Yu, Zhiyong, et al.
Publicado: (2015)

Using a Non-Image-Based Medium-Throughput Assay for Screening Compounds Targeting N-myristoylation in Intracellular Leishmania Amastigotes
por: Paape, Daniel, et al.
Publicado: (2014)

Selective Inhibitors of Protozoan Protein N-myristoyltransferases as Starting Points for Tropical Disease Medicinal Chemistry Programs
por: Bell, Andrew S., et al.
Publicado: (2012)

Global Analysis of Protein N-Myristoylation and Exploration of N-Myristoyltransferase as a Drug Target in the Neglected Human Pathogen Leishmania donovani
por: Wright, Megan H., et al.
Publicado: (2015)

Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivaxN-Myristoyltransferase
por: Rackham, Mark D., et al.
Publicado: (2012)

Design and Synthesis of High Affinity Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferases Directed by Ligand Efficiency Dependent Lipophilicity (LELP)
por: Rackham, Mark D., et al.
Publicado: (2014)

Fragment-derived inhibitors of human N-myristoyltransferase block capsid assembly and replication of the common cold virus
por: Mousnier, Aurélie, et al.
Publicado: (2018)

Genetic validation of Leishmania genes essential for amastigote survival in vivo using N-myristoyltransferase as a model
por: Paape, Daniel, et al.
Publicado: (2020)

Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani
por: Corpas-Lopez, Victoriano, et al.
Publicado: (2018)

N-Myristoyltransferase inhibitors as new leads to treat sleeping sickness
por: Frearson, Julie A., et al.
Publicado: (2010)

Biochemical and genetic characterization of Trypanosoma cruzi N-myristoyltransferase
por: Roberts, Adam J., et al.
Publicado: (2014)

Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases
por: Kallemeijn, Wouter W., et al.
Publicado: (2019)

Identification of potent and selective N-myristoyltransferase inhibitors of Plasmodium vivax liver stage hypnozoites and schizonts
por: Rodríguez-Hernández, Diego, et al.
Publicado: (2023)

QSAR and Pharmacophore Modeling of Nitrogen Heterocycles as Potent Human N-Myristoyltransferase (Hs-NMT) Inhibitors
por: Zaki, Magdi E. A., et al.
Publicado: (2021)

Structure-Guided Identification of Resistance Breaking Antimalarial N‑Myristoyltransferase Inhibitors
por: Schlott, Anja C., et al.
Publicado: (2019)

Whole Proteome Profiling of N-Myristoyltransferase Activity and Inhibition Using Sortase A
por: Goya Grocin, Andrea, et al.
Publicado: (2019)

N-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells
por: Thinon, Emmanuelle, et al.
Publicado: (2016)

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors
por: Harrison, Justin R., et al.
Publicado: (2018)

The role of N-myristoyltransferase 1 in tumour development
por: Wang, Hong, et al.
Publicado: (2023)

N-Myristoyltransferase Is a Cell Wall Target in Aspergillus fumigatus
por: Fang, Wenxia, et al.
Publicado: (2015)

Wheat pathogen Zymoseptoria tritici N-myristoyltransferase inhibitors: on-target antifungal activity and an unusual metabolic defense mechanism
por: Fedoryshchak, Roman O., et al.
Publicado: (2020)

Identification of Potential Leishmania N-Myristoyltransferase Inhibitors from Withania somnifera (L.) Dunal: A Molecular Docking and Molecular Dynamics Investigation
por: Orabi, Mohamed A. A., et al.
Publicado: (2023)

QSAR Study of N-Myristoyltransferase Inhibitors of Antimalarial Agents
por: Santos-Garcia, Letícia, et al.
Publicado: (2018)

Global Profiling and Inhibition of Protein Lipidation in Vector and Host Stages of the Sleeping Sickness Parasite Trypanosoma brucei
por: Wright, Megan H., et al.
Publicado: (2016)

Myristoyl-CoA:protein N-myristoyltransferase depletion in trypanosomes causes avirulence and endocytic defects
por: Price, Helen P., et al.
Publicado: (2010)

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
por: Bayliss, Tracy, et al.
Publicado: (2017)

Inhibition of N‐myristoyltransferase1 affects dengue virus replication
por: Suwanmanee, San, et al.
Publicado: (2019)

Inhibitor Trapping in N-Myristoyltransferases as a Mechanism for Drug Potency
por: Spassov, Danislav S., et al.
Publicado: (2023)

N-myristoyltransferase: A potential novel diagnostic marker for colon cancer
por: Shrivastav, Anuraag, et al.
Publicado: (2007)

Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase
por: Robinson, David A., et al.
Publicado: (2015)

Novel Hits for N-Myristoyltransferase Inhibition Discovered by Docking-Based Screening
por: Spassov, Danislav S., et al.
Publicado: (2022)

N-myristoyltransferase deficiency impairs AMPK activation and promotes synovial tissue inflammation
por: Wen, Zhenke, et al.
Publicado: (2019)

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors
por: Brand, Stephen, et al.
Publicado: (2011)

High-resolution snapshots of human N-myristoyltransferase in action illuminate a mechanism promoting N-terminal Lys and Gly myristoylation
por: Dian, Cyril, et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_ajn8fj5lnaso8tvhea8ucmfkoa