Cargando…

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

N-Myristoyltransferase (NMT) is a potential drug target in Leishmania parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for Leishmania donovani NMT; development led to high affinity inhibitors with excellent ligand efficiency. The bind...

Descripción completa

Detalles Bibliográficos
Autores principales:	Rackham, Mark D., Yu, Zhiyong, Brannigan, James A., Heal, William P., Paape, Daniel, Barker, K. Victoria, Wilkinson, Anthony J., Smith, Deborah F., Leatherbarrow, Robin J., Tate, Edward W.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Royal Society of Chemistry 2015
Materias:	Chemistry
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4757855/ https://www.ncbi.nlm.nih.gov/pubmed/26962429 http://dx.doi.org/10.1039/c5md00241a

Ejemplares similares

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

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

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

Structure-Based Design of Potent and Selective LeishmaniaN-Myristoyltransferase Inhibitors
por: Hutton, Jennie A., et al.
Publicado: (2014)

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)

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

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)

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

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

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

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

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)

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

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

Binding Affinity Determines Substrate Specificity and Enables Discovery of Substrates for N-Myristoyltransferases
por: Su, Dan, et al.
Publicado: (2021)

The identification of kala-azar and the discovery of Leishmania donovani.
por: Gibson, M E
Publicado: (1983)

Reply to Comment on “Binding Affinity Determines Substrate Specificity and Enables Discovery of substrates for N-Myristoyltransferases”
por: Su, Dan, et al.
Publicado: (2022)

LEISHMANIA DONOVANI IN THE PERIPHERAL BLOOD
por: Young, Charles W., et al.
Publicado: (1923)

Proteomic analysis of the secretome of Leishmania donovani
por: Silverman, J Maxwell, et al.
Publicado: (2008)

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

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

Surface antigens of Leishmania donovani promastigotes
Publicado: (1983)

Vaccine Development Against Leishmania donovani
por: Das, Amrita, et al.
Publicado: (2012)

Leishmania donovani bodies in bone marrow
por: Ali, Natasha, et al.
Publicado: (2014)

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

Leishmania donovani and Cutaneous Leishmaniasis, Sri Lanka
por: Siriwardana, H. V. Yamuna D., et al.
Publicado: (2007)

Global genome diversity of the Leishmania donovani complex
por: Franssen, Susanne U, et al.
Publicado: (2020)

Identification of Drosophila Gene Products Required for Phagocytosis of Leishmania donovani
por: Peltan, Adam, et al.
Publicado: (2012)

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

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

Leishmania donovani Develops Resistance to Drug Combinations
por: García-Hernández, Raquel, et al.
Publicado: (2012)

Hemophagocytosis in Experimental Visceral Leishmaniasis by Leishmania donovani
por: Morimoto, Ayako, et al.
Publicado: (2016)

On Transient Infections with Leishmania Donovani in Man and Animals
por: Knowles, R., et al.
Publicado: (1924)

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

Central Asian Rodents as Model Animals for Leishmania major and Leishmania donovani Research
por: Vojtkova, Barbora, et al.
Publicado: (2020)

Efficient infection of hamster with Leishmania donovani by retro-orbital inoculation
por: Jiménez-Antón, M. D., et al.
Publicado: (2019)

Bone marrow aspirate showing Leishmania donovani in polymorphs
por: Chandra, Harish, et al.
Publicado: (2013)

Seroepidemiology and molecular diversity of Leishmania donovani complex in Georgia
por: Babuadze, Giorgi, et al.
Publicado: (2016)

Fitness of Leishmania donovani Parasites Resistant to Drug Combinations
por: García-Hernández, Raquel, et al.
Publicado: (2015)

Cannot write session to /tmp/vufind_sessions/sess_1rtjng933401iqi2pq74tnma99