Drug discovery for neglected diseases: molecular target-based and phenotypic approaches: miniperspectives series on phenotypic screening for antiinfective targets

IH Gilbert - Journal of medicinal chemistry, 2013 - ACS Publications
Drug discovery for neglected tropical diseases is carried out using both target-based and
phenotypic approaches. In this paper, target-based approaches are discussed, with a …

Emerging targets for the development of novel antifungal therapeutics

AH Groll, AJ De Lucca, TJ Walsh - Trends in Microbiology, 1998 - cell.com
Invasive mycoses have become important causes of morbidity and mortality in
immunocompromised patients. New approaches for antifungal therapy are required to meet …

N-terminal N-myristoylation of proteins: refinement of the sequence motif and its taxon-specific differences

S Maurer-Stroh, B Eisenhaber, F Eisenhaber - Journal of molecular biology, 2002 - Elsevier
N-terminal N-myristoylation is a lipid anchor modification of eukaryotic and viral proteins
targeting them to membrane locations, thus changing the cellular function of modified …

Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase

M Masubuchi, H Ebiike, K Kawasaki, S Sogabe… - Bioorganic & medicinal …, 2003 - Elsevier
The C-4 side chain modification of lead compound 1 has resulted in the identification of a
potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor RO-09 …

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

S Brand, LAT Cleghorn, SP McElroy… - Journal of medicinal …, 2012 - ACS Publications
N-Myristoyltransferase (NMT) represents a promising drug target for human African
trypanosomiasis (HAT), which is caused by the parasitic protozoa Trypanosoma brucei. We …

Structure of N-myristoyltransferase with bound myristoylCoA and peptide substrate analogs

RS Bhatnagar, K Fütterer, TA Farazi, S Korolev… - nature structural …, 1998 - nature.com
N-myristoyltransferase (Nmt) attaches myristate to the N-terminal glycine of many important
eukaryotic and viral proteins. It is a target for anti-fungal and anti-viral therapy. We have …

[PDF][PDF] Crystal structures of Candida albicans N-myristoyltransferase with two distinct inhibitors

S Sogabe, M Masubuchi, K Sakata, TA Fukami… - Chemistry & Biology, 2002 - cell.com
Myristoyl-CoA: protein N-myristoyltransferase (Nmt) is a monomeric enzyme that catalyzes
the transfer of the fatty acid myristate from myristoyl-CoA to the N-terminal glycine residue of …

Two N-myristoyltransferase isozymes play unique roles in protein myristoylation, proliferation, and apoptosis

CE Ducker, JJ Upson, KJ French, CD Smith - Molecular cancer research, 2005 - AACR
N-myristoyltransferases (NMT) add myristate to the NH2 termini of certain proteins, thereby
regulating their localization and/or biological function. Using RNA interference, this study …

[HTML][HTML] Antheraea peptide and its analog: Their influence on the maturation of the reproductive system, embryogenesis, and early larval development in Tenebrio …

K Walkowiak-Nowicka, S Chowański… - Plos one, 2022 - journals.plos.org
In recent years, many new immunologically active peptides from insects have been
identified. Unfortunately, in most cases, their physiological functions are not fully known. One …

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

JR Harrison, S Brand, V Smith… - Journal of Medicinal …, 2018 - ACS Publications
Crystallography has guided the hybridization of two series of Trypanosoma brucei N-
myristoyltransferase (NMT) inhibitors, leading to a novel highly selective series. The effect of …