Mannich bases in medicinal chemistry and drug design

G Roman - European journal of medicinal chemistry, 2015 - Elsevier
The biological activity of Mannich bases, a structurally heterogeneous class of chemical
compounds that are generated from various substrates through the introduction of an …

A not-so-ancient grease history: click chemistry and protein lipid modifications

KF Suazo, KY Park, MD Distefano - Chemical reviews, 2021 - ACS Publications
Protein lipid modification involves the attachment of hydrophobic groups to proteins via
ester, thioester, amide, or thioether linkages. In this review, the specific click chemical …

Structure and Functional Diversity of GCN5-Related N-Acetyltransferases (GNAT)

AIM Salah Ud-Din, A Tikhomirova… - International journal of …, 2016 - mdpi.com
General control non-repressible 5 (GCN5)-related N-acetyltransferases (GNAT) catalyze the
transfer of an acyl moiety from acyl coenzyme A (acyl-CoA) to a diverse group of substrates …

Metabolic reprogramming of ovarian cancer involves ACSL1-mediated metastasis stimulation through upregulated protein myristoylation

Q Zhang, W Zhou, S Yu, Y Ju, SKY To, AST Wong… - Oncogene, 2021 - nature.com
As a result of the hostile microenvironment, metabolic alterations are required to enable the
malignant growth of cancer cells. To understand metabolic reprogramming during …

High-resolution snapshots of human N-myristoyltransferase in action illuminate a mechanism promoting N-terminal Lys and Gly myristoylation

C Dian, I Pérez-Dorado, F Rivière, T Asensio… - Nature …, 2020 - nature.com
The promising drug target N-myristoyltransferase (NMT) catalyses an essential protein
modification thought to occur exclusively at N-terminal glycines (Gly). Here, we present high …

Myristoylation confers noncanonical AMPK functions in autophagy selectivity and mitochondrial surveillance

J Liang, ZX Xu, Z Ding, Y Lu, Q Yu, KD Werle… - Nature …, 2015 - nature.com
AMP-activated protein kinase (AMPK) plays a central role in cellular energy sensing and
bioenergetics. However, the role of AMPK in surveillance of mitochondrial damage and …

Targeting N-myristoylation for therapy of B-cell lymphomas

E Beauchamp, MC Yap, A Iyer… - Nature …, 2020 - nature.com
Myristoylation, the N-terminal modification of proteins with the fatty acid myristate, is critical
for membrane targeting and cell signaling. Because cancer cells often have increased N …

Recent approaches to chemical discovery and development against malaria and the neglected tropical diseases human African trypanosomiasis and schistosomiasis

M Njoroge, NM Njuguna, P Mutai… - Chemical …, 2014 - ACS Publications
Neglected tropical diseases (NTDs) refer to a group of infectious diseases, which though
treatable and/or preventable, remain a leading cause of morbidity and mortality among the …

Design, synthesis, bio-evaluation, and in silico studies of some N-substituted 6-(chloro/nitro)-1 H-benzimidazole derivatives as antimicrobial and anticancer agents

EC Pham, TVT Le, TN Truong - RSC advances, 2022 - pubs.rsc.org
A new series of 6-substituted 1H-benzimidazole derivatives were synthesized by reacting
various substituted aromatic aldehydes with 4-nitro-o-phenylenediamine and 4-chloro-o …

Nuclear functions of the tyrosine kinase Src

G Bagnato, M Leopizzi, E Urciuoli… - International Journal of …, 2020 - mdpi.com
Src is the representative member of the Src-family kinases (SFKs), a group of tyrosine
kinases involved in several cellular processes. Its main function has been for long confined …