The chemical biology of modular biosynthetic enzymes

JL Meier, MD Burkart - Chemical Society Reviews, 2009 - pubs.rsc.org
Fatty acid synthase (FAS), polyketide synthase (PKS), and nonribosomal peptide synthetase
(NRPS) modular biosynthetic enzymes are responsible for the production of a multitude of …

Recent advances in targeting coenzyme A biosynthesis and utilization for antimicrobial drug development

WJA Moolman, M de Villiers… - Biochemical Society …, 2014 - portlandpress.com
The biosynthesis and utilization of CoA (coenzyme A), the ubiquitous and essential acyl
carrier in all organisms, have long been regarded as excellent targets for the development of …

Pantothenamides Are Potent, On-Target Inhibitors of Plasmodium falciparum Growth When Serum Pantetheinase Is Inactivated

C Spry, C Macuamule, Z Lin, KG Virga, RE Lee… - PloS one, 2013 - journals.plos.org
Growth of the virulent human malaria parasite Plasmodium falciparum is dependent on an
extracellular supply of pantothenate (vitamin B5) and is susceptible to inhibition by …

Structural modification of pantothenamides counteracts degradation by pantetheinase and improves antiplasmodial activity

M de Villiers, C Macuamule, C Spry… - ACS medicinal …, 2013 - ACS Publications
Pantothenamides are secondary or tertiary amides of pantothenic acid, the vitamin precursor
of the essential cofactor and universal acyl carrier coenzyme A. A recent study has …

Variation in pantothenate kinase type determines the pantothenamide mode of action and impacts on coenzyme A salvage biosynthesis

M de Villiers, L Barnard, L Koekemoer… - The FEBS …, 2014 - Wiley Online Library
N‐substituted pantothenamides are analogues of pantothenic acid, the vitamin precursor of
CoA, and constitute a class of well‐studied bacterial growth inhibitors that show potential as …

Combination of pantothenamides with vanin inhibitors as a novel antibiotic strategy against gram-positive bacteria

PAM Jansen, PHH Hermkens… - Antimicrobial agents …, 2013 - Am Soc Microbiol
The emergence of resistance against current antibiotics calls for the development of new
compounds to treat infectious diseases. Synthetic pantothenamides are pantothenate …

Antiplasmodial mode of action of pantothenamides: pantothenate kinase serves as a metabolic activator not as a target

M de Villiers, C Spry, CJ Macuamule… - ACS Infectious …, 2017 - ACS Publications
N-Substituted pantothenamides (PanAms) are pantothenate analogues with up to
nanomolar potency against blood-stage Plasmodium falciparum (the most virulent species …

Pantothenate utilization by Plasmodium as a target for antimalarial chemotherapy

C Spry, DA Van Schalkwyk, E Strauss… - … Formerly Current Drug …, 2010 - ingentaconnect.com
In the absence of an effective vaccine against malaria suitable for widespread deployment,
the control of this lethal infectious disease relies heavily on antimalarial chemotherapies …

Exploiting the coenzyme A biosynthesis pathway for the identification of new antimalarial agents: the case for pantothenamides

KJ Saliba, C Spry - Biochemical Society Transactions, 2014 - portlandpress.com
Malaria kills more than half a million people each year. There is no vaccine, and recent
reports suggest that resistance is developing to the antimalarial regimes currently …

Geminal dialkyl derivatives of N-substituted pantothenamides: synthesis and antibacterial activity

TO Akinnusi, K Vong, K Auclair - Bioorganic & medicinal chemistry, 2011 - Elsevier
As a key precursor of coenzyme A (CoA) biosynthesis, pantothenic acid has proven to be a
useful backbone to elaborate probes of this biosynthetic pathway, study CoA-utilizing …