Binding modes of reverse fosmidomycin analogs toward the antimalarial target IspC

S Konzuch, T Umeda, J Held, S Hähn… - Journal of medicinal …, 2014 - ACS Publications
1-Deoxy-d-xylulose 5-phosphate reductoisomerase of Plasmodium falciparum (Pf IspC, Pf
Dxr), believed to be the rate-limiting enzyme of the nonmevalonate pathway of isoprenoid …

Mechanism of Action of N-Acyl and N-Alkoxy Fosmidomycin Analogs: Mono- and Bisubstrate Inhibition of IspC from Plasmodium falciparum, a Causative Agent of …

MB Girma, HS Ball, X Wang, RC Brothers… - ACS …, 2021 - ACS Publications
Malaria is a global health threat that requires immediate attention. Malaria is caused by the
protozoan parasite Plasmodium, the most severe form of which is Plasmodium falciparum …

Prodrugs of reverse fosmidomycin analogues

K Brücher, T Gräwert, S Konzuch… - Journal of medicinal …, 2015 - ACS Publications
Fosmidomycin inhibits IspC (Dxr, 1-deoxy-d-xylulose 5-phosphate reductoisomerase), a key
enzyme in nonmevalonate isoprenoid biosynthesis that is essential in Plasmodium …

Targeting an Aromatic Hotspot in Plasmodium falciparum 1‐Deoxy‐d‐xylulose‐5‐phosphate Reductoisomerase with β‐Arylpropyl Analogues of Fosmidomycin

S Sooriyaarachchi, R Chofor, MDP Risseeuw… - …, 2016 - Wiley Online Library
Abstract Blocking the 2‐C‐methyl‐d‐erythrithol‐4‐phosphate pathway for isoprenoid
biosynthesis offers new ways to inhibit the growth of Plasmodium spp. Fosmidomycin [(3‐(N …

Antimalarial and structural studies of pyridine-containing inhibitors of 1-deoxyxylulose-5-phosphate reductoisomerase

J Xue, J Diao, G Cai, L Deng, B Zheng… - ACS medicinal …, 2013 - ACS Publications
1-Deoxy-d-xylulose-5-phosphate reductoisomerase (DXR) in the nonmevalonate isoprene
biosynthesis pathway is a target for developing antimalarial drugs. Fosmidomycin, a potent …

α-Substituted β-oxa isosteres of fosmidomycin: synthesis and biological evaluation

K Brücher, B Illarionov, J Held, S Tschan… - Journal of medicinal …, 2012 - ACS Publications
Specific inhibition of enzymes of the non-mevalonate pathway is a promising strategy for the
development of novel antiplasmodial drugs. α-Aryl-substituted β-oxa isosteres of …

MEPicides: α,β-unsaturated Fosmidomycin N-Acyl Analogs as Efficient Inhibitors of Plasmodium falciparum 1-Deoxy-d-xylulose-5-phosphate reductoisomerase

X Wang, RL Edwards, HS Ball, KM Heidel… - ACS Infectious …, 2023 - ACS Publications
Malaria, a mosquito-borne disease caused by several parasites of the Plasmodium genus,
remains a huge threat to global public health. There are an estimated 0.5 million malaria …

Studies Addressing the Importance of Charge in the Binding of Fosmidomycin‐Like Molecules to Deoxyxylulosephosphate Reductoisomerase

J Perruchon, R Ortmann, M Altenkämper… - ChemMedChem …, 2008 - Wiley Online Library
Fosmidomycin and its homologue FR900098 are inhibitors of 1‐deoxy‐d‐xylulose‐5‐
phosphate reductoisomerase, which is part of the mevalonate‐independent isoprenoid …

Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)

CT Behrendt, A Kunfermann, V Illarionova… - Journal of medicinal …, 2011 - ACS Publications
Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate
pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized …

Molecular basis of fosmidomycin's action on the human malaria parasite Plasmodium falciparum

T Umeda, N Tanaka, Y Kusakabe, M Nakanishi… - Scientific Reports, 2011 - nature.com
The human malaria parasite Plasmodium falciparum is responsible for the deaths of more
than a million people each year. Fosmidomycin has been proven to be efficient in the …