Inhibition of the non-Mevalonate Isoprenoid pathway by reverse Hydroxamate analogues of Fosmidomycin

C Lienau, S Konzuch, T Gräwert, B Illarionov… - Procedia …, 2015 - Elsevier
The non-mevalonate (methylerythritol phosphate, MEP) pathway for isoprenoid biosynthesis
is essential in Plasmodium spp.., but is absent in the human host. The pathway is a clinically …

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 …

New Insight into Isoprenoids Biosynthesis Process and Future Prospects for Drug Designing in Plasmodium

GS Saggu, ZR Pala, S Garg, V Saxena - Frontiers in Microbiology, 2016 - frontiersin.org
The MEP (Methyl Erythritol Phosphate) isoprenoids biosynthesis pathway is an attractive
drug target to combat malaria, due to its uniqueness and indispensability for the parasite. It …

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 …

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 …

Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure–activity studies

ZK Yao, PM Krai, EF Merino, ME Simpson… - Bioorganic & medicinal …, 2015 - Elsevier
Compounds that target isoprenoid biosynthesis in Plasmodium falciparum could be a
welcome addition to malaria chemotherapy, since the methylerythritol phosphate (MEP) …

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 …

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 …

Reverse N-Substituted Hydroxamic Acid Derivatives of Fosmidomycin Target a Previously Unknown Subpocket of 1-Deoxy-d-xylulose 5-Phosphate …

MA Abdullaziz, S Takada, B Illarionov… - ACS Infectious …, 2024 - ACS Publications
Reverse analogs of the phosphonohydroxamic acid antibiotic fosmidomycin are potent
inhibitors of the nonmevalonate isoprenoid biosynthesis enzyme 1-deoxy-d-xylulose 5 …

Novel reverse thia-analogs of fosmidomycin: Synthesis and antiplasmodial activity

C Lienau, T Gräwert, LAA Avelar, B Illarionov… - European Journal of …, 2019 - Elsevier
Thia analogs of fosmidomycin are potent inhibitors of the non-mevalonate isoprenoid
biosynthesis enzyme 1-deoxy-d-xylulose 5-phosphate reductoisomerase (IspC, Dxr) of …