Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01913
Abstract: Novel analogues of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs) are described that are potent inhibitors of the human geranylgeranyl pyrophosphate synthase (hGGPPS). Members of this class of compounds induce target-selective apoptosis of multiple myeloma (MM) cells and… read more here.
Keywords: inhibitors human; geranylgeranyl pyrophosphate; thienopyrimidine based; pyrophosphate synthase ... See more keywords
Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00886
Abstract: Post-translational prenylation of the small GTP-binding proteins (GTPases) is vital to a plethora of biological processes, including cellular proliferation. We have identified a new class of thienopyrimidine-based bisphosphonate (ThP-BP) inhibitors of the human geranylgeranyl pyrophosphate… read more here.
Keywords: multiple myeloma; geranylgeranyl pyrophosphate; prenylation; pyrophosphate synthase ... See more keywords
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01104
Abstract: Thienopyrimidine-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS), characterized by a chiral α-aminophosphonic acid moiety, were synthesized as enantiomerically enriched pairs and their binding mode was investigated by X-ray crystallography. A general consensus… read more here.
Keywords: farnesyl pyrophosphate; based allosteric; human farnesyl; allosteric inhibitors ... See more keywords
QSAR Models for Nitrogen Containing Monophosphonate and Bisphosphonate Derivatives as Human Farnesyl Pyrophosphate Synthase Inhibitors Based on Monte Carlo Method.
Sign Up to like & getrecommendations! Published in 2019 at "Drug research"
DOI: 10.1055/a-0652-5290
Abstract: Human farnesyl pyrophosphate synthase (hFPPS) is a well-settled therapeutic target and it is an enzyme of the mevalonate pathway which catalyzes the biosynthesis of the C-15 isoprenoid farnesyl pyrophosphate. QSAR studies by using Monte Carlo… read more here.
Keywords: farnesyl pyrophosphate; pyrophosphate synthase; qsar models; human farnesyl ... See more keywords
Ovarian transcriptome and metabolic responses of RNAi-mediated farnesyl pyrophosphate synthase knockdown in Neocaridina denticulata sinensis.
Sign Up to like & getrecommendations! Published in 2022 at "Genomics"
DOI: 10.2139/ssrn.4125379
Abstract: Methyl farnesoate (MF) is considered the equivalent of JH in crustaceans and plays an essential role in many crucial physiological processes. It is believed that farnesyl pyrophosphate synthase (FPPS) plays an essential role in the… read more here.
Keywords: neocaridina denticulata; role; pyrophosphate synthase; denticulata sinensis ... See more keywords
Anthranilic Acid Inhibitors of Undecaprenyl Pyrophosphate Synthase (UppS), an Essential Enzyme for Bacterial Cell Wall Biosynthesis
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DOI: 10.3389/fmicb.2018.03322
Abstract: We report the successful implementation of virtual screening in the discovery of new inhibitors of undecaprenyl pyrophosphate synthase (UppS) from Escherichia coli. UppS is an essential enzyme in the biosynthesis of bacterial cell wall. It… read more here.
Keywords: inhibitors undecaprenyl; upps essential; undecaprenyl pyrophosphate; synthase upps ... See more keywords
Crystal Structure of Geranylgeranyl Pyrophosphate Synthase (CrtE) Involved in Cyanobacterial Terpenoid Biosynthesis
Sign Up to like & getrecommendations! Published in 2020 at "Frontiers in Plant Science"
DOI: 10.3389/fpls.2020.00589
Abstract: Cyanobacteria are photosynthetic prokaryotes that perform oxygenic photosynthesis. Due to their ability to use the photon energy of sunlight to fix carbon dioxide into biomass, cyanobacteria are promising hosts for the sustainable production of terpenoids,… read more here.
Keywords: crte; crystal structure; pyrophosphate; geranylgeranyl pyrophosphate ... See more keywords