Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
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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
Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps
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DOI: 10.1038/s41467-021-27726-2
Abstract: Efflux transporters of the RND family confer resistance to multiple antibiotics in Gram-negative bacteria. Here, we identify and chemically optimize pyridylpiperazine-based compounds that potentiate antibiotic activity in E. coli through inhibition of its primary RND… read more here.
Keywords: pyridylpiperazine based; allosteric inhibitors; based allosteric; rnd type ... See more keywords
Peptide-based allosteric inhibitor targets TNFR1 conformationally active region and disables receptor–ligand signaling complex
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DOI: 10.1073/pnas.2308132121
Abstract: Significance Tumor necrosis factor (TNF) is a critical regulator of inflammatory responses against harmful stimuli such as infections. However, excessive amount of TNF can cause autoimmune diseases. Current anti-TNF therapeutics are expensive and can induce… read more here.
Keywords: peptide based; allosteric inhibitor; receptor ligand; conformationally active ... See more keywords