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Discovery of Allosteric and Selective Inhibitors of Inorganic Pyrophosphatase from Mycobacterium tuberculosis.

Pang AH1, Garzan A1, Larsen MJ2, McQuade TJ2, Garneau-Tsodikova S1, Tsodikov OV1.
ACS chemical biology.ACS Chem Biol.2016 Nov 18;11(11):3084-3092. Epub 2016 Sep 26.
Inorganic pyrophosphatase (PPiase) is an essential enzyme that hydrolyzes inorganic pyrophosphate (PPi), driving numerous metabolic processes. We report a discovery of an allosteric inhibitor (2,4-bis(aziridin-1-yl)-6-(1-phenylpyrrol-2-yl)-s-triazine) of bacterial PPiases. Analogues of this lead com
PMID 27622287

Isoniazid inhibits human erythroid 5-aminolevulinate synthase: Molecular mechanism and tolerance study with four X-linked protoporphyria patients.

Fratz-Berilla EJ1, Breydo L2, Gouya L3, Puy H3, Uversky VN2, Ferreira GC4.
Biochimica et biophysica acta.Biochim Biophys Acta.2016 Nov 10;1863(2):428-439. doi: 10.1016/j.bbadis.2016.11.011. [Epub ahead of print]
Mutations in the C-terminus of human erythroid 5-aminolevulinate synthase (hALAS2), a pyridoxal 5'-phosphate (PLP)-dependent enzyme, are associated with two different blood disorders, X-linked sideroblastic anemia (XLSA) and X-linked protoporphyria (XLPP). XLSA-causing mutations yield hALAS2 variant
PMID 27838491

Ogawa T1, Murakami K1, Yoshino M2.
FEMS microbiology letters.FEMS Microbiol Lett.2016 Sep;363(17). pii: fnw183. doi: 10.1093/femsle/fnw183. Epub 2016 Jul 31.
The effect of fructose 1,6-bisphosphate (Fru 1,6-P2) on the regulatory enzymes of pentose phosphate pathway of Escherichia coli was examined. Fru 1,6-P2 inhibited E. coli transaldolase (EC 2.2.1.2) competitively against fructose 6-phosphate and uncompetitively against erythrose 4-phosphate, whereas
PMID 27481705

Characterization of a thermostable 2,4-diaminopentanoate dehydrogenase from Fervidobacterium nodosum Rt17-B1(ENZYMOLOGY, PROTEIN ENGINEERING, AND ENZYME TECHNOLOGY)

α-Glucosidase inhibition of 6-hydroxyflavones. Part 3, Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-previous termglucosidasenext term inhibitors