Studies on daptomycin lactam‐based analogues
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DOI: 10.1002/psc.3430
Abstract: Herein, we report the synthesis and antibacterial evaluation of a series of daptomycin lactam‐based analogues. As compared with daptomycin, the daptomycin analogue with singly modified lactam has an eightfold increase in its minimum inhibitory concentration… read more here.
Keywords: antibacterial activity; based analogues; lactam based; daptomycin lactam ... See more keywords
Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists
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DOI: 10.1007/s10822-017-0025-6
Abstract: HX531, which contains a dibenzodiazepine skeleton, is one of the first retinoid X receptor (RXR) antagonists. Functioning via RXR-PPARγ heterodimer, this compound is receiving a lot of attention as a therapeutic drug candidate for diabetic… read more here.
Keywords: function fixed; docking mode; active conformation; retinoid receptor ... See more keywords
MCC950 closes the active conformation of NLRP3 to an inactive state
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DOI: 10.1038/s41589-019-0278-6
Abstract: NLRP3 (NOD-like receptor pyrin domain-containing protein 3) is an innate immune sensor that contributes to the development of different diseases, including monogenic autoinflammatory syndromes, gout, atherosclerosis, and Alzheimer’s disease. The molecule sulfonylurea MCC950 is a… read more here.
Keywords: mcc950; closes active; conformation; active conformation ... See more keywords
The K+-Dependent and -Independent Pyruvate Kinases Acquire the Active Conformation by Different Mechanisms
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DOI: 10.3390/ijms23031347
Abstract: Eukarya pyruvate kinases possess glutamate at position 117 (numbering of rabbit muscle enzyme), whereas bacteria have either glutamate or lysine. Those with E117 are K+-dependent, whereas those with K117 are K+-independent. In a phylogenetic tree,… read more here.
Keywords: pyruvate kinases; dependent independent; independent pyruvate; active conformation ... See more keywords