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Search indexed NASA NTRS and DOE OSTI research on propulsion, heat transfer, battery materials and energy systems. Follow report and document links to the original sources.
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Fluorinated HIV-1 protease inhibitors containing chiral hydroxyethylbenzene and indanol as P2′ ligands with potent activity against drug-resistant variants
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Automating biomedical literature review for rapid drug discovery: Leveraging GPT-4 to expedite pandemic response
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Mapping the lived experience of rural substance use stigma: A conceptual framework of salient attitudes, beliefs, and behaviors in people who use drugs
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A Robust Chromatographic Method for Drug Release profiling of liposomal doxorubicin HCl
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Size-Controlled Templating of Stable Drug Nanoparticles from Nanoemulsion Precursors for Versatile Nanoformulation
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Excipient-Induced Lattice Disorder in Active Pharmaceutical Ingredient: Implications on Drug Product Continuous Manufacturing
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Surfactant–Polymer Complexation and Competition on Drug Nanocrystal Surfaces Control Crystallinity
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The Novel Carbapenem, JDB/PQ-1-219, Has Potent Broad Spectrum Activity against Multi-Drug Resistant Acinetobacter baumannii
Carbapenem resistance in Acinetobacter baumannii, driven largely by class D, along with class A and class B β- lactamases, has severely compromised the utility of these last resort antibiotics. As a result, infections caused by such pathogens are characterized by extremely high mortality rates. Here we describe the antimicrobial activity of the novel C5 methyl-substituted carbapenem JDB/PQ-1−219 against multidrug resistant A. baumannii and the mechanism of its interaction with its major carbapenemase, OXA-23. JDB/PQ-1-219 exhibits potent antimicrobial activity against A. baumannii producing various carbapenemases, with MICs that are all in the clinically susceptible range. The compound has unrestricted ingress through porins and avoids egress by efflux pumps, a unique property when compared to all commercial carbapenems. Kinetic experiments demonstrated that unlike for other carbapenems, acylation of OXA-23 by JDB/ PQ-1-219 is monophasic, and mass spectrometry studies showed that this results from the conversion of all enzyme into a reversible tetrahedral intermediate which gradually transitions into the stable acyl-enzyme complex. No deacylation of this complex is observed over a physiologically relevant time period, making JDB/PQ-1−219 an extremely potent inhibitor of OXA-23. Time-resolved crystallography revealed fine details of active site dynamics, leading to complete inhibition of the enzyme. Together, these studies identify JDB/PQ-1-219 as a uniquely effective novel carbapenem with clinically significant levels of activity against multidrug resistant A. baumannii.
Structural bases for Na+-Cl− cotransporter inhibition by thiazide diuretic drugs and activation by kinases
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Structural basis for human NKCC1 inhibition by loop diuretic drugs
Abstract Na + –K + –Cl − cotransporters functions as an anion importers, regulating trans-epithelial chloride secretion, cell volume, and renal salt reabsorption. Loop diuretics, including furosemide, bumetanide, and torsemide, antagonize both NKCC1 and NKCC2, and are first-line medicines for the treatment of edema and hypertension. NKCC1 activation by the molecular crowding sensing WNK kinases is critical if cells are to combat shrinkage during hypertonic stress; however, how phosphorylation accelerates NKCC1 ion transport remains unclear. Here, we present co-structures of phospho-activated NKCC1 bound with furosemide, bumetanide, or torsemide showing that furosemide and bumetanide utilize a carboxyl group to coordinate and co-occlude a K + , whereas torsemide encroaches and expels the K + from the site. We also found that an amino-terminal segment of NKCC1, once phosphorylated, interacts with the carboxyl-terminal domain, and together, they engage with intracellular ion exit and appear to be poised to facilitate rapid ion translocation. Together, these findings enhance our understanding of NKCC-mediated epithelial ion transport and the molecular mechanisms of its inhibition by loop diuretics.
A membrane penetrating cyclic lipopeptide based nanocarrier for cancer drug delivery
The CLP5 self-assembles into spherical aggregates and encapsulates doxorubicin to form the CLP5@DOX nanomedicine, which exerts a combined antitumor effect by targeting caspase-3 and penetrating the cell membrane.
Dietary modulation of gut microbiota affects susceptibility to drug-induced liver injury
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