- A General Approach to Convert Hemicyanine Dyes into Highly Optimized Photoacoustic Scaffolds for Analyte Sensing**
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Most photoacoustic (PA) imaging agents are based on the repurposing of existing fluorescent dye platforms that exhibit non-optimal properties for PA applications. Herein, we introduce PA-HD, a new dye scaffold optimized for PA probe development that features a 4.8-fold increase in sensitivity and a red-shift of the λabs from 690 nm to 745 nm to enable ratiometric imaging. Computational modeling was used to elucidate the origin of these enhanced properties. To demonstrate the generalizability of our remodeling efforts, we developed three probes for β-galactosidase activity (PA-HD-Gal), nitroreductase activity (PA-HD-NTR), and H2O2 (PA-HD-H2O2). We generated two cancer models to evaluate PA-HD-Gal and PA-HD-NTR. We employed a murine model of Alzheimer's disease to test PA-HD-H2O2. There, we observed a PA signal increase at 735 nm of 1.79±0.20-fold relative to background, indicating the presence of oxidative stress. These results were confirmed via ratiometric calibration, which was not possible using the parent HD platform.
- Brady, Catharine J.,Chan, Jefferson,Gardner, Sarah H.,Hirschi, Jennifer S.,Keeton, Cameron,Lucero, Melissa Y.,Mallojjala, Sharath C.,Mirica, Liviu M.,Su, Shengzhang,Yadav, Anuj K.,Yu, Zhengxin
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Read Online
- Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue
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Analogues of the natural product cyclosporine A (CsA) were developed and assessed as antivirals against infection of hepatitis B virus (HBV) and its satellite hepatitis D virus (HDV). An analogue termed 27A exhibits potent inhibition of HBV/HDV infection by specifically blocking viral engagement to its cellular receptor NTCP, while it lacks immunosuppressive activity found in natural CsA. Intraperitoneal injection or oral intake of 27A protects HDV-susceptible mouse model from HDV infection. 27A serves as a promising lead for the development of novel anti-HDV/HBV agents.
- Liu, Yang,Ruan, Hanying,Li, Ying,Sun, Guoliang,Liu, Xiao,He, Wenhui,Mao, Fengfeng,He, Miaomiao,Yan, Liwei,Zhong, Guocai,Yan, Huan,Li, Wenhui,Zhang, Zhiyuan
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supporting information
p. 543 - 565
(2021/01/13)
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- NTCP INHIBITORS
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Provided are cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection (s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.
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Paragraph 0234; 0239
(2019/11/04)
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- NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
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This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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Page/Page column 65-66
(2010/12/26)
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- Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine
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Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula STR1 wherein R2, R3, R7 and R8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R2, R3, R7 and R8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.
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