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Spectrophotometric comparison of 4-Nitrophenyl carbonates & carbamates as base-labile protecting groups

Kocalar et al. | Dec 12, 2022

Spectrophotometric comparison of 4-Nitrophenyl carbonates & carbamates as base-labile protecting groups

In organic synthesis, protecting groups are derivatives of reactive functionalities that play a key role in ensuring chemoselectivity of chemical transformations. To protect alcohols and amines, acid-labile tert-butyloxycarbonyl protecting groups are often employed but are avoided when the substrate is acid-sensitive. Thus, orthogonal base-labile protecting groups have been in demand to enable selective deprotection and to preserve the reactivity of acid-sensitive substrates. To meet this demand, we present 4-nitrophenyl carbonates and carbamates as orthogonal base-labile protecting group strategies.

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Investigating the Role of the Novel ESCRT-III Recruitment Factor CCDC11 in HIV Budding: A Potential Target for Antiviral Therapy

Takemaru et al. | Feb 24, 2020

Investigating the Role of the Novel ESCRT-III Recruitment Factor CCDC11 in HIV Budding: A Potential Target for Antiviral Therapy

Acquired immunodeficiency syndrome (AIDS) is a life-threatening condition caused by the human immunodeficiency virus (HIV). In this work, Takemaru et al explored the role of Coiled-Coil Domain-Containing 11 (CCDC11) in HIV-1 budding. Their results suggest that CCDC11 is critical for efficient HIV-1 budding, potentially indicating CCDC11 a viable target for antiviral therapeutics without major side effects.

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The analysis of the viral transmission and structural interactions between the HIV-1 envelope glycoprotein and the lymphocyte receptor integrin α4β7

Ganesh et al. | Apr 28, 2021

The analysis of the viral transmission and structural interactions between the HIV-1 envelope glycoprotein and the lymphocyte receptor integrin α4β7

The Human Immunodeficiency Virus (HIV) infects approximately 40 million people globally, and one million people die every year from Acquired Immune Deficiency Syndrome (AIDS)-related illnesses. This study examined the interactions between the HIV-1 envelope glycoprotein gp120 and the human lymphocyte receptor integrin α4β7, the putative first long-range receptor for the envelope glycoprotein of the virus in mucosal tissues. Presented data support the claim that the V1 loop is involved in the binding between α4β7 and the HIV-1 envelope glycoprotein through molecular dockings.

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Effects of Temperature on Hand Sanitizer Efficiency

Molom-Ochir et al. | May 11, 2022

Effects of Temperature on Hand Sanitizer Efficiency

Here, recognizing the widespread use of hand sanitizers, the authors investigated their effectiveness in relation to storage temperature. They applied hand sanitizer before and after touching a cell phone and used LB-agar plates to monitor the growth of bacteria following this process. They found that 70% ethyl-alcohol-based sanitizers are least effective at temperatures above 107.27 °F and most effective at 96.17 °F.

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Testing the Effects of Resveratrol, Apigenin, and Glucosamine to Effectively Reduce Prostate Cancer Cell Proliferation, Migration Levels, and Increase Apoptosis

Yang et al. | Apr 16, 2020

Testing the Effects of Resveratrol, Apigenin, and Glucosamine to Effectively Reduce Prostate Cancer Cell Proliferation, Migration Levels, and Increase Apoptosis

The current five-year survival rate of metastasized prostate cancer is only 30% and occurs in every one in nine men. Researchers have shown that people with a type of dwarfism called Laron’s Syndrome are immune to cancer due to their low levels of insulin-like growth factor-1 (IGF-1). For this reason, experimentally modifying the level of IGF-1 could provide better insight into whether lowering the levels of IGF-1 in prostate cancer cell lines (e.g. PC-3) could be an effective treatment to reduce their rates of proliferation and migration and increase apoptosis. We selected three compounds, which researchers have shown decrease IGF-1 levels, to test and combine to determine which is the most promising.

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Developing anticholinergic drugs for the treatment of asthma with improved efficacy

Wong et al. | Jul 05, 2023

Developing anticholinergic drugs for the treatment of asthma with improved efficacy
Image credit: Wong et al.

Anticholinergics are used in treating asthma, a chronic inflammation of the airways. These drugs block human M1 and M2 muscarinic acetylcholine receptors, inhibiting bronchoconstriction. However, studies have reported complications of anticholinergic usage, such as exacerbated eosinophil production and worsened urinary retention. Modification of known anticholinergics using bioisosteric replacements to increase efficacy could potentially minimize these complications. The present study focuses on identifying viable analogs of anticholinergics to improve binding energy to the receptors compared to current treatment options. Glycopyrrolate (G), ipratropium (IB), and tiotropium bromide (TB) were chosen as parent drugs of interest, due to the presence of common functional groups within the molecules, specifically esters and alcohols. Docking score analysis via AutoDock Vina was used to evaluate the binding energy between drug analogs and the muscarinic acetylcholine receptors. The final results suggest that G-A3, IB-A3, and TB-A1 are the most viable analogs, as binding energy was improved when compared to the parent drug. G-A4, IB-A4, IB-A5, TB-A3, and TB-A4 are also potential candidates, although there were slight regressions in binding energy to both muscarinic receptors for these analogs. By researching the effects of bioisosteric replacements of current anticholinergics, it is evident that there is a potential to provide asthmatics with more effective treatment options.

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Who is at Risk for a Spinal Fracture? – A Comparative Study of National Health and Nutrition Examination Survey Data

He et al. | Mar 01, 2018

Who is at Risk for a Spinal Fracture? – A Comparative Study of National Health and Nutrition Examination Survey Data

One common age-related health problem is the loss of bone mineral density (BMD), which can lead to a variety of negative health outcomes, including increased risk of spinal fracture. In this study, the authors investigate risk factors that may be predictive of an individual's risk of spinal fracture. Their findings provide valuable information that clinicians can use in patient evaluations.

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