The Experts below are selected from a list of 303 Experts worldwide ranked by ideXlab platform

Bo Tang - One of the best experts on this subject based on the ideXlab platform.

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    Journal of the American Chemical Society, 2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the pos...

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the positive correlation between AChE and O2•– levels associated with depressive behaviors. This finding suggests that oxidative stress may induce AChE overactivation, leading to depression-related behaviors. This work provides a new and rewarding perspective to elucidate the role of oxidative stress regulating AChE in the pathology of depression

Xin Wang - One of the best experts on this subject based on the ideXlab platform.

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    Journal of the American Chemical Society, 2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the pos...

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the positive correlation between AChE and O2•– levels associated with depressive behaviors. This finding suggests that oxidative stress may induce AChE overactivation, leading to depression-related behaviors. This work provides a new and rewarding perspective to elucidate the role of oxidative stress regulating AChE in the pathology of depression

Wen Zhang - One of the best experts on this subject based on the ideXlab platform.

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    Journal of the American Chemical Society, 2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the pos...

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the positive correlation between AChE and O2•– levels associated with depressive behaviors. This finding suggests that oxidative stress may induce AChE overactivation, leading to depression-related behaviors. This work provides a new and rewarding perspective to elucidate the role of oxidative stress regulating AChE in the pathology of depression

Qi Ding - One of the best experts on this subject based on the ideXlab platform.

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    Journal of the American Chemical Society, 2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the pos...

  • Observation of AcetylcholinEsterase in Stress-Induced Depression Phenotypes by Two-Photon Fluorescence Imaging in the Mouse Brain
    2019
    Co-Authors: Xin Wang, Qi Ding, Wen Zhang, Bo Tang
    Abstract:

    Oxidative stress in depression is a prime cause of neurotransmitter metabolism dysfunction in the brain. AcetylcholinEsterase (AChE), a key hydrolase in the cholinergic system, directly determines the degradation of neurotransmitters. However, due to the complexity of the brain and lack of appropriate in situ imaging tools, the mechanism underlying the changes in AChE activity in depression remains unclear. Hence, we generated a two-photon fluorescence probe (MCYN) for real-time visualization of AChE with excellent sensitivity and selectivity. AChE can specifically recognize and cleave the Carbamic Acid Ester bond in MCYN, and MCYN emits bright fluorescence at 560 nm by two-photon excitation at 800 nm. By utilizing MCYN to monitor AChE, we discovered a significant increase in AChE activity in the brains of mice with depression phenotypes. Notably, with the assistance of a two-photon fluorescence imaging probe of the superoxide anion radical (O2•–), in vivo visualization for the first time revealed the positive correlation between AChE and O2•– levels associated with depressive behaviors. This finding suggests that oxidative stress may induce AChE overactivation, leading to depression-related behaviors. This work provides a new and rewarding perspective to elucidate the role of oxidative stress regulating AChE in the pathology of depression

Stefano Ponzano - One of the best experts on this subject based on the ideXlab platform.

  • Potent α-amino-β-lactam Carbamic Acid Ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies.
    European journal of medicinal chemistry, 2016
    Co-Authors: Andrea Nuzzi, Annalisa Fiasella, Jose Antonio Ortega, Chiara Pagliuca, Stefano Ponzano, Daniela Pizzirani, Sine Mandrup Bertozzi, Giuliana Ottonello, Glauco Tarozzo, Angelo Reggiani
    Abstract:

    4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate (3b) is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, we describe structure-activity relationship (SAR) studies on 3-aminoazetidin-2-one derivatives, which have led to the identification of 3b, and expand these studies to elucidate the principal structural and stereochemical features needed to achieve effective NAAA inhibition. Investigations on the influence of the substitution at the β-position of the 2-oxo-3-azetidinyl ring as well as on the effect of size and shape of the Carbamic Acid Ester side chain led to the discovery of 3ak, a novel inhibitor of human NAAA that shows an improved physicochemical and drug-like profile relative to 3b. This favourable profile, along with the structural diversity of the Carbamic Acid chain of 3b, identify this compound as a promising new tool to investigate the potential of NAAA inhibitors as therapeutic agents for the treatment of pain and inflammation.

  • Synthesis, Biological Evaluation, and 3D QSAR Study of 2-Methyl-4-oxo-3-oxetanylCarbamic Acid Esters as N-Acylethanolamine Acid Amidase (NAAA) Inhibitors
    Journal of medicinal chemistry, 2014
    Co-Authors: Stefano Ponzano, Anna Berteotti, Rita Petracca, Romina Vitale, Luisa Mengatto, Tiziano Bandiera, Andrea Cavalli, Daniele Piomelli, Fabio Bertozzi, Giovanni Bottegoni
    Abstract:

    N-(2-Oxo-3-oxetanyl)Carbamic Acid Esters have recently been reported to be noncompetitive inhibitors of the N-acylethanolamine Acid amidase (NAAA) potentially useful for the treatment of pain and inflammation. In the present study, we further explored the structure–activity relationships of the Carbamic Acid Ester side chain of 2-methyl-4-oxo-3-oxetanylCarbamic Acid Ester derivatives. Additional favorable features in the design of potent NAAA inhibitors have been found together with the identification of a single digit nanomolar inhibitor. In addition, we devised a 3D QSAR using the atomic property field method. The model turned out to be able to account for the structural variability and was prospectively validated by designing, synthesizing, and testing novel inhibitors. The fairly good agreement between predictions and experimental potency values points to this 3D QSAR model as the first example of quantitative structure–activity relationships in the field of NAAA inhibitors.

  • Synthesis, Biological Evaluation, and 3D QSAR Study of 2‑Methyl-4-oxo-3-oxetanylCarbamic Acid Esters as N‑Acylethanolamine Acid Amidase (NAAA) Inhibitors
    2014
    Co-Authors: Stefano Ponzano, Anna Berteotti, Rita Petracca, Romina Vitale, Luisa Mengatto, Tiziano Bandiera, Andrea Cavalli, Daniele Piomelli, Fabio Bertozzi, Giovanni Bottegoni
    Abstract:

    N-(2-Oxo-3-oxetanyl)­Carbamic Acid Esters have recently been reported to be noncompetitive inhibitors of the N-acylethanolamine Acid amidase (NAAA) potentially useful for the treatment of pain and inflammation. In the present study, we further explored the structure–activity relationships of the Carbamic Acid Ester side chain of 2-methyl-4-oxo-3-oxetanylCarbamic Acid Ester derivatives. Additional favorable features in the design of potent NAAA inhibitors have been found together with the identification of a single digit nanomolar inhibitor. In addition, we devised a 3D QSAR using the atomic property field method. The model turned out to be able to account for the structural variability and was prospectively validated by designing, synthesizing, and testing novel inhibitors. The fairly good agreement between predictions and experimental potency values points to this 3D QSAR model as the first example of quantitative structure–activity relationships in the field of NAAA inhibitors