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Artikel ; Online: Asymmetric Synthesis of CIDD-0072424 via an Enantioselective Nitro-Mannich Reaction: A Central Nervous System Penetrant, Selective Small Molecule Inhibitor of Protein Kinase C Epsilon.

De Kraker, Harmannus / Wang, Hua-Yu Leo / Arman, Hadi D / Renteria, Rachel N / Fleischer, Caleb N / Messing, Robert O / McHardy, Stanton F

The Journal of organic chemistry

2024 Band 89, Heft 7, Seite(n) 5134–5141

Abstract: CIDD-0072424 is a novel small molecule ... ...

Abstract	CIDD-0072424 is a novel small molecule developed
Mesh-Begriff(e)	Protein Kinase C-epsilon ; Stereoisomerism ; Catalysis
Chemische Substanzen	Protein Kinase C-epsilon (EC 2.7.11.13)
Sprache	Englisch
Erscheinungsdatum	2024-03-15
Erscheinungsland	United States
Dokumenttyp	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	123490-0
ISSN	1520-6904 ; 0022-3263
ISSN (online)	1520-6904
ISSN	0022-3263
DOI	10.1021/acs.joc.3c02917
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel: The Effect of Temperature and Moisture on Colonization of Apple Fruit and Branches by Botryosphaeria dothidea

Liu, Jing / Zhang, Lu-yao / Wang, Hua-yu / Liu, Na / Lian, Sen / Xu, Xiang-ming / Li, Bao-hua

Phytopathology. 2022 Aug., v. 112, no. 8

2022

Abstract: Botryosphaeria dothidea causes severe disease of apple trees in China. The process of conidium germination, colonization, and infection of apple fruit and branches was examined on ‘Fuji’ apple and the effect of temperature, surface wetness and relative ... ...

Abstract	Botryosphaeria dothidea causes severe disease of apple trees in China. The process of conidium germination, colonization, and infection of apple fruit and branches was examined on ‘Fuji’ apple and the effect of temperature, surface wetness and relative humidity (RH), and host surface washates on these processes was studied in controlled environments. Initial germ tube development and hyphal growth resulted in the colonization of the host surface without forming an infection structure. Hyphae expanded radially across the host surface and, after entering lenticels, developed into a dense mycelium mass or differentiated pseudoparenchyma. Hyphae from the bottom of the pseudoparenchyma either directly penetrated the lenticel surface intercellularly through the cell layer, or formed an undifferentiated hypha that invaded the lenticel through cracks formed during the lenticel development. Conidial germination and hyphal colonization occurred at 10 to 40°C, with an optimum of approximately 28°C. Conidial germination required an RH > 95% or surface wetness but, for hyphal colonization, an RH > 90% was sufficient. Conidia germinated and formed germ tubes within 1 h under optimum conditions. However, the pathogen required a longer period at RH > 90% or surface wetness for hyphae to colonize and form pseudoparenchyma or dense mycelia on the host surface. Hyphal colonization is a crucial stage for infection of apple tissues by B. dothidea.
Schlagwörter	Botryosphaeria dothidea ; apples ; conidia ; disease severity ; germ tube ; germination ; mycelium ; pathogens ; plant pathology ; relative humidity ; temperature ; China
Sprache	Englisch
Erscheinungsverlauf	2022-08
Umfang	p. 1698-1709.
Erscheinungsort	The American Phytopathological Society
Dokumenttyp	Artikel
ZDB-ID	208889-7
ISSN	1943-7684 ; 0031-949X
ISSN (online)	1943-7684
ISSN	0031-949X
DOI	10.1094/PHYTO-11-21-0487-R
Datenquelle	NAL Katalog (AGRICOLA)

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Artikel ; Online: Discovery and Optimization of N-Arylated Tetracyclic Dicarboximides That Target Primary Glioma Stem-like Cells.

Wang, Hua-Yu / Nguyen, Thu P / Sternisha, Alex C / Carroll, Christopher L / Cross, Bethany / Morlock, Lorraine / Williams, Noelle S / McBrayer, Samuel / Nijhawan, Deepak / De Brabander, Jef K

Journal of medicinal chemistry

2024

Abstract: We recently discovered a novel N-aryl tetracyclic dicarboximide MM0299 ( ...

Abstract	We recently discovered a novel N-aryl tetracyclic dicarboximide MM0299 (
Sprache	Englisch
Erscheinungsdatum	2024-05-28
Erscheinungsland	United States
Dokumenttyp	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.4c00402
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Infection Screening in Biofluids with Glucose Test Strips.

Bekhit, Michael / Wang, Hua-Yu / McHardy, Stanton / Gorski, Waldemar

Analytical chemistry

2020 Band 92, Heft 5, Seite(n) 3860–3866

Abstract: The four glucosyl esters were synthesized and tested for the determination of infection enzyme leukocyte esterase (LE) in human synovial (joint) fluid and urine. The esters acted as LE substrates releasing glucose in a direct proportion to the activity ... ...

Abstract	The four glucosyl esters were synthesized and tested for the determination of infection enzyme leukocyte esterase (LE) in human synovial (joint) fluid and urine. The esters acted as LE substrates releasing glucose in a direct proportion to the activity of LE in a sample. The freed glucose was then detected by a coupled-enzyme assay at either a nitrogen-doped carbon nanotube (N-CNT) electrode or a commercial glucose test strip. The assays at the N-CNT electrode detected LE down to 0.81 nM (25 μg L
Mesh-Begriff(e)	Carboxylic Ester Hydrolases/analysis ; Carboxylic Ester Hydrolases/metabolism ; Carboxylic Ester Hydrolases/urine ; Electrochemical Techniques/instrumentation ; Electrochemical Techniques/methods ; Electrodes ; Glucose/chemistry ; Glucose/metabolism ; Humans ; Kinetics ; Limit of Detection ; Nanotubes, Carbon/chemistry ; Nitrogen/chemistry ; Synovial Fluid/enzymology
Chemische Substanzen	Nanotubes, Carbon ; leukocyte esterase (EC 3.1.-) ; Carboxylic Ester Hydrolases (EC 3.1.1.-) ; Glucose (IY9XDZ35W2) ; Nitrogen (N762921K75)
Sprache	Englisch
Erscheinungsdatum	2020-02-20
Erscheinungsland	United States
Dokumenttyp	Journal Article
ZDB-ID	1508-8
ISSN	1520-6882 ; 0003-2700
ISSN (online)	1520-6882
ISSN	0003-2700
DOI	10.1021/acs.analchem.9b05313
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel: Infection Screening in Biofluids with Glucose Test Strips

Bekhit, Michael / Wang, Hua-Yu / McHardy, Stanton / Gorski, Waldemar

Analytical chemistry. 2020 Feb. 10, v. 92, no. 5

2020

Abstract	The four glucosyl esters were synthesized and tested for the determination of infection enzyme leukocyte esterase (LE) in human synovial (joint) fluid and urine. The esters acted as LE substrates releasing glucose in a direct proportion to the activity of LE in a sample. The freed glucose was then detected by a coupled-enzyme assay at either a nitrogen-doped carbon nanotube (N-CNT) electrode or a commercial glucose test strip. The assays at the N-CNT electrode detected LE down to 0.81 nM (25 μg L–1) and showed the fastest kinetics (2.1 × 105 M–1 s–1) for esters with the least crowded space around their carbonyl group. When used with glucose strips, the esters discerned clinically relevant levels of LE up to at least 26 nM (800 μg L–1) in the microliter-sized samples of bodily fluids. The reading of glucose strips with a potentiostat, instead of a personal glucose meter (blood glucometer), shortened the time of required sample incubation from 3 h to 5 min. Correcting the signal of incubated sample for that of original sample eliminated matrix effects and accounted for the presence of native glucose. The new esters have a potential to extend the use of glucose strips (already used by millions for diabetes monitoring) to the quantification of the severity of urinary tract and periprosthetic joint infections.
Schlagwörter	carbon nanotubes ; diabetes ; electrodes ; esterases ; esters ; glucose ; humans ; leukocytes ; moieties ; monitoring ; screening ; urinary tract ; urine
Sprache	Englisch
Erscheinungsverlauf	2020-0210
Umfang	p. 3860-3866.
Erscheinungsort	American Chemical Society
Dokumenttyp	Artikel
ZDB-ID	1508-8
ISSN	1520-6882 ; 0003-2700
ISSN (online)	1520-6882
ISSN	0003-2700
DOI	10.1021/acs.analchem.9b05313
Datenquelle	NAL Katalog (AGRICOLA)

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Artikel: The Effect of Temperature and Moisture on Colonization of Apple Fruit and Branches by

Liu, Jing / Zhang, Lu-Yao / Wang, Hua-Yu / Liu, Na / Lian, Sen / Xu, Xiang-Ming / Li, Bao-Hua

Phytopathology

2022 Band 112, Heft 8, Seite(n) 1698–1709

Abstract: Botryosphaeria ... ...

Abstract	Botryosphaeria dothidea
Mesh-Begriff(e)	Ascomycota/pathogenicity ; Fruit/microbiology ; Humidity ; Malus/microbiology ; Plant Diseases/microbiology ; Temperature
Sprache	Englisch
Erscheinungsdatum	2022-07-01
Erscheinungsland	United States
Dokumenttyp	Journal Article
ZDB-ID	208889-7
ISSN	1943-7684 ; 0031-949X
ISSN (online)	1943-7684
ISSN	0031-949X
DOI	10.1094/PHYTO-11-21-0487-R
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Modulation of α1β3γ2 GABA

Borghese, Cecilia M / Wang, Hua-Yu L / McHardy, Stanton F / Messing, Robert O / Trudell, James R / Harris, R Adron / Bertaccini, Edward J

Proceedings of the National Academy of Sciences of the United States of America

2021 Band 118, Heft 8

Abstract: Tethered photoswitches are molecules with two photo-dependent isomeric forms, each with different actions on their biological targets. They include reactive chemical groups capable of covalently binding to their target. Our aim was to develop a β-subunit- ...

Abstract	Tethered photoswitches are molecules with two photo-dependent isomeric forms, each with different actions on their biological targets. They include reactive chemical groups capable of covalently binding to their target. Our aim was to develop a β-subunit-tethered propofol photoswitch (MAP20), as a tool to better study the mechanism of anesthesia through the GABA
Mesh-Begriff(e)	Anesthetics, Intravenous/pharmacology ; Animals ; Cell Membrane/drug effects ; Cell Membrane/metabolism ; Cell Membrane/radiation effects ; Humans ; Light ; Oocytes/drug effects ; Oocytes/metabolism ; Oocytes/radiation effects ; Propofol/pharmacology ; Protein Conformation ; Protein Domains ; Receptors, GABA-A/chemistry ; Receptors, GABA-A/drug effects ; Receptors, GABA-A/metabolism ; Receptors, GABA-A/radiation effects ; Xenopus laevis ; gamma-Aminobutyric Acid
Chemische Substanzen	Anesthetics, Intravenous ; Receptors, GABA-A ; gamma-Aminobutyric Acid (56-12-2) ; Propofol (YI7VU623SF)
Sprache	Englisch
Erscheinungsdatum	2021-02-08
Erscheinungsland	United States
Dokumenttyp	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	209104-5
ISSN	1091-6490 ; 0027-8424
ISSN (online)	1091-6490
ISSN	0027-8424
DOI	10.1073/pnas.2008178118
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Selective and brain-penetrant lanosterol synthase inhibitors target glioma stem-like cells by inducing 24(S),25-epoxycholesterol production.

Nguyen, Thu P / Wang, Wentian / Sternisha, Alex C / Corley, Chase D / Wang, Hua-Yu Leo / Wang, Xiaoyu / Ortiz, Francisco / Lim, Sang-Kyun / Abdullah, Kalil G / Parada, Luis F / Williams, Noelle S / McBrayer, Samuel K / McDonald, Jeffrey G / De Brabander, Jef K / Nijhawan, Deepak

Cell chemical biology

2023 Band 30, Heft 2, Seite(n) 214–229.e18

Abstract: Glioblastoma (GBM) is an aggressive adult brain cancer with few treatment options due in part to the challenges of identifying brain-penetrant drugs. Here, we investigated the mechanism of MM0299, a tetracyclic dicarboximide with anti-glioblastoma ... ...

Abstract	Glioblastoma (GBM) is an aggressive adult brain cancer with few treatment options due in part to the challenges of identifying brain-penetrant drugs. Here, we investigated the mechanism of MM0299, a tetracyclic dicarboximide with anti-glioblastoma activity. MM0299 inhibits lanosterol synthase (LSS) and diverts sterol flux away from cholesterol into a "shunt" pathway that culminates in 24(S),25-epoxycholesterol (EPC). EPC synthesis following MM0299 treatment is both necessary and sufficient to block the growth of mouse and human glioma stem-like cells by depleting cellular cholesterol. MM0299 exhibits superior selectivity for LSS over other sterol biosynthetic enzymes. Critical for its application in the brain, we report an MM0299 derivative that is orally bioavailable, brain-penetrant, and induces the production of EPC in orthotopic GBM tumors but not normal mouse brain. These studies have implications for the development of an LSS inhibitor to treat GBM or other neurologic indications.
Mesh-Begriff(e)	Adult ; Humans ; Lanosterol/pharmacology ; Lanosterol/metabolism ; Brain/metabolism ; Glioma/drug therapy ; Glioma/metabolism ; Cholesterol ; Glioblastoma/drug therapy
Chemische Substanzen	lanosterol synthase (EC 5.4.99.7) ; 24,25-epoxycholesterol (68138-65-8) ; Lanosterol (1J05Z83K3M) ; Cholesterol (97C5T2UQ7J)
Sprache	Englisch
Erscheinungsdatum	2023-02-08
Erscheinungsland	United States
Dokumenttyp	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ISSN	2451-9448
ISSN (online)	2451-9448
DOI	10.1016/j.chembiol.2023.01.005
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Noncoupled Fluorescent Assay for Direct Real-Time Monitoring of Nicotinamide N-Methyltransferase Activity.

Neelakantan, Harshini / Vance, Virginia / Wang, Hua-Yu Leo / McHardy, Stanton F / Watowich, Stanley J

Biochemistry

2017 Band 56, Heft 6, Seite(n) 824–832

Abstract: Nicotinamide N-methyltransferase (NNMT) is an important biotransforming enzyme that catalyzes the transfer of a labile methyl group from the ubiquitous cofactor S-5'-adenosyl-l-methionine (SAM) to endogenous and exogenous small molecules to form ... ...

Abstract	Nicotinamide N-methyltransferase (NNMT) is an important biotransforming enzyme that catalyzes the transfer of a labile methyl group from the ubiquitous cofactor S-5'-adenosyl-l-methionine (SAM) to endogenous and exogenous small molecules to form methylated end products. NNMT has been implicated in a number of chronic disease conditions, including metabolic disorders, cardiovascular disease, cancer, osteoarthritis, kidney disease, and Parkinson's disease. We have developed a novel noncoupled fluorescence-based methyltransferase assay that allows direct ultrasensitive real-time detection of the NNMT reaction product 1-methylquinolinium. This is the first assay reported to date to utilize fluorescence spectroscopy to directly monitor NNMT product formation and activity in real time. This assay provided accurate kinetic data that allowed detailed comparative analysis of the NNMT reaction mechanism and kinetic parameters. A reaction model based on a random bireactant mechanism produced global curve fits that were most consistent with steady-state initial velocity data collected across an array of substrate concentrations. On the basis of the reaction mechanism, each substrate could independently bind to the NNMT apoenzyme; however, both substrates bound to the complementary binary complexes with an affinity ∼20-fold stronger compared to their binding to the apoenzyme. This reaction mechanism implies either substrate-induced conformational changes or bireactant intermolecular interactions may stabilize the binding of the substrate to the binary complex and formation of the ternary complex. Importantly, this assay could rapidly generate concentration response curves for known NNMT inhibitors, suggesting its applicability for high-throughput screening of chemical libraries to identify novel NNMT inhibitors. Furthermore, our novel assay potentially offers a robust detection technology for use in SAM substrate competition assays for the discovery and development of SAM-dependent methyltransferase inhibitors.
Mesh-Begriff(e)	Apoenzymes/antagonists & inhibitors ; Apoenzymes/chemistry ; Apoenzymes/genetics ; Apoenzymes/metabolism ; Biocatalysis/drug effects ; Calibration ; Enzyme Inhibitors/pharmacology ; High-Throughput Screening Assays ; Humans ; Limit of Detection ; Methylation/drug effects ; Models, Molecular ; Nicotinamide N-Methyltransferase/antagonists & inhibitors ; Nicotinamide N-Methyltransferase/chemistry ; Nicotinamide N-Methyltransferase/genetics ; Nicotinamide N-Methyltransferase/metabolism ; Protein Conformation ; Protein Refolding/drug effects ; Quinolinium Compounds/metabolism ; Recombinant Proteins/chemistry ; Recombinant Proteins/isolation & purification ; Recombinant Proteins/metabolism ; Reproducibility of Results ; S-Adenosylmethionine/metabolism ; Spectrometry, Fluorescence
Chemische Substanzen	Apoenzymes ; Enzyme Inhibitors ; Quinolinium Compounds ; Recombinant Proteins ; 1-methylquinolinium (21979-19-1) ; S-Adenosylmethionine (7LP2MPO46S) ; NNMT protein, human (EC 2.1.1.1) ; Nicotinamide N-Methyltransferase (EC 2.1.1.1)
Sprache	Englisch
Erscheinungsdatum	2017-02-14
Erscheinungsland	United States
Dokumenttyp	Comparative Study ; Journal Article
ZDB-ID	1108-3
ISSN	1520-4995 ; 0006-2960
ISSN (online)	1520-4995
ISSN	0006-2960
DOI	10.1021/acs.biochem.6b01215
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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Artikel ; Online: Recent advances in acetylcholinesterase Inhibitors and Reactivators: an update on the patent literature (2012-2015).

McHardy, Stanton F / Wang, Hua-Yu Leo / McCowen, Shelby V / Valdez, Matthew C

Expert opinion on therapeutic patents

2017 Band 27, Heft 4, Seite(n) 455–476

Abstract: Introduction: Acetylcholinesterase (AChE) is the major enzyme that hydrolyzes acetylcholine, a key neurotransmitter for synaptic transmission, into acetic acid and choline. Mild inhibition of AChE has been shown to have therapeutic relevance in ... ...

Abstract	Introduction: Acetylcholinesterase (AChE) is the major enzyme that hydrolyzes acetylcholine, a key neurotransmitter for synaptic transmission, into acetic acid and choline. Mild inhibition of AChE has been shown to have therapeutic relevance in Alzheimer's disease (AD), myasthenia gravis, and glaucoma among others. In contrast, strong inhibition of AChE can lead to cholinergic poisoning. To combat this, AChE reactivators have to be developed to remove the offending AChE inhibitor, restoring acetylcholine levels to normal. Areas covered: This article covers recent advances in the development of acetylcholinesterase modulators, including both inhibitors of acetylcholinesterase for the efforts in development of new chemical entities for treatment of AD, as well as re-activators for resurrection of organophosphate bound acetylcholinesterase. Expert opinion: Over the past three years, research efforts have continued to identify novel small molecules as AChE inhibitors for both CNS and peripheral diseases. The more recent patent activity has focused on three AChE ligand design areas: derivatives of known AChE ligands, natural product based scaffolds and multifunctional ligands, all of which have produced some unique chemical matter with AChE inhibition activities in the mid picomolar to low micromolar ranges. New AChE inhibitors with polypharmacology or dual inhibitory activity have also emerged as highlighted by new AChE inhibitors with dual activity at L-type calcium channels, GSK-3, BACE1 and H3, although most only show low micromolar activity, thus further research is warranted. New small molecule reactivators of organophosphate-inhibited AChE have also been disclosed, which focused on the design of neutral ligands with improved pharmaceutical properties and blood-brain barrier (BBB) penetration. Gratifyingly, some research in this area is moving away from the traditional quaternary pyridinium oximes AChE reactivators, while still employing the necessary reactivation group (oximes). However, selectivity over inhibition of native AChE enzyme, effectiveness of reactivation, broad-spectrum reactivation against multiple organophosphates and reactivation of aged-enzyme continue to be hurdles for this area of research.
Mesh-Begriff(e)	Acetylcholinesterase/drug effects ; Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Alzheimer Disease/physiopathology ; Animals ; Cholinesterase Inhibitors/pharmacology ; Cholinesterase Inhibitors/therapeutic use ; Drug Design ; Glaucoma/drug therapy ; Glaucoma/physiopathology ; Humans ; Ligands ; Myasthenia Gravis/drug therapy ; Myasthenia Gravis/physiopathology ; Patents as Topic
Chemische Substanzen	Cholinesterase Inhibitors ; Ligands ; Acetylcholinesterase (EC 3.1.1.7)
Sprache	Englisch
Erscheinungsdatum	2017-04
Erscheinungsland	England
Dokumenttyp	Journal Article ; Review
ZDB-ID	1186201-4
ISSN	1744-7674 ; 0962-2594 ; 1354-3776
ISSN (online)	1744-7674
ISSN	0962-2594 ; 1354-3776
DOI	10.1080/13543776.2017.1272571
Datenquelle	MEDical Literature Analysis and Retrieval System OnLINE

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