Potential drugs

Acetylcholinesterase (AChE) has been one of the important and potential targets in the discovery, and development of new drugs for treating and slowing the progression of Alzheimer's disease (AD). This research suggests potential structural frameworks for synthesizing AChE inhibitor derivatives for treating AD.

11p vihyuga 04-03-2025 0 0   Download

Acetylcholinesterase (AChE) is a key therapeutic target for developing new Alzheimer's disease (AD) treatments due to its regulatory function in acetylcholine hydrolysis. This research contributed to the development of a novel scaffold for AChE inhibitors, which are potential drugs for treating AD.

17p vihyuga 04-03-2025 0 0   Download

The nasal route for drug administration has the potential for local and systemic delivery of a wide variety of therapeutics. Nasal spray drug delivery has the potential to administer drugs to the bloodstream, avoiding the use of painful needles. While there is great potential, studies in the area are limited and somewhat conflicting. This study aimed to support the improvement of nasal drug delivery through experimental work on a model nasal cavity and through experimental characterisation of nasal spray behaviour. Four different brands of nasal spray were investigated.

91p runthenight04 02-02-2023 13 3   Download

The nasal route for drug administration has the potential for local and systemic delivery of a wide variety of therapeutics. Nasal spray drug delivery has the potential to administer drugs to the bloodstream, avoiding the use of painful needles. While there is great potential, studies in the area are limited and somewhat conflicting. The thesis "Experimental Studies in Aid of Improving Nasal Drug Delivery" aimed to support the improvement of nasal drug delivery through experimental work on a model nasal cavity and through experimental characterisation of nasal spray behaviour.

91p runordie3 06-07-2022 8 3   Download

Preliminary experiments shows, that [3+2] cycloadditions reactions proceeds with full regioselectivity and high stereoselectivity. In consequence, 3,4-trans-2-methyl-3-(3,4,5-trimethoxyphenyl)-4-halo-4-nitroisoxazolidines are forming as predominantly (or sole) products. Additionally, prognosis for the synthesized compounds to be potential ingredients of drugs is good.

6p tocectocec 26-05-2020 24 2   Download

Regulator of G-protein signaling (RGS) proteins were originally identified as negative regulators of G-protein-coupled receptor (GPCR) signaling via their GTPase-accelerating protein (GAP) activity. All RGS proteins contain evolutionarily conserved RGS domain; however, they differ in their size and regulatory domains. RGS1 and RGS10 are smaller than other RGS proteins, and their functions involve various inflammatory responses including autoimmune responses in both the periphery and the central nervous system (CNS). Neuroinflammation is the chronic inflammatory response in the CNS.

5p caothientrangnguyen 09-05-2020 30 2   Download

Biotherapeutics (BTs), one of the fastest growing classes of drug molecules, offer several advantages over the traditional small molecule pharmaceuticals because of their relatively high specificity, low off-target effects, and biocompatible metabolism, in addition to legal and logistic advantages. However, their clinical utility is limited, among other things, by their high immunogenic potential and/or variable therapeutic efficacy in different patient populations.

7p caothientrangnguyen 09-05-2020 27 1   Download

The objectives of the thesis: Molecular docking studies on acetylcholinesterase were performed to predict the chalcone structure has good in silico AChE acetylcholinesterase inhibitory activity. The potential chalcone compounds were synthesized and studied for their in vitro and in vivo AChE inhibitory activities

25p xacxuoc4321 09-07-2019 43 7   Download

Liver microsomal preparations are routinely used to predict drug interactions that can occurin vivo as a result of inhi-bition of cytochrome P450 (CYP)-mediated metabolism. However, the concentration of free drug (substrate and inhibitor)at its intrahepatic site of action, a variable that cannot be directly measured, may be significantly different from that in microsomal incubation systems.

10p tumor12 20-04-2013 48 4   Download

The Hsp90 molecular chaperone catalyses the final activa-tion step of many of themost important regulatory proteins of eukaryotic cells. The antibiotics geldanamycin and rad-icicol act as highly selective inhibitors of in vivo Hsp90 function through their ability to bindwithin the ADP/ATP binding pocket of the chaperone. Drugs based on these compounds are now being developed as anticancer agents, their administration having the potential to inactivate sim-ultaneously several of the targets critical for counteracting multistep carcinogenesis. ...

7p fptmusic 12-04-2013 45 3   Download

The transient receptor potential channel vanilloid receptor subunit 1 (TRPV1) is amolecular integrator of physical and chemical stimuli in the peripheral nociceptor terminals. TRPV1 is an ionotropic channel that plays a critical role in both thermal nociception and inflammatoryhyperalgesia. Structure–function relationships are providing fundamental insights of the modular architecture of this neuronal recep-tor.

7p dell39 03-04-2013 49 3   Download

Onconase, a member of the ribonuclease superfamily, is a potent cytotoxicagent that isundergoingphase II/IIIhuman clinical trials as an antitumor drug. Native onconase from Rana pipiensand its amphibian homologs have an N-ter-minal pyroglutamyl residue that is essential for obtaining fully active enzymes with their full potential as cytotoxins. When expressed cytosolically in bacteria, Onconase is isolated with an additional methionyl (Met1) residue and glutaminyl insteadof a pyroglutamyl residue at position 1 of the N-terminus and is consequently inactivated....

9p dell39 03-04-2013 34 4   Download

Cyclic nucleotide specific phosphodiesterases (PDEs) are important components of all cAMP signalling networks. In humans, 11 different PDE families have been identified to date, all of which belong to the class I PDEs. Pharmaco-logically, theyhavebecome of great interest as targets for the development of drugs for a large variety of clinical condi-tions. PDEs in parasitic protozoa have not yet been exten-sively investigated, despite their potential as antiparasitic drug targets.

11p dell39 03-04-2013 42 4   Download

Hexameric DnaB helicase unwinds the DNA double helix during replica-tion of genetic material in bacteria. DnaB is an essential bacterial protein; therefore, it is an important potential target for antibacterial drug disco-very. We report a crystal structure of the N-terminal region of DnaB from the pathogen Mycobacterium tuberculosis(MtDnaBn), determined at 2.0 A˚ resolution.

8p galaxyss3 07-03-2013 50 4   Download

6-Phosphogluconate dehydrogenase is a potential target for new drugs against African trypanosomiasis. Phosphorylated aldonic acids are strong inhibitors of 6-phosphogluconate dehydrogenase, and 4-phospho-d-erythro-nate (4PE) and 4-phospho-d-erythronohydroxamate are two of the stron-gest inhibitors of theTrypanosoma bruceienzyme.

10p media19 05-03-2013 37 3   Download

The crystal structure of uridine monophosphate kinase (UMP kinase, UMPK) from the opportunistic pathogenUreaplasma parvumwas deter-mined and showed similar three-dimensional fold as other bacterial and archaeal UMPKs that all belong to the amino acid kinase family.

12p media19 05-03-2013 37 3   Download

The genome ofLeishmania major, the causative agent of cutaneous leish-maniasis, contains three almost identical genes encoding putative glutathi-one peroxidases, which differ only at their N- and C-termini. Because the gene homologues are essential in trypanosomes, they may also represent potential drug targets inLeishmania.

16p media19 04-03-2013 38 1   Download

Human P-glycoprotein is an ATP-binding cassette transporter that plays an important role in the defence against potentially harmful molecules from the environment. It is involved in conferring resistance against cancer therapeutics and plays an important role for the pharmacokinetics of drugs.

10p vinaphone15 27-02-2013 22 3   Download

ArylamineN-acetyltransferases (NATs) play an important role in both the detoxification of arylamine and hydrazine drugs and the activation of aryl-amine carcinogens. Because the catalytic triad, Cys-His-Asp, of mammalian NATs has been shown to be essential for maintaining protein stability, ren-dering it impossible to assess alterations of the triad on catalysis, we explored the impact of the highly conserved proximal residue

14p viettel02 20-02-2013 40 3   Download

The ever-increasing number of drug-resistant bacteria is a major challenge in healthcare and creates an urgent need for novel compounds for treat-ment. Host defense antimicrobial peptides have high potential to become the new generation of antibiotic compounds. Antimicrobial peptides consti-tute a major part of the innate defense system in all life forms.

9p viettel02 20-02-2013 47 3   Download