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Article ; Online: Antimalarials Targeting the Malaria Parasite Cation ATPase

Zagórska, Agnieszka / Jaromin, Anna

2022 Volume 23, Issue 3, Page(s) 214–226

Abstract: Malaria, caused by parasites of the Plasmodium species and transmitted through the bites of infected female Anopheles mosquitoes, is still a fatal and dangerous disease in mainly tropical and subtropical regions. The widespread resistance of P. ... ...

Abstract	Malaria, caused by parasites of the Plasmodium species and transmitted through the bites of infected female Anopheles mosquitoes, is still a fatal and dangerous disease in mainly tropical and subtropical regions. The widespread resistance of P. falciparum to antimalarial drugs forces the search for new molecules with activity against this parasite. While a large number of compounds can inhibit P. falciparum growth in vitro, unfortunately, only a limited number of targets have been identified so far. One of the most promising approaches has been the identification of effective inhibitors of P-type cation-transporter ATPase 4 (PfATP4) in P. falciparum. PfATP4 is a Na+ efflux pump that maintains a low cytosolic Na+ in the parasite. Thus, upon treatment with PfATP4 inhibitors, the parasites rapidly accumulate Na+, which triggers processes leading to parasite death. PfATP4 is present in the parasite plasma membrane but is absent in mammals; its exclusivity thus makes it a good antimalarial drug target. The current review presents PfATP4 function in the context of the pharmacological influence of its inhibitors. In addition, compounds with inhibitory activities belonging to spiroindolones, dihydroisoquinolones, aminopyrazoles, pyrazoleamides, and 4-cyano-3-methylisoquinolines, are also reviewed. Particular emphasis is placed on the results of preclinical and clinical studies in which their effectiveness was tested. PfATP4-associated antimalarials rapidly cleared parasites in mouse models and preliminary human trials. These findings highlight a fundamental biochemical mechanism sensitive to pharmacological intervention that can form a medicinal chemistry approach for antimalarial drug design to create new molecules with potent PfATP4 inhibitory activity.
MeSH term(s)	Animals ; Mice ; Female ; Humans ; Adenosine Triphosphatases/metabolism ; Antimalarials/chemistry ; Parasites ; Plasmodium falciparum ; Malaria/drug therapy ; Cations/metabolism ; Cations/pharmacology ; Cations/therapeutic use ; Malaria, Falciparum/drug therapy ; Malaria, Falciparum/parasitology ; Mammals/metabolism
Chemical Substances	Adenosine Triphosphatases (EC 3.6.1.-) ; Antimalarials ; Cations
Language	English
Publishing date	2022-12-01
Publishing country	United Arab Emirates
Document type	Review ; Journal Article
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/1568026623666221121154354
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Article ; Online: Polish adaptation of the Inventory of the Dimensions of Emerging Adulthood (IDEA-PL).

Zagórska, Wanda / Skoczeń, Ilona / Lipska, Anna / Arnett, Jeffrey J

Current issues in personality psychology

2023 Volume 11, Issue 3, Page(s) 251–257

Abstract: Background: Emerging adulthood refers to a new phase in life that is related to the transition period from adolescence to adulthood. The concept spread around the world and has been examined in various cultural contexts. This article aims to introduce a ...

Abstract	Background: Emerging adulthood refers to a new phase in life that is related to the transition period from adolescence to adulthood. The concept spread around the world and has been examined in various cultural contexts. This article aims to introduce a Polish adaptation of the Inventory of the Dimensions of Emerging Adulthood (IDEA-PL) developed to assess attitudes toward emerging adulthood among young people. Participants and procedure: In total, 1,414 randomly assigned emerging adults aged between 18 and 29 took part in this study. Participants were asked to describe the extent to which they considered their current life as a time of identity exploration, experimentation/possibilities, negativity/instability, self-focused, feeling in-between, and other-focused. Responses were given on a Likert-type scale ranging from 1 ( Results: The results were analyzed in two steps: via exploratory factor analysis (EFA) to check the underlying structure of the measure and via confirmatory factor analysis (CFA) to assess the model fit. The EFA results showed that the IDEA-PL items loaded onto the originally dedicated six factors; however, some achieved low loadings and/or cross-loadings. In the second step of the analysis, the problematic items were eliminated and the CFA results showed that a five-factor solution with 15 items achieved satisfactory parameters. Conclusions: In this paper, we introduce a Polish adaptation of the Inventory of the Dimensions of Emerging Adulthood (IDEA-PL). These results add value to the existing literature and scholars and clinicians can use this questionnaire for research and practice purposes.
Language	English
Publishing date	2023-03-14
Publishing country	Poland
Document type	Journal Article
ZDB-ID	3030312-6
ISSN	2353-561X ; 2353-4192
ISSN (online)	2353-561X
ISSN	2353-4192
DOI	10.5114/cipp/159277
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Article: Fibrous Structures Produced Using the Solution Blow-Spinning Technique for Advanced Air Filtration Process.

Penconek, Agata / Jackiewicz-Zagórska, Anna / Przekop, Rafał / Moskal, Arkadiusz

Materials (Basel, Switzerland)

2023 Volume 16, Issue 22

Abstract: This study proposes utilising the solution blow-spinning process (SBS) for manufacturing a biodegradable filtration structure that ensures high efficiency of particle filtration with an acceptable pressure drop. The concept of multi-layer filters was ... ...

Abstract	This study proposes utilising the solution blow-spinning process (SBS) for manufacturing a biodegradable filtration structure that ensures high efficiency of particle filtration with an acceptable pressure drop. The concept of multi-layer filters was applied during the design of filters. Polylactic acid (PLA) was used to produce various layers, which may be mixed in different sequences, building structures with varying filtration properties. Changing the process parameters, one can create layers with diverse average fibre diameters and thicknesses. It enables the design and creation of optimal filtration materials prepared for aerosol particle filtration. The structures were numerically modelled using the lattice Boltzmann approach to obtain detailed production guidelines using the blow-spinning technique. The advantage of this method is the ability to blow fibres with diameters in the nanoscale, applying relatively simple and cost-effective equipment. For tested PLA solutions, i.e., 6% and 10%, the mean fibre diameter decreases as the concentration decreases. Therefore, the overall filtering efficiency decreases as the concentration of the used solution increases. The produced multi-layer filters have 96% overall filtration efficiency for particles ranging from 0.26 to 16.60 micrometres with a pressure drop of less than 160 Pa. Obtained results are auspicious and are a step in producing efficient, biodegradable air filters.
Language	English
Publishing date	2023-11-10
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2487261-1
ISSN	1996-1944
ISSN	1996-1944
DOI	10.3390/ma16227118
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Article: Drug Discovery and Development Targeting Dementia.

Zagórska, Agnieszka / Czopek, Anna / Fryc, Monika / Jaromin, Anna / Boyd, Ben J

Pharmaceuticals (Basel, Switzerland)

2023 Volume 16, Issue 2

Abstract: Dementia, most often associated with neurodegenerative diseases, affects millions of people worldwide, predominantly the elderly. Unfortunately, no treatment is still available. Therefore, there is an urgent need to address this situation. This review ... ...

Abstract	Dementia, most often associated with neurodegenerative diseases, affects millions of people worldwide, predominantly the elderly. Unfortunately, no treatment is still available. Therefore, there is an urgent need to address this situation. This review presents the state of the art of drug discovery and developments in targeting dementia. Several approaches are discussed, such as drug repurposing, the use of small molecules, and phosphodiesterase inhibitors. Furthermore, the review also provides insights into clinical trials of these molecules. Emphasis has been placed on small molecules and multi-target-directed ligands, as well as disease-modifying therapies. Finally, attention is drawn to the possibilities of applications of nanotechnology in managing dementia.
Language	English
Publishing date	2023-01-19
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph16020151
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Article ; Online: Perspectives for New and More Efficient Multifunctional Ligands for Alzheimer's Disease Therapy.

Zagórska, Agnieszka / Jaromin, Anna

Molecules (Basel, Switzerland)

2020 Volume 25, Issue 15

Abstract: Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. ...

Abstract	Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. This review analyses the relevance of multiple ligands in drug discovery for AD as a versatile toolbox for a polypharmacological approach to AD. Herein, we highlight major targets associated with AD, ranging from acetylcholine esterase (AChE), beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), glycogen synthase kinase 3 beta (GSK-3β),
MeSH term(s)	Acetylcholinesterase ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Amyloid Precursor Protein Secretases/antagonists & inhibitors ; Aspartic Acid Endopeptidases/antagonists & inhibitors ; Clinical Trials as Topic ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; GPI-Linked Proteins/antagonists & inhibitors ; Glycogen Synthase Kinase 3 beta/antagonists & inhibitors ; Humans ; Ligands ; Molecular Structure ; Monoamine Oxidase/metabolism ; Phosphoric Diester Hydrolases/metabolism ; Polypharmacology ; Receptors, Histamine H3/metabolism ; Receptors, N-Methyl-D-Aspartate/antagonists & inhibitors ; Receptors, Serotonin/metabolism
Chemical Substances	Enzyme Inhibitors ; GPI-Linked Proteins ; Ligands ; Receptors, Histamine H3 ; Receptors, N-Methyl-D-Aspartate ; Receptors, Serotonin ; Monoamine Oxidase (EC 1.4.3.4) ; GSK3B protein, human (EC 2.7.11.1) ; Glycogen Synthase Kinase 3 beta (EC 2.7.11.1) ; ACHE protein, human (EC 3.1.1.7) ; Acetylcholinesterase (EC 3.1.1.7) ; Phosphoric Diester Hydrolases (EC 3.1.4.-) ; Amyloid Precursor Protein Secretases (EC 3.4.-) ; Aspartic Acid Endopeptidases (EC 3.4.23.-) ; BACE1 protein, human (EC 3.4.23.46)
Language	English
Publishing date	2020-07-23
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules25153337
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Article: Influence of Grout Properties on the Tensile Performance of Rockbolts Based on Modified Cable Elements.

Chen, Jianhang / Wang, Shiji / Zhao, Yiqiang / Liu, Lei / Skrzypkowski, Krzysztof / Zagórski, Krzysztof / Zagórska, Anna

Materials (Basel, Switzerland)

2023 Volume 16, Issue 15

Abstract: The grout annulus (GA) has a significant effect on the tensile performance of rockbolts in mining engineering. However, little research has been conducted to use modified cable elements to study this effect quantitatively. This paper used the modified ... ...

Abstract	The grout annulus (GA) has a significant effect on the tensile performance of rockbolts in mining engineering. However, little research has been conducted to use modified cable elements to study this effect quantitatively. This paper used the modified cable elements in FLAC3D to study the effect of the GA on the tensile performance of rockbolts. The two-stage coupling law was used to simulate the behaviour of the GA. The stress had a linear relation with the slippage before the shear strength (SS). After the SS, the stress decreased exponentially. Numerical in situ roadway reinforcement cases were used to study the influence of the grout annulus on the tensile performance of rockbolts. The results showed that, when the SS of the GA increased from 3.2 MPa to 6.4 Mpa, the peak force of rockbolts increased from 247 kN to 425 kN. Moreover, when the SS of the GA increased from 3.2 Mpa to 6.4 Mpa, the distance between the position of the maximum tensile capacity and the external end decreased from 1.17 m to 0.81 m. Last, for the circular roadway, the peak force in rockbolts installed in the lateral side was 171.7 kN, which was significantly larger than the top side of 72.3 kN.
Language	English
Publishing date	2023-07-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2487261-1
ISSN	1996-1944
ISSN	1996-1944
DOI	10.3390/ma16155362
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Article ; Online: Perspectives for New and More Efficient Multifunctional Ligands for Alzheimer′s Disease Therapy

Agnieszka Zagórska / Anna Jaromin

Molecules, Vol 25, Iss 3337, p

2020 Volume 3337

Abstract: Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer′s disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. ...

Abstract	Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer′s disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. This review analyses the relevance of multiple ligands in drug discovery for AD as a versatile toolbox for a polypharmacological approach to AD. Herein, we highlight major targets associated with AD, ranging from acetylcholine esterase (AChE), beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), glycogen synthase kinase 3 beta (GSK-3β), N -methyl- d -aspartate (NMDA) receptor, monoamine oxidases (MAOs), metal ions in the brain, 5-hydroxytryptamine (5-HT) receptors, the third subtype of histamine receptor (H 3 receptor), to phosphodiesterases (PDEs), along with a summary of their respective relationship to the disease network. In addition, a multitarget strategy for AD is presented, based on reported milestones in this area and the recent progress that has been achieved with multitargeted-directed ligands (MTDLs). Finally, the latest publications referencing the enlarged panel of new biological targets for AD related to the microglia are highlighted. However, the question of how to find meaningful combinations of targets for an MTDLs approach remains unanswered.
Keywords	multitarget drug discovery ; MTDLs ; tacrine ; donepezil ; AChE inhibitors ; BACE-1 inhibitors ; Organic chemistry ; QD241-441
Language	English
Publishing date	2020-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis, computational simulations and biological evaluation of new dual 5HT

Zagórska, Agnieszka / Partyka, Anna / Jastrzębska-Więsek, Magdalena / Czopek, Anna / Fryc, Monika / Siwek, Agata / Głuch-Lutwin, Monika / Mordyl, Barbara / Maślanka, Anna / Jaromin, Anna / Kurczab, Rafał

Bioorganic chemistry

2023 Volume 139, Page(s) 106737

Abstract: The new dual ... ...

Abstract	The new dual 5HT
MeSH term(s)	Animals ; Ligands ; Molecular Docking Simulation ; Fluorine ; Antidepressive Agents/pharmacology ; Structure-Activity Relationship ; Purines/chemistry
Chemical Substances	Ligands ; Fluorine (284SYP0193) ; Antidepressive Agents ; Purines
Language	English
Publishing date	2023-07-19
Publishing country	United States
Document type	Journal Article
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2023.106737
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Article: Efficient One-Pot Synthesis of Novel Caffeic Acid Derivatives as Potential Antimalarials.

Sidoryk, Katarzyna / Parapini, Silvia / Basilico, Nicoletta / Zaremba-Czogalla, Magdalena / Kubiszewski, Marek / Cybulski, Marcin / Gubernator, Jerzy / Zagórska, Agnieszka / Jaromin, Anna

Journal of parasitology research

2023 Volume 2023, Page(s) 6675081

Abstract: New protocol for the preparation of the novel caffeic acid derivatives using the Wittig reaction has been applied to follow the principles of green chemistry. The compounds have been evaluated against chloroquine-sensitive and chloroquine- ... ...

Abstract	New protocol for the preparation of the novel caffeic acid derivatives using the Wittig reaction has been applied to follow the principles of green chemistry. The compounds have been evaluated against chloroquine-sensitive and chloroquine-resistant
Language	English
Publishing date	2023-11-24
Publishing country	United States
Document type	Journal Article
ZDB-ID	2563542-6
ISSN	2090-0031 ; 2090-0023
ISSN (online)	2090-0031
ISSN	2090-0023
DOI	10.1155/2023/6675081
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Article ; Online: Assessment of Challenges to the Adoption of IOT for the Safety Management of Small Construction Projects in Malaysia

Ahsan Waqar / Muhammad Basit Khan / Nasir Shafiq / Krzysztof Skrzypkowski / Krzysztof Zagórski / Anna Zagórska

Applied Sciences, Vol 13, Iss 3340, p

Structural Equation Modeling Approach

2023 Volume 3340

Abstract: The Internet of Things is a comprehensive system of connected computing devices and sensors that provide extensive data sharing capability for any specific purpose. For the construction industry, the applications of the Internet of Things have been ... ...

Abstract	The Internet of Things is a comprehensive system of connected computing devices and sensors that provide extensive data sharing capability for any specific purpose. For the construction industry, the applications of the Internet of Things have been increasing over the past few years, and it is because technology can provide full support to construction projects in attaining significant efficiency. The most critical part of construction products where the internet of things can be adopted is safety management because hundreds of accidents happen every year that result in significant injuries to construction workers and even death in some cases. For small construction projects, the situation is much worse, as there are never enough resources to adopt the latest technology, such as the Internet of Things. This study is structured with the aim of identifying the critical implementation barriers of the internet of things that affect small construction projects in Malaysia specifically. A mixed methodology study design is followed in which, after identifying the implementation barriers of the internet of things from existing literature, they are filtered with expert opinion. A pilot survey was conducted on which exploratory factor analysis was applied to further identify the significant barriers relating to the Internet of Things in small construction projects in Malaysia. A main survey was conducted afterwards, on which the structural equation modelling was done to develop the model involving the final 16 barriers divided into 5 formative constructs. The most critical barriers are found to be related to databases and technology, while the least impact is created by management barriers. Positive theoretical and managerial implications are indicated for future researchers and construction workers, respectively, by which they can improve the implementation of internet of things in small construction projects in Malaysia.
Keywords	internet of things (IoT) ; safety management ; small construction projects ; Malaysia ; Technology ; T ; Engineering (General). Civil engineering (General) ; TA1-2040 ; Biology (General) ; QH301-705.5 ; Physics ; QC1-999 ; Chemistry ; QD1-999
Subject code	690
Language	English
Publishing date	2023-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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