Acetylcholinesterase and ATPases: targets of biologically active compounds
Само за регистроване кориснике
Конференцијски прилог (Објављена верзија)
Метаподаци
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Acetylcholinesterase is a serine hydrolase whose key biological role is the termination of impulse transmission at cholinergic synapses by rapid hydrolysis of the neurotransmitter acetylcholine. The reversible inhibition of brain acetylcholinesterase is the major therapeutic target in the treatment of Alzheimer’s disease associated with loss of cholinergic neurons in the brain and the decreased level of acetylcholine, whereas toxic effects are related to irreversible modulators of the enzyme activity. Na+/K+-ATPase is a transmembrane protein regulating many cellular functions, involving those associated with tumor cell growth. In addition, particular Na+/K+-ATPase subunits are expressed in some cancer cells and changes in Na+/K+-ATPase activity and relative subunit abundance were detected in various carcinoma cell lines. Accordingly, design and synthesis of novel compounds have been directed towards new modulators of Na+/K+-ATPase, which selectively target these cellular abnormalities.... Ecto-nucleoside triphosphate diphosphohydrolases (ENTPDases) are plasma membrane bound enzymes representing the major part of purinergic signaling. Increased E-NTPDases levels were observed in cancer cells due to their abnormal cellular growth and proliferation. Accordingly, the decrease of E-NTPDase activity could be regarded as a new approach in the development of antitumor drugs. This presentation will be focused on metal-based compounds such as polyoxometalates which are discrete, negatively charged metal-oxo clusters of early d-block metal ions in high oxidation states, surrounded by oxygen atoms. These compounds were approved to exhibit a variety of biological actions such as anticancer, antimicrobial and antidiabetic properties. However, the mechanism of their bioactivities has not been completely understood yet. It has been assumed that polyoxometalates interact with different enzyme families extracellularly located on the plasma membrane such as phosphatases and ecto-nucleotidases. This presentation will primarily be directed to acetylcholinesterase, Na+/K+-ATPase and E-NTPDases as potential targets of polyoxometalate pharmacological and toxicological activities.
Извор:
7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts, 2022, 14-14Напомена:
- PDSS 2022 : Virtual event : September 8-9, 2022, Paris, France.
Колекције
Институција/група
VinčaTY - CONF AU - Čolović, Mirjana PY - 2022 UR - https://vinar.vin.bg.ac.rs/handle/123456789/12922 AB - Acetylcholinesterase is a serine hydrolase whose key biological role is the termination of impulse transmission at cholinergic synapses by rapid hydrolysis of the neurotransmitter acetylcholine. The reversible inhibition of brain acetylcholinesterase is the major therapeutic target in the treatment of Alzheimer’s disease associated with loss of cholinergic neurons in the brain and the decreased level of acetylcholine, whereas toxic effects are related to irreversible modulators of the enzyme activity. Na+/K+-ATPase is a transmembrane protein regulating many cellular functions, involving those associated with tumor cell growth. In addition, particular Na+/K+-ATPase subunits are expressed in some cancer cells and changes in Na+/K+-ATPase activity and relative subunit abundance were detected in various carcinoma cell lines. Accordingly, design and synthesis of novel compounds have been directed towards new modulators of Na+/K+-ATPase, which selectively target these cellular abnormalities. Ecto-nucleoside triphosphate diphosphohydrolases (ENTPDases) are plasma membrane bound enzymes representing the major part of purinergic signaling. Increased E-NTPDases levels were observed in cancer cells due to their abnormal cellular growth and proliferation. Accordingly, the decrease of E-NTPDase activity could be regarded as a new approach in the development of antitumor drugs. This presentation will be focused on metal-based compounds such as polyoxometalates which are discrete, negatively charged metal-oxo clusters of early d-block metal ions in high oxidation states, surrounded by oxygen atoms. These compounds were approved to exhibit a variety of biological actions such as anticancer, antimicrobial and antidiabetic properties. However, the mechanism of their bioactivities has not been completely understood yet. It has been assumed that polyoxometalates interact with different enzyme families extracellularly located on the plasma membrane such as phosphatases and ecto-nucleotidases. This presentation will primarily be directed to acetylcholinesterase, Na+/K+-ATPase and E-NTPDases as potential targets of polyoxometalate pharmacological and toxicological activities. C3 - 7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts T1 - Acetylcholinesterase and ATPases: targets of biologically active compounds SP - 14 EP - 14 UR - https://hdl.handle.net/21.15107/rcub_vinar_12922 ER -
@conference{ author = "Čolović, Mirjana", year = "2022", abstract = "Acetylcholinesterase is a serine hydrolase whose key biological role is the termination of impulse transmission at cholinergic synapses by rapid hydrolysis of the neurotransmitter acetylcholine. The reversible inhibition of brain acetylcholinesterase is the major therapeutic target in the treatment of Alzheimer’s disease associated with loss of cholinergic neurons in the brain and the decreased level of acetylcholine, whereas toxic effects are related to irreversible modulators of the enzyme activity. Na+/K+-ATPase is a transmembrane protein regulating many cellular functions, involving those associated with tumor cell growth. In addition, particular Na+/K+-ATPase subunits are expressed in some cancer cells and changes in Na+/K+-ATPase activity and relative subunit abundance were detected in various carcinoma cell lines. Accordingly, design and synthesis of novel compounds have been directed towards new modulators of Na+/K+-ATPase, which selectively target these cellular abnormalities. Ecto-nucleoside triphosphate diphosphohydrolases (ENTPDases) are plasma membrane bound enzymes representing the major part of purinergic signaling. Increased E-NTPDases levels were observed in cancer cells due to their abnormal cellular growth and proliferation. Accordingly, the decrease of E-NTPDase activity could be regarded as a new approach in the development of antitumor drugs. This presentation will be focused on metal-based compounds such as polyoxometalates which are discrete, negatively charged metal-oxo clusters of early d-block metal ions in high oxidation states, surrounded by oxygen atoms. These compounds were approved to exhibit a variety of biological actions such as anticancer, antimicrobial and antidiabetic properties. However, the mechanism of their bioactivities has not been completely understood yet. It has been assumed that polyoxometalates interact with different enzyme families extracellularly located on the plasma membrane such as phosphatases and ecto-nucleotidases. This presentation will primarily be directed to acetylcholinesterase, Na+/K+-ATPase and E-NTPDases as potential targets of polyoxometalate pharmacological and toxicological activities.", journal = "7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts", title = "Acetylcholinesterase and ATPases: targets of biologically active compounds", pages = "14-14", url = "https://hdl.handle.net/21.15107/rcub_vinar_12922" }
Čolović, M.. (2022). Acetylcholinesterase and ATPases: targets of biologically active compounds. in 7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts, 14-14. https://hdl.handle.net/21.15107/rcub_vinar_12922
Čolović M. Acetylcholinesterase and ATPases: targets of biologically active compounds. in 7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts. 2022;:14-14. https://hdl.handle.net/21.15107/rcub_vinar_12922 .
Čolović, Mirjana, "Acetylcholinesterase and ATPases: targets of biologically active compounds" in 7th Edition of Global Conference on Pharmaceutics and Novel Drug Delivery Systems : PDSS 2022 : Book of abstracts (2022):14-14, https://hdl.handle.net/21.15107/rcub_vinar_12922 .