Q3056430 (Q3056430): Difference between revisions
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(Created claim: summary (P836): An industrial study is planned. The aim of the project is to develop treonil-tRNA (ThrRS) inhibitors as leading compounds for the detection of antimalarial drugs. Inhibition of ThrRS disrupts protein biosynthesis and can be achieved by inhibitors that bind to the catalytic centre of the enzyme or to the site of borelidine binding. Borelidine is a natural substance that is an active inhibitor of ThrRS and exhibits very high antimalarial activity....) |
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An industrial study is planned. The aim of the project is to develop treonil-tRNA (ThrRS) inhibitors as leading compounds for the detection of antimalarial drugs. Inhibition of ThrRS disrupts protein biosynthesis and can be achieved by inhibitors that bind to the catalytic centre of the enzyme or to the site of borelidine binding. Borelidine is a natural substance that is an active inhibitor of ThrRS and exhibits very high antimalarial activity. Unfortunately, it has low selectivity against human ThrRS and is therefore very toxic. The complex structure and availability of Borelidine is a major barrier to the production of analogues by semi-synthesis or total synthesis, which prevents the necessary properties of the drug from being achieved. As part of this project, it is intended to create synthetic ThrRS inhbitrators, which are borelidine mimetics and show high selectivity in relation to human ThrRS. The instructors are designed to be implemented using modern grass detection approaches such as fragmentary method, virtual high-permeability screening as well as the design of grasses based on structural information. The inhbitors obtained during the liquor detection process are to be further optimised to achieve inhibition of the growth of malaria parasite in cell tests, selectivity to human ThrRS and ADME properties required for grasses. The project will co-operate with specialists in organic chemistry, molecular modelling, biophysical chemistry, stuctural biology and pharmacology. The result is to obtain a series of patentable leading compounds to be used for the development of grasses to treat the rapidly growing resistant malaria. Keywords: Threonil-tRNA synthetase, malaria, grass detection, natural substances, fragment method. The objective of the project shall be consistent with: 1) smart development for “biomedicine, medical technology, biopharmaceutical and biotechnology” and for the “Development and research of new and existing human and veterinary medicines” in the smart specialisation field of biomedicine; 2) RIS3 6. As a priority for growth, by contributing to increasing knowledge and human resources in knowledge-based health and biotechnology. Relevant fields of science: 1.4. Chemical science; 1.3 Physical science; 1.6. Biological science According to NACE clasificators the project will be implemented – 72.1. Research and experimental development in natural sciences and engineering – field.Type of project: Industrial research not related to economic activity Project manager: Dr Aigars Jürgensons Total funding: EUR 648 646,00 ERDF contribution: 374 917.38 EurPlanned activities: 1. Research; 2. Publication of results; 3 Protection of intellectual property Expected results: Anti-malarial leader line series, 3 scientific publications, 1 PCT patent application Duration of the project: 36 monthsStarting date: 1 October 2020 Final date: 30 September 2023 (English) | |||||||||||||||
| Property / summary: An industrial study is planned. The aim of the project is to develop treonil-tRNA (ThrRS) inhibitors as leading compounds for the detection of antimalarial drugs. Inhibition of ThrRS disrupts protein biosynthesis and can be achieved by inhibitors that bind to the catalytic centre of the enzyme or to the site of borelidine binding. Borelidine is a natural substance that is an active inhibitor of ThrRS and exhibits very high antimalarial activity. Unfortunately, it has low selectivity against human ThrRS and is therefore very toxic. The complex structure and availability of Borelidine is a major barrier to the production of analogues by semi-synthesis or total synthesis, which prevents the necessary properties of the drug from being achieved. As part of this project, it is intended to create synthetic ThrRS inhbitrators, which are borelidine mimetics and show high selectivity in relation to human ThrRS. The instructors are designed to be implemented using modern grass detection approaches such as fragmentary method, virtual high-permeability screening as well as the design of grasses based on structural information. The inhbitors obtained during the liquor detection process are to be further optimised to achieve inhibition of the growth of malaria parasite in cell tests, selectivity to human ThrRS and ADME properties required for grasses. The project will co-operate with specialists in organic chemistry, molecular modelling, biophysical chemistry, stuctural biology and pharmacology. The result is to obtain a series of patentable leading compounds to be used for the development of grasses to treat the rapidly growing resistant malaria. Keywords: Threonil-tRNA synthetase, malaria, grass detection, natural substances, fragment method. The objective of the project shall be consistent with: 1) smart development for “biomedicine, medical technology, biopharmaceutical and biotechnology” and for the “Development and research of new and existing human and veterinary medicines” in the smart specialisation field of biomedicine; 2) RIS3 6. As a priority for growth, by contributing to increasing knowledge and human resources in knowledge-based health and biotechnology. Relevant fields of science: 1.4. Chemical science; 1.3 Physical science; 1.6. Biological science According to NACE clasificators the project will be implemented – 72.1. Research and experimental development in natural sciences and engineering – field.Type of project: Industrial research not related to economic activity Project manager: Dr Aigars Jürgensons Total funding: EUR 648 646,00 ERDF contribution: 374 917.38 EurPlanned activities: 1. Research; 2. Publication of results; 3 Protection of intellectual property Expected results: Anti-malarial leader line series, 3 scientific publications, 1 PCT patent application Duration of the project: 36 monthsStarting date: 1 October 2020 Final date: 30 September 2023 (English) / rank | |||||||||||||||
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| Property / summary: An industrial study is planned. The aim of the project is to develop treonil-tRNA (ThrRS) inhibitors as leading compounds for the detection of antimalarial drugs. Inhibition of ThrRS disrupts protein biosynthesis and can be achieved by inhibitors that bind to the catalytic centre of the enzyme or to the site of borelidine binding. Borelidine is a natural substance that is an active inhibitor of ThrRS and exhibits very high antimalarial activity. Unfortunately, it has low selectivity against human ThrRS and is therefore very toxic. The complex structure and availability of Borelidine is a major barrier to the production of analogues by semi-synthesis or total synthesis, which prevents the necessary properties of the drug from being achieved. As part of this project, it is intended to create synthetic ThrRS inhbitrators, which are borelidine mimetics and show high selectivity in relation to human ThrRS. The instructors are designed to be implemented using modern grass detection approaches such as fragmentary method, virtual high-permeability screening as well as the design of grasses based on structural information. The inhbitors obtained during the liquor detection process are to be further optimised to achieve inhibition of the growth of malaria parasite in cell tests, selectivity to human ThrRS and ADME properties required for grasses. The project will co-operate with specialists in organic chemistry, molecular modelling, biophysical chemistry, stuctural biology and pharmacology. The result is to obtain a series of patentable leading compounds to be used for the development of grasses to treat the rapidly growing resistant malaria. Keywords: Threonil-tRNA synthetase, malaria, grass detection, natural substances, fragment method. The objective of the project shall be consistent with: 1) smart development for “biomedicine, medical technology, biopharmaceutical and biotechnology” and for the “Development and research of new and existing human and veterinary medicines” in the smart specialisation field of biomedicine; 2) RIS3 6. As a priority for growth, by contributing to increasing knowledge and human resources in knowledge-based health and biotechnology. Relevant fields of science: 1.4. Chemical science; 1.3 Physical science; 1.6. Biological science According to NACE clasificators the project will be implemented – 72.1. Research and experimental development in natural sciences and engineering – field.Type of project: Industrial research not related to economic activity Project manager: Dr Aigars Jürgensons Total funding: EUR 648 646,00 ERDF contribution: 374 917.38 EurPlanned activities: 1. Research; 2. Publication of results; 3 Protection of intellectual property Expected results: Anti-malarial leader line series, 3 scientific publications, 1 PCT patent application Duration of the project: 36 monthsStarting date: 1 October 2020 Final date: 30 September 2023 (English) / qualifier | |||||||||||||||
point in time: 15 July 2021
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Revision as of 12:34, 15 July 2021
Project Q3056430 in Latvia
| Language | Label | Description | Also known as |
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| English | No label defined |
Project Q3056430 in Latvia |
Statements
374,917.38 Euro
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648,646.0 Euro
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1 October 2020
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30 September 2023
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Atvasināta publiska persona "Latvijas Organiskās sintēzes institūts"
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56°58'34.79"N, 24°11'29.72"E
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Plānots rūpnieciskais pētījums. Projekta mērķis ir izveidot treonil-tRNS (ThrRS) inhibitorus kā līdersavienojumus pretmalārijas zāļvielu atklāšanai. ThrRS inhibīcija izjauc proteīnu biosintēzi, un to var panākt ar inhibitoriem, kas saistās enzīma katalītiskajā centrā vai borelidīna saistīšanās vietā. Borelidīns ir dabasviela, kas ir aktīvs ThrRS inhibitors un uzrāda ļoti augstu pretmalārijas aktvitāti. Diemžēl tam piemīt zema selektivitāte attiecībā pret cilvēka ThrRS un tādēļ tas ir ļoti toksisks. Borelidīna sarežģītā struktūra un pieejamība ir būtisks šķērslis tā analogu iegūšanai semi-sintēzes vai totālās sintēzes ceļā, kas kavē sasniegt zāļvielai nepieciešamās īpašības. Šī projekta ietvaros ir paredzēts izveidot sintētiskos ThrRS inhbitorus, kas ir borelidīna mimētiķi un uzrāda augstu selektivitāti attiecība pret cilvēka ThrRS. Inhbitoru izveidi paredzēts realizēt, izmantojot mūsdienīgas zāļvielu atklāšanas pieejas tādas kā fragmentu metodi, virtuālo augstas caurlaidības skrīningu kā arī zāļvielu dizainu balstoties uz strukturālo informāciju. Līdersavienojuma atklāšanas procesā iegūtos inhbitorus paredzēts tālāk optimizēt, lai sasniegtu malārijas parazīta augšanas inhibīciju šūnu testos, selektivitāti attiecība pret cilvēka ThrRS un zāļvielām nepieciešamās ADME īpašības. Projektā sadarbosies organiskās ķīmijas, molekulārās modelēšanas, biofizikālās ķīmijas, stukturālās bioloģijas un farmakoloģijas speciālisti. Rezultātā paredzēts iegūt patentējamu līdersavienojumu sēriju, kas izmantojama zāļvielu izveidei, lai ārstētu strauji pieaugošo rezistento malāriju. Atslēgas vārdi: threonil-tRNS sintetāze, malārija, zāļvielu atklāšana, dabasvielas, fragmentu metode. Projekta mērķis atbilst: 1) viedās attīstības jomai „biomedicīna, medicīnas tehnoloģija, biofarmācija un biotehnoloģija” un biomedicīnas viedās specializācijas nišai “ Jaunu un esošo humāno un veterināro zāļu izstrāde un izpēte”; 2) RIS3 6. Izaugsmes prioritātei, sniedzot ieguldījumu zināšanu un cilvēkresursu palielināšanā zināšanu balstītas veselības un biotehnoloģijas jomās. Atbilstošās zinātnes nozares: 1.4. Ķīmijas zinātne; 1.3 Fizikas zinātne; 1.6. Bioloģijas zinātneSaskaņā ar NACE klsifikatoru projekts tiks īstenots - 72.1. Pētījumu un eksperimentālo izstrāžu veikšana dabaszinātnēs un inženierzinātnēs - jomā.Projekta veids: Ar saimniecisko darbību nesaistīts industriālais pētijumsProjekta vadītājs: Dr. Aigars JirgensonsKopējais finansējums: 648 646,00 Eur. ERAF finansējums: 374 917.38 EurPlānotās aktivitātes: 1. Pētniecība; 2. Rezultātu publicēšana; 3 Intelektuālā īpašuma aizsardzībaParedzamie rezultāti: Pret-malārijas līdersavienojumu sērija, 3 zinātniskās publikācijas, 1 PCT patenta pieteikums Projekta ilgums: 36 mēnešiUzsākšanas datums: 2020. gada 1. oktobrisBeigu datums: 2023. gada 30. septembris (Latvian)
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An industrial study is planned. The aim of the project is to develop treonil-tRNA (ThrRS) inhibitors as leading compounds for the detection of antimalarial drugs. Inhibition of ThrRS disrupts protein biosynthesis and can be achieved by inhibitors that bind to the catalytic centre of the enzyme or to the site of borelidine binding. Borelidine is a natural substance that is an active inhibitor of ThrRS and exhibits very high antimalarial activity. Unfortunately, it has low selectivity against human ThrRS and is therefore very toxic. The complex structure and availability of Borelidine is a major barrier to the production of analogues by semi-synthesis or total synthesis, which prevents the necessary properties of the drug from being achieved. As part of this project, it is intended to create synthetic ThrRS inhbitrators, which are borelidine mimetics and show high selectivity in relation to human ThrRS. The instructors are designed to be implemented using modern grass detection approaches such as fragmentary method, virtual high-permeability screening as well as the design of grasses based on structural information. The inhbitors obtained during the liquor detection process are to be further optimised to achieve inhibition of the growth of malaria parasite in cell tests, selectivity to human ThrRS and ADME properties required for grasses. The project will co-operate with specialists in organic chemistry, molecular modelling, biophysical chemistry, stuctural biology and pharmacology. The result is to obtain a series of patentable leading compounds to be used for the development of grasses to treat the rapidly growing resistant malaria. Keywords: Threonil-tRNA synthetase, malaria, grass detection, natural substances, fragment method. The objective of the project shall be consistent with: 1) smart development for “biomedicine, medical technology, biopharmaceutical and biotechnology” and for the “Development and research of new and existing human and veterinary medicines” in the smart specialisation field of biomedicine; 2) RIS3 6. As a priority for growth, by contributing to increasing knowledge and human resources in knowledge-based health and biotechnology. Relevant fields of science: 1.4. Chemical science; 1.3 Physical science; 1.6. Biological science According to NACE clasificators the project will be implemented – 72.1. Research and experimental development in natural sciences and engineering – field.Type of project: Industrial research not related to economic activity Project manager: Dr Aigars Jürgensons Total funding: EUR 648 646,00 ERDF contribution: 374 917.38 EurPlanned activities: 1. Research; 2. Publication of results; 3 Protection of intellectual property Expected results: Anti-malarial leader line series, 3 scientific publications, 1 PCT patent application Duration of the project: 36 monthsStarting date: 1 October 2020 Final date: 30 September 2023 (English)
15 July 2021
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Aizkraukles iela 21, Rīga, LV-1006
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Identifiers
1.1.1.1/19/A/019
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