The Experts below are selected from a list of 306 Experts worldwide ranked by ideXlab platform
Francisca Vicente - One of the best experts on this subject based on the ideXlab platform.
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discovery and antibacterial activity of glabramycin a c from neosartorya glabra by an Antisense Strategy
The Journal of Antibiotics, 2009Co-Authors: Hiranthi Jayasuriya, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, Mary Lee Goldman, Mary Motyl, Gabe DezenyAbstract:Treatment of drug-resistant bacteria is a significant unmet medical need. This challenge can be met only by the discovery and development of new antibiotics. Antisense technology is one of the newest discovery tools that provides enhanced sensitivity for detection of antibacterials, and has led to the discovery of a number of interesting new antibacterial natural products. Continued utilization of this technology led to the discovery of three new bicyclic lactones, glabramycins A–C, from a Neosartorya glabra strain. Glabramycin C showed strong antibiotic activity against Streptococcus pneumoniae (MIC 2 μg ml−1) and modest antibiotic activity against Staphylococcus aureus (MIC 16 μg ml−1). The isolation, structure, relative configuration and antibacterial activity, and plausible biogenesis of these compounds have been discussed.
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Discovery and antibacterial activity of glabramycin A–C from Neosartorya glabra by an Antisense Strategy
The Journal of Antibiotics, 2009Co-Authors: Hiranthi Jayasuriya, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, Mary Lee Goldman, Mary Motyl, Gabe DezenyAbstract:Treatment of drug-resistant bacteria is a significant unmet medical need. This challenge can be met only by the discovery and development of new antibiotics. Antisense technology is one of the newest discovery tools that provides enhanced sensitivity for detection of antibacterials, and has led to the discovery of a number of interesting new antibacterial natural products. Continued utilization of this technology led to the discovery of three new bicyclic lactones, glabramycins A–C, from a Neosartorya glabra strain. Glabramycin C showed strong antibiotic activity against Streptococcus pneumoniae (MIC 2 μg ml−1) and modest antibiotic activity against Staphylococcus aureus (MIC 16 μg ml−1). The isolation, structure, relative configuration and antibacterial activity, and plausible biogenesis of these compounds have been discussed.
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isolation structure and antibacterial activities of lucensimycins d g discovered from streptomyces lucensis ma7349 using an Antisense Strategy
Journal of Natural Products, 2009Co-Authors: Suresh B Singh, Deborah L Zink, Oscar Salazar, Angela Basilio, Francisca Vicente, Kevin M Byrne, Mary Motyl, Karen Dorso, Sookhee Ha, Olga GenilloudAbstract:Bacterial resistance to existing antibiotics continues to grow, necessitating the discovery of new compounds of this type. Antisense-based whole-cell target-based screening is a new and highly sens...
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isolation structure and antibacterial activity of pleosporone from a pleosporalean ascomycete discovered by using Antisense Strategy
Bioorganic & Medicinal Chemistry, 2009Co-Authors: Chaowei Zhang, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, John G Ondeyka, Gonzalo Platas, Karen Dorso, Mary MotylAbstract:Abstract Protein synthesis is one of the best antibacterial targets that have led to the development of a number of highly successful clinical drugs. Protein synthesis is catalyzed by ribosome, which is comprised of a number of ribosomal proteins that help the catalysis process. Ribosomal protein S4 (RPSD) is one of the proteins that is a part of the ribosomal machinery and is a potential new target for the discovery of antibacterial agents. Screening of microbial extracts using Antisense-sensitized rpsD Staphylococcus aureus strain led to the isolation of pleosporone, a new compound, with modest antibacterial activities with MIC ranging from 1 to 64 μg/mL. This compound showed the highest sensitivity for Streptococcus pneumoniae and Haemophilus influenzae , and exhibited MIC’s of 4 and 1 μg/mL, respectively. Pleosporone showed modest selectivity for the inhibition of RNA synthesis compared to DNA and protein synthesis, and showed activity against HeLa cells. Isolation, structure elucidation, and biological activity of pleosporone have been described.
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isolation structure and antibacterial activity of phaeosphenone from a phaeosphaeria sp discovered by Antisense Strategy
Journal of Natural Products, 2008Co-Authors: Chaowei Zhang, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, John G Ondeyka, Gonzalo Platas, Karen DorsoAbstract:Ribosomal protein S4 (RPSD), a part of the ribosomal small subunit, is one of the proteins that is a part of the ribosomal machinery and is a potential new target for the discovery of antibacterial agents. Continued screening of microbial extracts using Antisense-sensitized rpsD Staphylococcus aureus strain led to the isolation of a new dimeric compound, phaeosphenone (2). Compound 2 showed broad-spectrum antibacterial activity against Gram-positive bacteria, exhibiting MIC values ranging from 8 to 64 μg/mL. Phaeosphenone showed the highest sensitivity for Streptococcus pneumoniae (8 μg/mL) and inhibited the growth of Candida albicans with an MIC of 8 μg/mL. Phaeosphenone showed a modest selectivity for the inhibition of RNA synthesis over DNA and protein synthesis in S. aureus.
Kevin M Byrne - One of the best experts on this subject based on the ideXlab platform.
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isolation structure and antibacterial activities of lucensimycins d g discovered from streptomyces lucensis ma7349 using an Antisense Strategy
Journal of Natural Products, 2009Co-Authors: Suresh B Singh, Deborah L Zink, Oscar Salazar, Angela Basilio, Francisca Vicente, Kevin M Byrne, Mary Motyl, Karen Dorso, Sookhee Ha, Olga GenilloudAbstract:Bacterial resistance to existing antibiotics continues to grow, necessitating the discovery of new compounds of this type. Antisense-based whole-cell target-based screening is a new and highly sens...
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discovery of lucensimycins a and b from streptomyces lucensis ma7349 using an Antisense Strategy
Organic Letters, 2006Co-Authors: Suresh B Singh, Deborah L Zink, Joann Huber, Olga Genilloud, Oscar Salazar, Maria Teresa Diez, Angela Basilio, Francisca Vicente, Kevin M ByrneAbstract:Inhibition of protein synthesis is one of the validated and highly successful targets for inhibition of bacterial growth; this mechanism is a target of a large number of clinical drugs. Ribosomal protein S4, a primary protein, is a potential target for the discovery of antibacterial agents. We describe, using an Antisense-sensitized rpsD Streptomyces aureus strain, the discovery and activity of lucensimycins A and B.
Tangui Maurice - One of the best experts on this subject based on the ideXlab platform.
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differential involvement of the sigma1 σ1 receptor in the anti amnesic effect of neuroactive steroids as demonstrated using an in vivo Antisense Strategy in the mouse
British Journal of Pharmacology, 2001Co-Authors: Tangui Maurice, Vânly Phan, Alexandre Urani, Isabelle GuillemainAbstract:The sigma1 (σ1) receptor cDNA was cloned in several animal species. Molecular tools are now available to identify its endogenous effectors, such as neuroactive steroids, and to establish its precise physiological role. In particular, the σ1 receptor is involved in memory processes, as observed in pharmacological and pathological rodent models of amnesia. In order to establish the involvement of σ1 receptors in memory, a 16-mer oligodeoxynucleotide Antisense to the σ1 receptor cDNA (aODN), and its mismatched control (mODN) were prepared and centrally administered into the mouse brain. The anti-amnesic effects induced by the selective σ1 agonist PRE-084 and the steroid dehydroepiandrosterone (DHEA) sulphate or pregnenolone sulphate were examined in ODN-treated animals. The aODN treatment failed to affect the dissociation constant (Kd) but significantly decreased the number of σ1 sites (Bmax) labelled with [3H]-(+)-SKF-10,047 in the hippocampus and cortex. In these structures, the in vivo binding levels were also diminished, according to the dose and number of injections, as compared with control animals injected with saline or mODN. Cannulation and injections failed to affect the open-field behaviour of the animals. However, the anti-amnesic effects of PRE-084 and DHEA sulphate against the dizocilpine-induced impairments were blocked after aODN treatment in the short- and long-term memory tests. The anti-amnesic effects of pregnenolone sulphate remained unchanged. These observations bring a molecular basis to the modulatory role of σ1 receptors in memory, and reveal that the anti-amnesic action of neuroactive steroids may not similarly involve an interaction with σ1 receptors. British Journal of Pharmacology (2001) 134, 1731–1741; doi:10.1038/sj.bjp.0704355
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the anti amnesic effects of sigma1 σ1 receptor agonists confirmed by in vivo Antisense Strategy in the mouse
Brain Research, 2001Co-Authors: Tangui Maurice, Vânly Phan, Alain PrivatAbstract:Abstract The sigma 1 ( σ 1 ) receptor cDNA was recently cloned in several animal species, including the mouse. In order to firmly establish the implication of σ 1 receptors in memory, a phosphorothioate-modified Antisense oligodeoxynucleotide (aODN) targeting the σ 1 receptor mRNA and a mismatched analog (mODN) were administered intracerebroventricularly for 3 days in mice. Scatchard analyses of in vitro (+)-[ 3 H]SKF-10,047 binding to σ 1 sites showed that B max values were significantly decreased in the hippocampus (−58.5%) and cortex (−38.1%), but not in the cerebellum, of aODN treated mice, as compared to saline- or mODN-treated animals. In vivo binding levels were also significantly decreased after aODN treatment in the hippocampus and cortex but not in the cerebellum. The anti-amnesic effects of the selective σ 1 agonists PRE-084 or SA4503 were evaluated against the learning impairments induced by dizocilpine or scopolamine, respectively, using spontaneous alternation behavior and passive avoidance task. The anti-amnesic effects of PRE-084 or SA4503, observed after saline- or mODN-treatment, were blocked after aODN administration. These observations bring a molecular basis to the modulatory role of σ 1 receptors in memory processes.
Olga Genilloud - One of the best experts on this subject based on the ideXlab platform.
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isolation structure and antibacterial activities of lucensimycins d g discovered from streptomyces lucensis ma7349 using an Antisense Strategy
Journal of Natural Products, 2009Co-Authors: Suresh B Singh, Deborah L Zink, Oscar Salazar, Angela Basilio, Francisca Vicente, Kevin M Byrne, Mary Motyl, Karen Dorso, Sookhee Ha, Olga GenilloudAbstract:Bacterial resistance to existing antibiotics continues to grow, necessitating the discovery of new compounds of this type. Antisense-based whole-cell target-based screening is a new and highly sens...
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discovery of lucensimycins a and b from streptomyces lucensis ma7349 using an Antisense Strategy
Organic Letters, 2006Co-Authors: Suresh B Singh, Deborah L Zink, Joann Huber, Olga Genilloud, Oscar Salazar, Maria Teresa Diez, Angela Basilio, Francisca Vicente, Kevin M ByrneAbstract:Inhibition of protein synthesis is one of the validated and highly successful targets for inhibition of bacterial growth; this mechanism is a target of a large number of clinical drugs. Ribosomal protein S4, a primary protein, is a potential target for the discovery of antibacterial agents. We describe, using an Antisense-sensitized rpsD Streptomyces aureus strain, the discovery and activity of lucensimycins A and B.
Angela Basilio - One of the best experts on this subject based on the ideXlab platform.
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discovery and antibacterial activity of glabramycin a c from neosartorya glabra by an Antisense Strategy
The Journal of Antibiotics, 2009Co-Authors: Hiranthi Jayasuriya, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, Mary Lee Goldman, Mary Motyl, Gabe DezenyAbstract:Treatment of drug-resistant bacteria is a significant unmet medical need. This challenge can be met only by the discovery and development of new antibiotics. Antisense technology is one of the newest discovery tools that provides enhanced sensitivity for detection of antibacterials, and has led to the discovery of a number of interesting new antibacterial natural products. Continued utilization of this technology led to the discovery of three new bicyclic lactones, glabramycins A–C, from a Neosartorya glabra strain. Glabramycin C showed strong antibiotic activity against Streptococcus pneumoniae (MIC 2 μg ml−1) and modest antibiotic activity against Staphylococcus aureus (MIC 16 μg ml−1). The isolation, structure, relative configuration and antibacterial activity, and plausible biogenesis of these compounds have been discussed.
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Discovery and antibacterial activity of glabramycin A–C from Neosartorya glabra by an Antisense Strategy
The Journal of Antibiotics, 2009Co-Authors: Hiranthi Jayasuriya, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, Mary Lee Goldman, Mary Motyl, Gabe DezenyAbstract:Treatment of drug-resistant bacteria is a significant unmet medical need. This challenge can be met only by the discovery and development of new antibiotics. Antisense technology is one of the newest discovery tools that provides enhanced sensitivity for detection of antibacterials, and has led to the discovery of a number of interesting new antibacterial natural products. Continued utilization of this technology led to the discovery of three new bicyclic lactones, glabramycins A–C, from a Neosartorya glabra strain. Glabramycin C showed strong antibiotic activity against Streptococcus pneumoniae (MIC 2 μg ml−1) and modest antibiotic activity against Staphylococcus aureus (MIC 16 μg ml−1). The isolation, structure, relative configuration and antibacterial activity, and plausible biogenesis of these compounds have been discussed.
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isolation structure and antibacterial activities of lucensimycins d g discovered from streptomyces lucensis ma7349 using an Antisense Strategy
Journal of Natural Products, 2009Co-Authors: Suresh B Singh, Deborah L Zink, Oscar Salazar, Angela Basilio, Francisca Vicente, Kevin M Byrne, Mary Motyl, Karen Dorso, Sookhee Ha, Olga GenilloudAbstract:Bacterial resistance to existing antibiotics continues to grow, necessitating the discovery of new compounds of this type. Antisense-based whole-cell target-based screening is a new and highly sens...
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isolation structure and antibacterial activity of pleosporone from a pleosporalean ascomycete discovered by using Antisense Strategy
Bioorganic & Medicinal Chemistry, 2009Co-Authors: Chaowei Zhang, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, John G Ondeyka, Gonzalo Platas, Karen Dorso, Mary MotylAbstract:Abstract Protein synthesis is one of the best antibacterial targets that have led to the development of a number of highly successful clinical drugs. Protein synthesis is catalyzed by ribosome, which is comprised of a number of ribosomal proteins that help the catalysis process. Ribosomal protein S4 (RPSD) is one of the proteins that is a part of the ribosomal machinery and is a potential new target for the discovery of antibacterial agents. Screening of microbial extracts using Antisense-sensitized rpsD Staphylococcus aureus strain led to the isolation of pleosporone, a new compound, with modest antibacterial activities with MIC ranging from 1 to 64 μg/mL. This compound showed the highest sensitivity for Streptococcus pneumoniae and Haemophilus influenzae , and exhibited MIC’s of 4 and 1 μg/mL, respectively. Pleosporone showed modest selectivity for the inhibition of RNA synthesis compared to DNA and protein synthesis, and showed activity against HeLa cells. Isolation, structure elucidation, and biological activity of pleosporone have been described.
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isolation structure and antibacterial activity of phaeosphenone from a phaeosphaeria sp discovered by Antisense Strategy
Journal of Natural Products, 2008Co-Authors: Chaowei Zhang, Deborah L Zink, Joann Huber, Angela Basilio, Francisca Vicente, Javier Collado, Gerald F Bills, John G Ondeyka, Gonzalo Platas, Karen DorsoAbstract:Ribosomal protein S4 (RPSD), a part of the ribosomal small subunit, is one of the proteins that is a part of the ribosomal machinery and is a potential new target for the discovery of antibacterial agents. Continued screening of microbial extracts using Antisense-sensitized rpsD Staphylococcus aureus strain led to the isolation of a new dimeric compound, phaeosphenone (2). Compound 2 showed broad-spectrum antibacterial activity against Gram-positive bacteria, exhibiting MIC values ranging from 8 to 64 μg/mL. Phaeosphenone showed the highest sensitivity for Streptococcus pneumoniae (8 μg/mL) and inhibited the growth of Candida albicans with an MIC of 8 μg/mL. Phaeosphenone showed a modest selectivity for the inhibition of RNA synthesis over DNA and protein synthesis in S. aureus.
