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27 results on '"Cooper Curt S"'

1. From Bacterial Genomes to Novel Antibacterial Agents: Discovery, Characterization, and Antibacterial Activity of Compounds that Bind to HI0065 (YjeE) from Haemophilus influenzae

Author

Lerner, Claude G., Hajduk, Philip J., Wagner, Rolf, Wagenaar, Frank L., Woodall, Charlotte, Gu, Yu-Gui, Searle, Xenia B., Florjancic, Alan S., Zhang, Tianyuan, Clark, Richard F., Cooper, Curt S., Mack, Jamey C., Yu, Liping, Cai, Mengli, Betz, Steven F., Chovan, Linda E., McCall, J. Owen, Black-Schaefer, Candace L., Kakavas, Stephan J., Schurdak, Mark E., Comess, Kenneth M., Walter, Karl A., Edalji, Rohinton, Dorwin, Sarah A., Smith, Richard A., Hebert, Eric J., Harlan, John E., Metzger, Randy E., Merta, Philip J., Baranowski, John L., Coen, Michael L., Thornewell, Susan J., Shivakumar, Annapur G., Saiki, Anne Y., Soni, Niru, Bui, Mai, Balli, Darlene J., Sanders, William J., Nilius, Angela M., Holzman, Thomas F., Fesik, Stephen W., and Beutel, Bruce A.

Published
2007

2. Structure-based Optimization of MurF Inhibitors

Author

Stamper, Geoffrey F., Longenecker, Kenton L., Fry, Elizabeth H., Jakob, Clarissa G., Florjancic, Alan S., Gu, Yu-Gui, Anderson, David D., Cooper, Curt S., Zhang, Tianyuan, Clark, Richard F., Cia, Yingna, Black-Schaefer, Candace L., McCall, J. Owen, Lerner, Claude G., Hajduk, Philip J., Beutel, Bruce A., and Stoll, Vincent S.

Published
2006

3. From Bacterial Genomes to Novel Antibacterial Agents: Discovery, Characterization, and Antibacterial Activity of Compounds that Bind to HI0065 (YjeE) from Haemophilus influenzae

Author

Tianyuan Zhang, Richard A. G. Smith, Rohinton Edalji, Yu-Gui Gu, John L. Baranowski, William J. Sanders, Bruce A. Beutel, Liping Yu, Philip J. Hajduk, Annapur Gurulingappa Shivakumar, Stephan J. Kakavas, Frank L. Wagenaar, Darlene J. Balli, Steven F. Betz, Richard F. Clark, Kenneth M. Comess, Eric J. Hebert, J. Owen McCall, Jamey Mack, Linda E. Chovan, Randy E. Metzger, Thomas F. Holzman, Anne Y. Saiki, Sarah A. Dorwin, Niru B. Soni, Mai Bui, Angela M. Nilius, Susan J. Thornewell, Cooper Curt S, Mark E. Schurdak, Michael L. Coen, Rolf Wagner, Alan S. Florjancic, Philip J. Merta, Claude G. Lerner, Charlotte Woodall, Candace Black-Schaefer, John E. Harlan, Mengli Cai, Karl A. Walter, Xenia B. Searle, and Stephen W. Fesik

Subjects
Magnetic Resonance Spectroscopy, Chemistry, Pharmaceutical, Molecular Sequence Data, Plasma protein binding, Bacterial genome size, medicine.disease_cause, Biochemistry, Mass Spectrometry, Microbiology, Haemophilus influenzae, Structure-Activity Relationship, Bacterial Proteins, Drug Discovery, medicine, Animals, Amino Acid Sequence, Adenosine Triphosphatases, Pharmacology, B-Lymphocytes, biology, Drug discovery, Organic Chemistry, Genomics, biology.organism_classification, Anti-Bacterial Agents, Mechanism of action, Essential gene, Drug Design, Molecular Medicine, medicine.symptom, Antibacterial activity, Genome, Bacterial, Bacteria, Protein Binding
Abstract

As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR- and mass spectrometry-based affinity selection screens were performed to identify compounds that bind to protein targets uniquely found in bacteria and encoded by genes essential for microbial viability. A biphenyl acid lead series emerged from an NMR-based screen with the Haemophilus influenzae protein HI0065, a member of a family of probable ATP-binding proteins found exclusively in eubacteria. The structure-activity relationships developed around the NMR-derived biphenyl acid lead were consistent with on-target antibacterial activity as the Staphylococcus aureus antibacterial activity of the series correlated extremely well with binding affinity to HI0065, while the correlation of binding affinity with B-cell cytotoxicity was relatively poor. Although further studies are needed to conclusively establish the mode of action of the biphenyl series, these compounds represent novel leads that can serve as the basis for the development of novel antibacterial agents that appear to work via an unprecedented mechanism of action. Overall, these results support the genomics-driven hypothesis that targeting bacterial essential gene products that are not present in eukaryotic cells can identify novel antibacterial agents.

Published
2007
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5. Structure-based optimization of MurF inhibitors

Author

J. Owen McCall, Bruce A. Beutel, Philip J. Hajduk, Geoffrey F. Stamper, Richard F. Clark, Yingna Cia, Kenton L. Longenecker, Elizabeth H. Fry, Candace Black-Schaefer, Clarissa G. Jakob, Cooper Curt S, Alan S. Florjancic, Claude G. Lerner, Vincent S. Stoll, Yu-Gui Gu, David D. Anderson, and Tianyuan Zhang

Subjects
Pharmacology, chemistry.chemical_classification, Models, Molecular, Sulfonamides, Magnetic Resonance Spectroscopy, Chemistry, Organic Chemistry, Crystallography, X-Ray, Ligands, Biochemistry, Cocrystal, Bacterial cell structure, Substrate Specificity, Inhibitory Concentration 50, Structure-Activity Relationship, Enzyme, Drug Discovery, Molecular Medicine, Structure based, Enzyme Inhibitors, Peptide Synthases, Crystallization, Function (biology)
Abstract

The D-Ala-D-Ala adding enzyme (MurF) from Streptococcus pneumoniae catalyzes the ATP-dependent formation of the UDP-MurNAc-pentapeptide, a critical component of the bacterial cell wall. MurF is a potential target for antibacterial design because it is unique to bacteria and performs an essential non-redundant function in the bacterial cell. The recent discovery and subsequent cocrystal structure determination of MurF in complex with a new class of inhibitors served as a catalyst to begin a medicinal chemistry program aimed at improving their potency. We report here a multidisciplinary approach to this effort that allowed for rapid generation of cocrystal structures, thereby providing the crystallographic information critical for driving the inhibitor optimization process. This effort resulted in the discovery of low-nanomolar inhibitors of this bacterial enzyme.

Published
2006

6. Structure-activity relationships of novel potent MurF inhibitors

Author

J. Owen McCall, Claude G. Lerner, Tianyuan Zhang, Cooper Curt S, Richard F. Clark, Geoffrey F. Stamper, Yingna Cai, Candace Black-Schaefer, David D. Anderson, Philip J. Hajduk, Yu Gui Gu, Alan S. Florjancic, and Bruce A. Beutel

Subjects
Chemistry, Organic Chemistry, Clinical Biochemistry, Sulfonamide (medicine), Pharmaceutical Science, Peptidoglycan, Biochemistry, Chemical synthesis, In vitro, chemistry.chemical_compound, Structure-Activity Relationship, Biosynthesis, Bacterial Proteins, Drug Discovery, medicine, Molecular Medicine, Enzyme Inhibitors, Peptide Synthases, Antibacterial activity, Molecular Biology, medicine.drug
Abstract

A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers.

Published
2003

7. Aviation Security: Biometric Technology and Risk Based Security Aviation Passenger Screening Program

Author

NAVAL POSTGRADUATE SCHOOL MONTEREY CA, Cooper, Curt S, NAVAL POSTGRADUATE SCHOOL MONTEREY CA, and Cooper, Curt S

Abstract

Since 9/11, the Transportation Security Administration (TSA) has struggled to maintain a balance between providing a secure world-class aviation passenger-screening program (APSP) while providing efficiency, convenience and security for the traveling public and the airline industry. For years the TSA has applied resources and procedures uniformly to all passengers during aviation passenger screening. It is mainly a one size fits all screening where all passengers are treated as equal risk, which has exponentially increased resources, procedures and equipment required to do aviation passenger screening, Recently, the Transportation Security Administration has sought to find a better way to conduct aviation passenger screening and is transitioning to Risk Based Security (RBS). The RBS initiatives have greatly improved the aviation passenger screening experience while increasing the efficiency of checkpoint screening by shortening the amount of wait times. Furthermore, it has allowed resources to be applied to high-risk individuals and lessen the burden of passenger screening on low-risk individuals. This has freed up resources reduced procedures while simultaneously increasing the efficiency of the checkpoint. The research here provides options on how to better enable current RBS initiatives by incorporating biometric technology into the aviation passenger-screening program. This research has reviewed other government programs that have incorporated biometrics into their procedures to improve the efficiency and reliability by using biometrically enhanced security measures. Through the application or modification of these biometrically enhanced security programs of other agencies, the TSA could standardize and incorporate biometrics into the RBS APSP allowing for authentication of both identity verification and identification. This research will explore how to incorporate biometrics into the current Risk-Based Security Aviation Passenger Screening Program.

Published
2012

8. Aviation security: biometric technology and risk based security aviation passenger screening program

Author

Fernandez, Lauren, Kiernan, Kathleen, Homeland Security, Cooper, Curt S., Fernandez, Lauren, Kiernan, Kathleen, Homeland Security, and Cooper, Curt S.

Abstract

Since 9/11, the Transportation Security Administration (TSA) has struggled to maintain a balance between providing a secure world-class aviation passenger-screening program (APSP) while providing efficiency, convenience and security for the traveling public and the airline industry. For years the TSA has applied resources and procedures uniformly to all passengers during aviation passenger screening. It is mainly a one size fits all screening where all passengers are treated as equal risk, which has exponentially increased resources, procedures and equipment required to do aviation passenger screening, Recently, the Transportation Security Administration has sought to find a better way to conduct aviation passenger screening and is transitioning to Risk Based Security (RBS). The RBS initiatives have greatly improved the aviation passenger screening experience while increasing the efficiency of checkpoint screening by shortening the amount of wait times. Furthermore, it has allowed resources to be applied to high-risk individuals and lessen the burden of passenger screening on low-risk individuals. This has freed up resources reduced procedures while simultaneously increasing the efficiency of the checkpoint. The research here provides options on how to better enable current RBS initiatives by incorporating biometric technology into the aviation passenger-screening program. This research has reviewed other government programs that have incorporated biometrics into their procedures to improve the efficiency and reliability by using biometrically enhanced security measures. Through the application or modification of these biometrically enhanced security programs of other agencies, the TSA could standardize and incorporate biometrics into the RBS APSP allowing for authentication of both identity verification and identification. This research will explore how to incorporate biometrics into the current Risk-Based Security Aviation Passenger Screening Program.

Published
2012

9. Synthesis and antimicrobial activity of 4H-4-oxoquinolizine derivatives: consequences of structural modification at the C-8 position

Author

Linus L. Shen, Angela M. Nilius, Yat Sun Or, Qun Li, Sanyi Wang, Anthony K. L. Fung, Robert K. Flamm, Zhenkun Ma, Jeffery D. Alder, Cooper Curt S, Jonathan A. Meulbroek, and Daniel T. W. Chu

Subjects
biology, Chemistry, Stereoisomerism, Antimicrobial, biology.organism_classification, medicine.disease_cause, Gram-Positive Bacteria, Anti-Bacterial Agents, Ciprofloxacin, Mice, Structure-Activity Relationship, Antibiotic resistance, Biochemistry, In vivo, Staphylococcus aureus, Drug Discovery, Gram-Negative Bacteria, medicine, Molecular Medicine, Animals, Antibacterial activity, Bacteria, Quinolizines, Antibacterial agent, medicine.drug
Abstract

The antibacterial 4H-4-oxoquinolizines were introduced recently to overcome bacterial resistance to fluoroquinolones. They exhibit potent antibacterial activity against Gram-positive, Gram-negative, and anaerobic organisms and are highly active against some quinolone-resistant bacteria including quinolone-resistant MRSA. Preliminary studies indicated that oxoquinolizines possess distinct activity and toxicity profiles as compared with their parent quinolones. In order to develop a potent antibacterial agent with the desired spectrum of activity, good tolerability, and balanced pharmacokinetic profile, we synthesized and evaluated a series of oxoquinolizines with various substituents at the C-8 position. Most compounds tested in this study demonstrated better activity against Gram-positive bacteria than ciprofloxacin and exhibited good susceptibility against ciprofloxacin- and methicillin-resistant S. aureus. While maintaining potent in vitro activity, several compounds showed improved in vivo efficacy over ABT-719 as indicated by the mouse protection test. As an example, the oral ED(50) values for the cis-3-amino-4-methylpiperidine analogue 3ss against S. aureus NCTC 10649M, S. pneumoniae ATCC 6303, and E. coli JUHL were 0. 8, 2.0, and 1.4 mg/kg, compared to 3.0, 10.0, and 8.3 mg/kg for ABT-719. The current study revealed that the steric and electronic environment, conformation, and absolute stereochemistry of the C-8 group are very important to the antibacterial profiles. Structural modifications of the C-8 group provide a useful means to improve the antibacterial activities, physicochemical properties, and pharmacokinetic profiles. Manipulation of the C-8 group also allows us to generate analogues with the desired spectrum of activity, such as analogues that are selective against respiratory pathogens.

Published
1999

10. Structure–activity relationships of novel potent MurF inhibitors

Author

Gu, Yu Gui, primary, Florjancic, Alan S., additional, Clark, Richard F., additional, Zhang, Tianyuan, additional, Cooper, Curt S., additional, Anderson, David D., additional, Lerner, Claude G., additional, McCall, J.Owen, additional, Cai, Yingna, additional, Black-Schaefer, Candace L., additional, Stamper, Geoffrey F., additional, Hajduk, Philip J., additional, and Beutel, Bruce A., additional

Published
2004
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11. Synthesis and Antimicrobial Activity of 4H-4-Oxoquinolizine Derivatives: Consequences of Structural Modification at the C-8 Position

Author

Ma, Zhenkun, primary, Chu, Daniel T. W., additional, Cooper, Curt S., additional, Li, Qun, additional, Fung, Anthony K. L., additional, Wang, Sanyi, additional, Shen, Linus L., additional, Flamm, Robert K., additional, Nilius, Angela M., additional, Alder, Jeffery D., additional, Meulbroek, Jonathan A., additional, and Or, Yat Sun, additional

Published
1999
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15. Synthesis and Structure−Activity Relationships of 2-Pyridones: A Novel Series of Potent DNA Gyrase Inhibitors as Antibacterial Agents

Author

Li, Qun, primary, Chu, Daniel T. W., additional, Claiborne, Akiyo, additional, Cooper, Curt S., additional, Lee, Cheuk M., additional, Raye, Kathleen, additional, Berst, Kristine B., additional, Donner, Pamela, additional, Wang, Weibo, additional, Hasvold, Lisa, additional, Fung, Anthony, additional, Ma, Zhenkun, additional, Tufano, Michael, additional, Flamm, Robert, additional, Shen, Linus L., additional, Baranowski, John, additional, Nilius, Angela, additional, Alder, Jeff, additional, Meulbroek, Jonathan, additional, Marsh, Kennan, additional, Crowell, DeAnne, additional, Hui, Yuhua, additional, Seif, Louis, additional, Melcher, Laura M., additional, Henry, Rodger, additional, Spanton, Steven, additional, Faghih, Ramin, additional, Klein, Larry L., additional, Tanaka, S. Ken, additional, and Plattner, Jacob J., additional

Published
1996
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19. Aviation security: biometric technology and risk based security aviation passenger screening program

Author

Fernandez, Lauren, Kiernan, Kathleen, Homeland Security, Cooper, Curt S., Fernandez, Lauren, Kiernan, Kathleen, Homeland Security, and Cooper, Curt S.

Abstract

Since 9/11, the Transportation Security Administration (TSA) has struggled to maintain a balance between providing a secure world-class aviation passenger-screening program (APSP) while providing efficiency, convenience and security for the traveling public and the airline industry. For years the TSA has applied resources and procedures uniformly to all passengers during aviation passenger screening. It is mainly a one size fits all screening where all passengers are treated as equal risk, which has exponentially increased resources, procedures and equipment required to do aviation passenger screening, Recently, the Transportation Security Administration has sought to find a better way to conduct aviation passenger screening and is transitioning to Risk Based Security (RBS). The RBS initiatives have greatly improved the aviation passenger screening experience while increasing the efficiency of checkpoint screening by shortening the amount of wait times. Furthermore, it has allowed resources to be applied to high-risk individuals and lessen the burden of passenger screening on low-risk individuals. This has freed up resources reduced procedures while simultaneously increasing the efficiency of the checkpoint. The research here provides options on how to better enable current RBS initiatives by incorporating biometric technology into the aviation passenger-screening program. This research has reviewed other government programs that have incorporated biometrics into their procedures to improve the efficiency and reliability by using biometrically enhanced security measures. Through the application or modification of these biometrically enhanced security programs of other agencies, the TSA could standardize and incorporate biometrics into the RBS APSP allowing for authentication of both identity verification and identification. This research will explore how to incorporate biometrics into the current Risk-Based Security Aviation Passenger Screening Program., http://archive.org/details/aviationsecurity1094527811, Department of Homeland Security, Approved for public release; distribution is unlimited.

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