Chemicals and Drugs Commons^™

Dengue Virus Ns2b/Ns3 Protease Inhibitors Exploiting The Prime Side, Kuan-Hung Lin, Akbar Ali, Linah Rusere, Djade I. Soumana, Nese Kurt Yilmaz, Celia A. Schiffer

Celia A. Schiffer

The mosquito-transmitted dengue virus (DENV) infects millions of people in tropical and subtropical regions. Maturation of DENV particles requires proper cleavage of the viral polyprotein, including processing of 8 of the 13 substrate cleavage sites by dengue virus NS2B/NS3 protease. With no available direct-acting antiviral targeting DENV, NS2/NS3 protease is a promising target for inhibitor design. Current design efforts focus on the nonprime side of the DENV protease active site, resulting in highly hydrophilic and nonspecific scaffolds. However, the prime side also significantly modulates DENV protease binding affinity, as revealed by engineering the binding loop of aprotinin, a small protein …

Interdependence Of Inhibitor Recognition In Hiv-1 Protease, Janet L. Paulsen, Florian Leidner, Debra A. Ragland, Nese Kurt Yilmaz, Celia A. Schiffer

Celia A. Schiffer

Molecular recognition is a highly interdependent process. Subsite couplings within the active site of proteases are most often revealed through conditional amino acid preferences in substrate recognition. However, the potential effect of these couplings on inhibition and thus inhibitor design is largely unexplored. The present study examines the interdependency of subsites in HIV-1 protease using a focused library of protease inhibitors, to aid in future inhibitor design. Previously a series of darunavir (DRV) analogs was designed to systematically probe the S1' and S2' subsites. Co-crystal structures of these analogs with HIV-1 protease provide the ideal opportunity to probe subsite interdependency. …

In-Season N Fertilization Strategies Using Active Sensors, Daniel Barker, John Sawyer

John E. Sawyer

The objectives of this project were to measure corn yield response to applied nitrogen (N) fertilizer based on active canopy sensing during the mid-vegetative corn growth stage (V10) and compare yield and N use efficiency between pre-plant N (PP-N), pre-plant + sensor N (PP+S-N), split N strategy (SNS), and rescue N strategy (RNS).

In-Season N Fertilization Strategies Using Active Sensors, Daniel Barker, John Sawyer

John E. Sawyer

The objectives of this project were to measure corn yield response to applied nitrogen (N) fertilizer based on active canopy sensing during the mid-vegetative corn growth stage (V10) and compare yield and N use efficiency between pre-plant N (PP-N), pre-plant + sensor N (PP+S-N), split N strategy (SNS), and rescue N strategy (RNS).

In-Season N Fertilization Strategies Using Active Sensors, Daniel Barker, John Sawyer

John E. Sawyer

The objectives of this project were to measure corn yield response to applied nitrogen (N) fertilizer based on active canopy sensing during the mid-vegetative corn growth stage (V10) and compare yield and N use efficiency between pre-plant N (PP-N), pre-plant + sensor N (PP+S-N), split N strategy (SNS), and rescue N strategy (RNS).

Impacts Of Cover Crops On Phosphorus And Nitrogen Loss With Surface Runoff, Antonio Mallarino, Richard Cruse, Dan Jaynes, John Sawyer, Pablo Barbieri

John E. Sawyer

Iowa research has demonstrated that cover crops can improve soil productivity and water quality by increasing soil organic matter and reducing nitrate nitrogen (N) leaching. Other research has investigated and is investigating the agronomic and economic viability of using cereal rye cover crops in continuous corn or corn-soybean rotations. However, no Iowa research has evaluated under natural rainfall the impact of cover crops on phosphorus (P) and N loss with surface runoff interacting with other management practices. The need for this type of research was indicated in the Iowa Nutrient Reduction Strategy documents. This effort assessed what would be needed …

Impact Of 4r Management On Crop Production And Nitrate-Nitrogen Loss In Tile Drainage, Matthew Helmers, John Sawyer, Josh Sievers

John E. Sawyer

Corn Belt corn and soybean producers are increasingly challenged to maximize crop production while addressing the contributions farm practices make to Gulf hypoxia. Based on the need for nitrate-N reductions to meet water quality goals, new management practices are needed to reduce nitrate-N losses at minimal cost and maximum economic benefits. This three-year field research and demonstration project is evaluating various promising N management methods and technologies by documenting the nitrate-N export and crop yield from various systems.

Methyl Transfer By Substrate Signaling From A Knotted Protein Fold, Thomas Christian, Reiko Sakaguchi, Agata P. Perlinska, George Lahoud, Takuhiro Ito, Erika A. Taylor, Shigeyuki Yokoyama, Joanna I. Sulkowska, Ya-Ming Hou

Erika A. Taylor, Ph.D.

Interrogating Metabolism In Brain Cancer, Travis Salzillo, Jingzhe Hu, Linda Nguyen, Nicholas Whiting, Jaehyuk Lee, Joseph Weygand, Prasanta Dutta, Shivanand Pudakalakatti, Niki Zacharias Millward, Seth Gammon, Frederick F. Lang, Amy B. Heimberger, Pratip Bhattacharya

Nicholas Whiting

Unexpected Synthesis Of 1,3,5-Triarly-1,5-Diketones From Aryl Ketones Via Di-Enamine Mechanism, Bin Liu, Junfeng Wang, Yi Pang, Zemei Ge, Runtao Li

Yi Pang

An unexpected reaction of aryl ketone with acetohydrazone of aromatic aldehyde via 1,2-di-enamine/diiminium mechanism was discovered, leading to efficient synthesis of 1,3,5-triaryl-1,5-diketones in good to excellent yields. (C) 2014 Elsevier Ltd. All rights reserved.

Binding-Induced, Turn-On Fluorescence Of The Egfr/Erbb Kinase Inhibitor, Lapatinib, James N. Wilson

James N Wilson

We report the photophysical properties, binding-induced turn-on emission, and fluorescence imaging of the cellular uptake and distribution of lapatinib, an EGFR/ERBB inhibitor. Lapatinib, a type II, i.e. inactive state, inhibitor that targets the ATP binding pocket of the EGFR family of receptor tyrosine kinases. DFT calculations predict that the 6-furanylquinazoline core of lapatinib should exhibit an excited state with charge transfer character and an S0 to S1 transition energy of 3.4 eV. Absorption confirms an optical tran- sition in the near UV to violet, while fluorescence spectroscopy shows that photoemission is highly sensi- tive to solvent polarity. The hydrophobicity of …

Warfarin Use And Outcomes In Patients With Advanced Chronic Systolic Heart Failure Without Atrial Fibrillation, Prior Thromboembolic Events, Or Prosthetic Valves, Marjan Mujib, Abu-Ahmed Rahman, Ravi Desai, Mustafa Ahmed, Margaret Feller, Inmaculada Aban, Tomas Love, Michel White, Prakash Deedwania, Wilbert Aronow, Gregg Fonarow, Ali Ahmed

Ravi V Desai MD

No abstract provided.

Influence Of Co-Existing Atrial Fibrillation On The Efficacy Of Atorvastatin Treatment In Patients With Dilated Cardiomyopathy: A Pilot Study, Agata Bielecka-Dabrowa, Jan Goch, Jacek Rysz, Marek Maciejewski, Ravi Desai, Wilbert Aronow

Ravi V Desai MD

No abstract provided.

Relationship Between Left And Right Ventricular Ejection Fractions In Chronic Advanced Systolic Heart Failure: Insights From The Best Trial, Ravi Desai, Philippe Meyer, Mustafa Ahmed, Marjan Mujib, Chris Adamopoulos, Michel White, Inmaculada Aban, Ami Iskandrian, Ali Ahmed

Ravi V Desai MD

No abstract provided.

Compliance With The Centers For Disease Control And Prevention Recommendations For The Diagnosis And Treatment Of Sexually Transmitted Diseases, Bryan Kane, Linda Degutis, Helen Sayward, Gail D'Onofrio

Bryan G Kane MD

No abstract provided.

Parallel Text Immersion, Daniel P. Becker Ph.D.

Daniel P. Becker

A new method of teaching foreign languages to beginning, intermediate, and advancing foreign language students is proposed involving reading out loud passages, chapters, and entire works of literature that are familiar to the student through required pre-reading in the students’ mother tongue. Testing is proposed to evaluate the success of the method.

Synthesis And In Vitro Binding Of N,N-Dialkyl-2-Phenylindol-3-Ylglyoxylamides For The Peripheral Benzodiazepine Binding Sites, T. P. Homes, F. Mattner, Paul A. Keller, A. Katsifis

Paul Keller

A series of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides bearing the halogens iodine and bromine were synthesised and their binding affinity for the peripheral benzodiazepine binding sites (PBBS) in rat kidney mitochondrial membranes were evaluated using [3H]-PK11195. Central benzodiazepine receptor (CBR) affinities were also evaluated in rat cortices using 3H-flumazenil to determine their selectivity for PBBS over CBR. The tested compounds had PBBS binding affinities (IC50) ranging from 7.86 nM to 618 nM, with all compounds showing high selectivity over the CBR (CBR IC50 > 5000 nM). Among the 12 compounds tested, those with a diethylamide group were the most potent. The highest affinity iodinated PBBS …