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Full-Text Articles in Medicinal and Pharmaceutical Chemistry
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
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
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. …
Parallel Text Immersion, Daniel P. Becker Ph.D.
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.
Characterization Of The Lignin Signature In Lake Mead, Nv, Sediment: Comparison Of On-Line Flash Chemopyrolysis (600°C) And Off-Line Chemolysis (250°C), Spencer Steinberg, Elkas Nemr, Mark Rudin
Characterization Of The Lignin Signature In Lake Mead, Nv, Sediment: Comparison Of On-Line Flash Chemopyrolysis (600°C) And Off-Line Chemolysis (250°C), Spencer Steinberg, Elkas Nemr, Mark Rudin
Mark J. Rudin
The distribution of lignin in sediment is a useful tool for tracing the transport of land-derived organic matter in an aquatic environment. Tetramethylammonium hydroxide (TMAH) flash chemopyrolysis, or chemolysis followed by GC-MS analysis can be used for evaluating the origin of organic carbon in sediments. TMAH chemopyrolysis or chemolysis of organic matter produces a myriad of semi-volatile products. Among these products are methylated phenols which are an indirect measure of lignin in sediment. In this study, total organic carbon, elemental carbon, and lignin were measured in Lake Mead sediments. This study indicates that terrestrial runoff makes a contribution to Lake …