HIV-1 Protease: Structural Perspectives on Drug Resistance
Antiviral inhibitors of HIV-1 protease are a notable success of structure-based drug design and have dramatically improved AIDS therapy. Analysis of the structures and activities of drug resistant protease variants has revealed novel molecular mechanisms
Irene T. Weber, Johnson Agniswamy
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Structure and Dynamics of Zika Virus Protease and Its Insights into Inhibitor Design
Zika virus (ZIKV)—a member of the Flaviviridae family—is an important human pathogen. Its genome encodes a polyprotein that can be further processed into structural and non-structural proteins.
Qingxin Li, Congbao Kang
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Comparative proteome analysis of multi-layer cocoon of the silkworm, Bombyx mori. [PDF]
Bombyx mori cocoon has a multi-layer structure that provides optimal protection for silkworm pupa. Research on the mechanical properties of the multi-layer structure revealed structure-property relationships of the cocoon.
Yan Zhang +8 more
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The role of the HIV-1 protease substrate in therapy resistance [PDF]
In Switzerland and Germany up to a half of the first-line regimens include protease inhibitors (PIs) [1, 2]. Although in the Swiss HIV Cohort Study (SHCS) most patients under antiretroviral therapy (ART) have suppressed viral loads [3], every third ...
Kletenkov, Konstantin
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Approximately 20 years has passed since the first human trial with HIV-1 protease inhibitors. Protease inhibitors set the stage for combination therapy in the mid-1990s but are now rarely used in first-line combination therapy and reserved for salvage ...
Arts Eric J
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C-Terminal Extended Hexapeptides as Potent Inhibitors of the NS2B-NS3 Protease of the ZIKA Virus
The Zika virus (ZIKV) protease is an attractive drug target for the design of novel inhibitors to control the ZIKV infection. As the protease substrate-binding site contains acidic residues, inhibitors with basic residues can be beneficial for the ...
Suyash Pant, Nihar R. Jena
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Genetic basis of hypersusceptibility to protease inhibitors and low replicative capacity of human immunodeficiency virus type 1 strains in primary infection [PDF]
The initial virus strains from as many as 12% of individuals with primary human immunodeficiency virus (HIV) infection have a 50% inhibitory concentration less than or equal to0.4-fold that of HIV type 1(NL4-3) (HIV-1(NL4-3)) to ritonavir ...
Joseph B. Margolick +29 more
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The Kunitz-type protease inhibitors are the best-characterized family of serine protease inhibitors, probably due to their abundance in several organisms.
Caroline B. F. Mourão +1 more
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The crosstalk between Dendritic and Natural Killer cells together with the function of Tumor Associated Macrophages (TAM) represent novel cancer-related targets for Human Immunodeficiency Type-1 Protease Inhibitors [PDF]
Inflammatory conditions and infections in selected organs increase the risk of cancer. In the tumor microenvironment, smoldering inflammation contributes to proliferation and survival of malignant cells, angiogenesis, metastasis and subversion of ...
Ciaglia, Elena
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Inhibitors of rhomboid proteases [PDF]
Rhomboid proteases form one of the most widespread families of intramembrane proteases. They utilize a catalytic serine-histidine dyad located several Å below the surface of the membrane for substrate hydrolysis. Multiple studies have implicated rhomboid proteases in biologically and medically relevant processes. Several assays have been developed that
Wolf, Eliane V., Verhelst, Steven
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