Nature Inspired Molecular Design: Stereoselective Synthesis of Bicyclic and Polycyclic Ethers for Potent HIV-1 Protease Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Asian journal of organic chemistry"
DOI: 10.1002/ajoc.201800255
Abstract: We have developed a conceptually new generation of non-peptidic HIV-1 protease inhibitors incorporating novel structural templates inspired by nature. This has resulted in protease inhibitors with exceptional potency and excellent pharmacological and drug-resistance profiles. The… read more here.
Keywords: polycyclic ethers; protease; chemistry; drug ... See more keywords
Diversity‐Oriented Synthesis of Diol‐Based Peptidomimetics as Potential HIV Protease Inhibitors and Antitumor Agents
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DOI: 10.1002/cbic.201800247
Abstract: Peptidomimetic HIV protease inhibitors are an important class of drugs used in the treatment of AIDS. The synthesis of a new type of diol‐based peptidomimetics is described. Our route is flexible, uses d‐glucal as an… read more here.
Keywords: hiv protease; based peptidomimetics; diol based; protease inhibitors ... See more keywords
Design, Synthesis, Biological Evaluation, and X‐ray Studies of HIV‐1 Protease Inhibitors with Modified P2′ Ligands of Darunavir
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DOI: 10.1002/cmdc.201700614
Abstract: The structure‐based design, synthesis, and biological evaluation of a series of nonpeptidic HIV‐1 protease inhibitors with rationally designed P2′ ligands are described. The inhibitors are designed to enhance backbone binding interactions, particularly at the S2′… read more here.
Keywords: design synthesis; biological evaluation; protease inhibitors; hiv protease ... See more keywords
Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach
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DOI: 10.1002/cmdc.202000024
Abstract: Pharmacophore searches that include anchors, fragments contributing above average to receptor binding, combined with one‐step syntheses are a powerful approach for the fast discovery of novel bioactive molecules. Here, we are presenting a pipeline for… read more here.
Keywords: discovery aspartyl; discovery; aspartyl protease; protease inhibitors ... See more keywords
Biochemical Screening of Potent Zika Virus Protease Inhibitors.
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DOI: 10.1002/cmdc.202100695
Abstract: As the Zika virus protease is an essential and well-established target for the development of antiviral agents, we here have biochemically screened for inhibitors using a purified recombinantly expressed form of this enzyme. As a… read more here.
Keywords: virus protease; biochemical screening; zika virus; protease inhibitors ... See more keywords
Accurate prediction of relative binding affinities of a series of HIV‐1 protease inhibitors using semi‐empirical quantum mechanical charge
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Computational Chemistry"
DOI: 10.1002/jcc.26218
Abstract: A major challenge in computer‐aided drug design is the accurate estimation of ligand binding affinity. Here, a new approach that combines the adaptive steered molecular dynamics (ASMD) and partial atomic charges calculated by semi‐empirical quantum… read more here.
Keywords: semi empirical; binding affinities; relative binding; empirical quantum ... See more keywords
Human CaaX protease ZMPSTE24 expressed in yeast: Structure and inhibition by HIV protease inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "Protein Science"
DOI: 10.1002/pro.3074
Abstract: The function and localization of proteins and peptides containing C‐terminal “CaaX” (Cys‐aliphatic‐aliphatic‐anything) sequence motifs are modulated by post‐translational attachment of isoprenyl groups to the cysteine sulfhydryl, followed by proteolytic cleavage of the aaX amino acids.… read more here.
Keywords: zmpste24; protease; inhibition; protease inhibitors ... See more keywords
Canonical or noncanonical? Structural plasticity of serine protease‐binding loops in Kunitz‐STI protease inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Protein Science"
DOI: 10.1002/pro.4570
Abstract: The Kunitz‐Soybean Trypsin Inhibitor (Kunitz‐STI) family is a large family of proteins with most of its members being protease inhibitors. The versatility of the inhibitory profile and the structural plasticity of these proteins, make this… read more here.
Keywords: binding loops; protease; kunitz sti; serine protease ... See more keywords
Serine Protease Inhibitors to Treat Lung Inflammatory Diseases.
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DOI: 10.1007/978-3-030-68748-9_13
Abstract: Lung is a vital organ that ensures breathing function. It provides the essential interface of air filtering providing oxygen to the whole body and eliminating carbon dioxide in the blood; because of its exposure to… read more here.
Keywords: treat lung; serine protease; inflammatory; protease inhibitors ... See more keywords
Repositioning HIV protease inhibitors and nucleos(t)ide RNA polymerase inhibitors for the treatment of SARS-CoV-2 infection and COVID-19
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DOI: 10.1007/s00228-021-03108-x
Abstract: Aims SARS-CoV-2 is a single-stranded RNA virus which is part of the ß-coronavirus family (like SARS 2002 and MERS 2012). The high prevalence of hospitalization and mortality, in addition to the lack of vaccines and… read more here.
Keywords: rna polymerase; polymerase inhibitors; protease inhibitors; hiv protease ... See more keywords
Proteomic characterization and antifungal activity of potato tuber proteins isolated from starch production waste under different temperature regimes
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DOI: 10.1007/s00253-018-9373-y
Abstract: Proteins were obtained from effluent of a starch manufacture by using different isolation temperatures (40, 60, 80, and 100 °C). The proteins, remaining in effluent after treatment of potato juice at 80 and 100 °C differed significantly… read more here.
Keywords: potato tuber; antifungal activity; potato; protease inhibitors ... See more keywords