scholarly journals Biophysical characterization of small molecule antiviral-loaded nanolipogels for HIV-1 chemoprophylaxis and topical mucosal application

2016 ◽  
Vol 36 ◽  
pp. 122-131 ◽  
Author(s):  
R. Ramanathan ◽  
Y. Jiang ◽  
B. Read ◽  
S. Golan-Paz ◽  
K.A. Woodrow
Keyword(s):  
Small Molecule ◽  
Biophysical Characterization ◽  
Hiv 1

Biophysical characterization of V3-lipopeptide liposomes influencing HIV-1 infectivity

2007 ◽  
Vol 355 (4) ◽  
pp. 963-969 ◽  
Author(s):  
Apostolos K. Rizos ◽  
Stavroula Baritaki ◽  
Ioannis Tsikalas ◽  
David C. Doetschman ◽  
Demetrios A. Spandidos ◽  
...  
Keyword(s):  
Biophysical Characterization ◽  
Hiv 1

scholarly journals Discovery and mechanism of action of small molecule inhibitors of ceramidases

2021 ◽  
Author(s):  
Sebastien Granier ◽  
Robert D Healey ◽  
Essa Saied ◽  
Xiaojing Cong ◽  
Gergely Karsai ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Small Molecules ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Integral Membrane Proteins ◽  
Sphingolipid Metabolism ◽  
New Paradigm ◽  
Biophysical Characterization ◽  
Sphingosine 1 Phosphate

Sphingolipid metabolism is tightly controlled by enzymes to regulate essential processes such as energy utilisation and cell proliferation. The central metabolite is ceramide, a pro-apoptotic lipid catabolized by ceramidase enzymes to ultimately produce pro-proliferative sphingosine-1-phosphate. Human ceramidases can be soluble proteins (acid and neutral ceramidase) or integral membrane proteins (alkaline ceramidases). Increasing ceramide levels to increase apoptosis has shown efficacy as a cancer treatment using small molecules inhibiting a soluble ceramidase. Due to the transmembrane nature of alkaline ceramidases, no specific small molecule inhibitors have been reported. Here, we report novel fluorescent substrates (FRETceramides) of ceramidases that can be used to monitor enzyme activity in real-time. We use FRETceramides to discover the first drug-like inhibitors of alkaline ceramidase 3 (ACER3) which are active in cell-based assays. Biophysical characterization of enzyme:inhibitor interactions reveal a new paradigm for inhibition of lipid metabolising enzymes with non-lipidic small molecules.

scholarly journals De Novo Design and Biophysical Characterization of an Affinity-Enhanced Protein Displaying the Structure of the Broadly Neutralizing HIV-1 2F5 Antibody Epitope

2016 ◽  
Vol 110 (3) ◽  
pp. 346a
Author(s):  
Isabelle Freire Tabosa Viana ◽  
Eduardo Nascimento ◽  
Jodi Craigo ◽  
Marco Krieger ◽  
Robbie Mailliard ◽  
...  
Keyword(s):  
De Novo ◽  
De Novo Design ◽  
Biophysical Characterization ◽  
Antibody Epitope ◽  
Hiv 1

scholarly journals Recombinant expression, purification, and biophysical characterization of the transmembrane and membrane proximal domains of HIV-1 gp41

2014 ◽  
Vol 23 (11) ◽  
pp. 1607-1618 ◽  
Author(s):  
Zhen Gong ◽  
Sarah A. Kessans ◽  
Lusheng Song ◽  
Katerina Dörner ◽  
Ho-Hsien Lee ◽  
...  
Keyword(s):  
Recombinant Expression ◽  
Biophysical Characterization ◽  
Hiv 1

Biophysical characterization of recombinant HIV-1 subtype C virus infectivity factor

Amino Acids ◽  
2010 ◽  
Vol 40 (3) ◽  
pp. 981-989 ◽  
Author(s):  
Daniela Gallerano ◽  
Siva Charan Devanaboyina ◽  
Ines Swoboda ◽  
Birgit Linhart ◽  
Irene Mittermann ◽  
...  
Keyword(s):  
Virus Infectivity ◽  
Subtype C ◽  
Biophysical Characterization ◽  
Hiv 1

Computational Characterization of Binding of Small Molecule Inhibitors to HIV-1 gp41

2011 ◽  
Vol 29 (7) ◽  
pp. 1307-1311 ◽  
Author(s):  
Kuizhong Song ◽  
Ju Bao ◽  
Yueming Sun ◽  
John Z. H. Zhang
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Hiv 1

scholarly journals Biophysical Characterization of a Vaccine Candidate against HIV-1: The Transmembrane and Membrane Proximal Domains of HIV-1 gp41 as a Maltose Binding Protein Fusion

PLoS ONE ◽  
2015 ◽  
Vol 10 (8) ◽  
pp. e0136507 ◽  
Author(s):  
Zhen Gong ◽  
Jose M. Martin-Garcia ◽  
Sasha M. Daskalova ◽  
Felicia M. Craciunescu ◽  
Lusheng Song ◽  
...  
Keyword(s):  
Vaccine Candidate ◽  
Binding Protein ◽  
Maltose Binding Protein ◽  
Protein Fusion ◽  
Biophysical Characterization ◽  
Maltose Binding Protein Fusion ◽  
Hiv 1
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