scholarly journals Structure-Based Design, Synthesis, and Characterization of Dual Hotspot Small-Molecule HIV-1 Entry Inhibitors

2012 ◽  
Vol 55 (9) ◽  
pp. 4382-4396 ◽  
Author(s):  
Judith M. LaLonde ◽  
Young Do Kwon ◽  
David M. Jones ◽  
Alexander W. Sun ◽  
Joel R. Courter ◽  
...  
Keyword(s):  
Small Molecule ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Hiv 1

scholarly journals Design, Synthesis, and antiviral activity of a series of CD4-mimetic small-molecule HIV-1 entry inhibitors

2021 ◽  
pp. 116000
Author(s):  
Francesca Curreli ◽  
Shahad Ahmed ◽  
Sofia M. Benedict Victor ◽  
Ildar R. Iusupov ◽  
Evgeny A. Spiridonov ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Small Molecule ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Hiv 1

scholarly journals Design, synthesis and evaluation of small molecule CD4-mimics as entry inhibitors possessing broad spectrum anti-HIV-1 activity

2016 ◽  
Vol 24 (22) ◽  
pp. 5988-6003 ◽  
Author(s):  
Francesca Curreli ◽  
Dmitry S. Belov ◽  
Ranjith R. Ramesh ◽  
Naisargi Patel ◽  
Andrea Altieri ◽  
...  
Keyword(s):  
Small Molecule ◽  
Broad Spectrum ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Bifunctional Small Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins

2019 ◽  
Author(s):  
Ziyang Zhang ◽  
Kevan M. Shokat
Keyword(s):  
Small Molecule ◽  
Therapeutic Strategy ◽  
Cyclophilin A ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Biochemical Assays ◽  
Intracellular Proteins ◽  
Small Molecule Ligands ◽  
Ligand Scaffolds

AbstractHere we report the design, synthesis and characterization of bifunctional chemical ligands that induce the association of Ras with ubiquitously expressed immunophilin proteins such as FKBP12 and cyclophilin A. We show this approach is applicable to two distinct Ras ligand scaffolds, and that both the identity of the immunophilin ligand and the linker chemistry affect compound efficacy in biochemical and cellular contexts. These ligands bind to Ras in an immunophilin-dependent fashion and mediate the formation of tripartite complexes of Ras, immunophilin and the ligand. The recruitment of cyclophilin A to GTP-bound Ras blocks its interaction with B-Raf in biochemical assays. Our study demonstrates the feasibility of ligand-induced association of Ras with intracellular proteins and suggests it as a promising therapeutic strategy for Rasdriven cancers.

The Discovery and Development of Oxalamide and Pyrrole Small Molecule Inhibitors of gp120 and HIV Entry - A Review

2019 ◽  
Vol 19 (18) ◽  
pp. 1650-1675 ◽  
Author(s):  
Damoder Reddy Motati ◽  
Dilipkumar Uredi ◽  
E. Blake Watkins
Keyword(s):  
Small Molecule ◽  
Viral Entry ◽  
Biological Evaluation ◽  
New Drugs ◽  
Design Synthesis ◽  
Mortality And Morbidity ◽  
Glycoprotein Gp120 ◽  
Hiv Entry ◽  
Immunodeficiency Syndrome ◽  
Hiv 1

Human immunodeficiency virus type-1 (HIV-1) is the causative agent responsible for the acquired immunodeficiency syndrome (AIDS) pandemic. More than 60 million infections and 25 million deaths have occurred since AIDS was first identified in the early 1980s. Advances in available therapeutics, in particular combination antiretroviral therapy, have significantly improved the treatment of HIV infection and have facilitated the shift from high mortality and morbidity to that of a manageable chronic disease. Unfortunately, none of the currently available drugs are curative of HIV. To deal with the rapid emergence of drug resistance, off-target effects, and the overall difficulty of eradicating the virus, an urgent need exists to develop new drugs, especially against targets critically important for the HIV-1 life cycle. Viral entry, which involves the interaction of the surface envelope glycoprotein, gp120, with the cellular receptor, CD4, is the first step of HIV-1 infection. Gp120 has been validated as an attractive target for anti-HIV-1 drug design or novel HIV detection tools. Several small molecule gp120 antagonists are currently under investigation as potential entry inhibitors. Pyrrole, piperazine, triazole, pyrazolinone, oxalamide, and piperidine derivatives, among others, have been investigated as gp120 antagonist candidates. Herein, we discuss the current state of research with respect to the design, synthesis and biological evaluation of oxalamide derivatives and five-membered heterocycles, namely, the pyrrole-containing small molecule as inhibitors of gp120 and HIV entry.

scholarly journals Design of an n-type low glass transition temperature radical polymer

2021 ◽  
Author(s):  
Teng Chi ◽  
Siddhartha Akkiraju ◽  
Zihao Liang ◽  
Ying Tan ◽  
Ho Joong Kim ◽  
...  
Keyword(s):  
Glass Transition ◽  
Transition Temperature ◽  
Glass Transition Temperature ◽  
Synthesis And Characterization ◽  
Design Synthesis

We document the design, synthesis, and characterization of the first low glass transition temperature, n-type (i.e., preferentially-reduced) radical polymer.

Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines

ChemMedChem ◽  
2020 ◽  
Vol 15 (13) ◽  
pp. 1150-1162
Author(s):  
Yu Lin ◽  
Zhanhui Li ◽  
Haikuo Ma ◽  
Yujie Wang ◽  
Xu Wang ◽  
...  
Keyword(s):  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Cyclic Amines ◽  
Cxcr4 Antagonists
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