scholarly journals ‘Et tu, inhibitor?’: the potential for HIV inhibitors to prime P-gp-mediated chemoresistance in cancer

2018 ◽  
Vol 4 (2) ◽  
pp. FSO269
Author(s):  
Austin Y Shull ◽  
Christopher L Farrell
Keyword(s):  
Hiv Inhibitors

ChemInform Abstract: QSAR of HIV Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 25 (34) ◽  
pp. no-no
Author(s):  
C. HANSCH ◽  
L. ZHANG
Keyword(s):  
Hiv Inhibitors

scholarly journals Secreted phospholipases A2, a new class of HIV inhibitors that block virus entry into host cells

1999 ◽  
Vol 104 (5) ◽  
pp. 611-618 ◽  
Author(s):  
David Fenard ◽  
Gérard Lambeau ◽  
Emmanuel Valentin ◽  
Jean-Claude Lefebvre ◽  
Michel Lazdunski ◽  
...  
Keyword(s):  
Virus Entry ◽  
Host Cells ◽  
Phospholipases A2 ◽  
New Class ◽  
Hiv Inhibitors

Novel Dual Small-Molecule HIV inhibitors: Scaffolds and Discovery Strategies

2014 ◽  
Vol 21 (7) ◽  
pp. 950-962 ◽  
Author(s):  
Anran Song ◽  
Haiqing Yu ◽  
Changyuan Wang ◽  
Xingqi Zhu ◽  
Kexin Liu ◽  
...  
Keyword(s):  
Small Molecule ◽  
Hiv Inhibitors

scholarly journals Targeting the HIV-1 Spike and Coreceptor with Bi- and Trispecific Antibodies for Single-Component Broad Inhibition of Entry

2018 ◽  
Vol 92 (18) ◽  
Author(s):  
Salar N. Khan ◽  
Devin Sok ◽  
Karen Tran ◽  
Arlette Movsesyan ◽  
Viktoriya Dubrovskaya ◽  
...  
Keyword(s):  
Animal Models ◽  
Hiv Infection ◽  
Binding Sites ◽  
Neutralizing Antibodies ◽  
Single Component ◽  
Single Chain ◽  
Broadly Neutralizing Antibodies ◽  
Hiv Replication ◽  
Hiv Inhibitors ◽  
The Individual

ABSTRACTProtection against acquiring human immunodeficiency virus (HIV) infection may not require a vaccine in the conventional sense, because broadly neutralizing antibodies (bNAbs) alone prevent HIV infection in relevant animal challenge models. Additionally, bNAbs as therapeutics can effectively suppress HIV replication in infected humans and in animal models. Combinations of bNAbs are generally even more effective, and bNAb-derived multivalent antibody-like molecules also inhibit HIV replication bothin vitroandin vivo. To expand the available array of multispecific HIV inhibitors, we designed single-component molecules that incorporate two (bispecific) or three (trispecific) bNAbs that recognize HIV Env exclusively, a bispecific CrossMAb targeting two epitopes on the major HIV coreceptor, CCR5, and bi- and trispecifics that cross-target both Env and CCR5. These newly designed molecules displayed exceptional breadth, neutralizing 98 to 100% of a 109-virus panel, as well as additivity and potency compared to those of the individual parental control IgGs. The bispecific molecules, designed as tandem single-chain variable fragments (scFvs) (10E8fv-N6fv and m36.4-PRO 140fv), displayed median 50% inhibitory concentration (IC50s) of 0.0685 and 0.0131 μg/ml, respectively. A trispecific containing 10E8-PGT121-PGDM1400 Env-specific binding sites was equally potent (median IC50of 0.0135 μg/ml), while a trispecific molecule targeting Env and CCR5 simultaneously (10E8Fab-PGDM1400fv-PRO 140fv) demonstrated even greater potency, with a median IC50of 0.007 μg/ml. By design, some of these molecules lacked Fc-mediated effector function; therefore, we also constructed a trispecific prototype possessing reconstituted CH2-CH3 domains to restore Fc receptor binding capacity. The molecules developed here, along with those described previously, possess promise as prophylactic and therapeutic agents against HIV.IMPORTANCEBroadly neutralizing antibodies (bNAbs) prevent HIV infection in monkey challenge models and suppress HIV replication in infected humans. Combinations of bNAbs are more effective at suppression, and antibody-like molecules engineered to have two or three bNAb combining sites also inhibit HIV replication in monkeys and other animal models. To expand the available array of multispecific HIV inhibitors, we designed single-component molecules that incorporate two (bispecific) or three (trispecific) bNAb binding sites that recognize the HIV envelope glycoprotein (Env) or the HIV coreceptor (CCR5) or that cross-target both Env and CCR5. Several of the bi- and trispecific molecules neutralized most viruses in a diverse cross-clade panel, with greater breadth and potency than those of the individual parental bNAbs. The molecules described here provide additional options for preventing or suppressing HIV infection.

scholarly journals Identification of myxobacteria-derived HIV inhibitors by a high-throughput two-step infectivity assay

2013 ◽  
Vol 12 (1) ◽  
pp. 85 ◽  
Author(s):  
Javier P Martinez ◽  
Bettina Hinkelmann ◽  
Eric Fleta-Soriano ◽  
Heinrich Steinmetz ◽  
Rolf Jansen ◽  
...  
Keyword(s):  
High Throughput ◽  
Infectivity Assay ◽  
Hiv Inhibitors

scholarly journals Probing Vulnerability of the gp41 C-Terminal Heptad Repeat as Target for Miniprotein HIV Inhibitors

2020 ◽  
Vol 432 (20) ◽  
pp. 5577-5592
Author(s):  
Samuel Jurado ◽  
Christiane Moog ◽  
Mario Cano-Muñoz ◽  
Sylvie Schmidt ◽  
Géraldine Laumond ◽  
...  
Keyword(s):  
Heptad Repeat ◽  
Hiv Inhibitors

Graphene Quantum Dots Based Systems As HIV Inhibitors

2018 ◽  
Vol 29 (9) ◽  
pp. 3084-3093 ◽  
Author(s):  
Daniela Iannazzo ◽  
Alessandro Pistone ◽  
Stefania Ferro ◽  
Laura De Luca ◽  
Anna Maria Monforte ◽  
...  
Keyword(s):  
Quantum Dots ◽  
Graphene Quantum Dots ◽  
Hiv Inhibitors
Sign in / Sign up

Export Citation Format

Share Document