Naphthalene sulfonate polymers with CD4-blocking and anti-human immunodeficiency virus type 1 activities

Rusconi, Stefano; Moonis, Mona; Merrill, Debra P.; Pallai, Peter V.; Neidhardt, E A; Singh, Sunit K.; Willis, K J; Osburne, Marcia S.; Profy, Albert T.; Jenson, James C.; Hirsch, M. S.

doi:10.1128/aac.40.1.234

Cited by 143 publications

(64 citation statements)

References 18 publications

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“…PIs are generally less sensitive than TCLA HIV-1 to inhibition by polyanions [22,29,30]. TCLA HIV-1 acquire a more basic V3 loop on passage through cell lines increasing virus susceptibility to polyanions [9,22,31], whereas X4 primary isolates that have not been passaged thus have less basic V3 loops [8,31].…”

Section: Discussionmentioning

confidence: 99%

Structural features and anti-HIV-1 activity of novel polysaccharides from red algae Grateloupia longifolia and Grateloupia filicina

Wang

Bligh

Shi

et al. 2007

International Journal of Biological Macromolecules

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Section: Discussionmentioning

confidence: 99%

Structural features and anti-HIV-1 activity of novel polysaccharides from red algae Grateloupia longifolia and Grateloupia filicina

Wang

Bligh

Shi

et al. 2007

International Journal of Biological Macromolecules

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“…Compounds tested were Advantage-S, a 3.5% N-9 product; 2% PRO 2000 gel; and hydroxyethylcellulose (HEC) gel. Advantage-S was selected because it has been extensively studied in human clinical trials; 2% PRO 2000, a naphthalene sulfonic acid polymer that blocks HSV and HIV entry [17][18][19], was selected because it is currently in phase 2 and 3 clinical trials; and HEC was selected because it is being used in several clinical trials as a placebo gel.…”

mentioning

confidence: 99%

A Comprehensive Murine Model to Evaluate Topical Vaginal Microbicides: Mucosal Inflammation and Susceptibility to Genital Herpes as Surrogate Markers of Safety

Galen¹,

Martín²,

Hazrati³

et al. 2007

J INFECT DIS

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A critical gap in microbicide development is the absence of surrogate safety markers. The objective of the present study was to develop a murine model to examine the mucosal response to microbicides and to assess the functional implication of observed changes. Mice received 14 daily intravaginal doses of nonoxynol-9, PRO 2000, or placebo gel. Nonoxynol-9 induced an inflammatory response characterized by increases in levels of cytokines and chemokines, recruitment of neutrophils and monocytes into the genital tract, and activation of the transcription factors NF- kappa B and activator protein-1. Minimal inflammation was observed in response to 2% PRO 2000. Nonoxynol-9-treated mice were significantly more susceptible to challenge with a low dose of herpes simplex virus type 2; the response of PRO 2000-treated mice was similar to the response to placebo. These findings suggest that PRO 2000 has little deleterious effect on mucosal immunity and, if validated by clinical experiences, support the inclusion of this model in the preclinical evaluation of future candidate microbicides.

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“…PRO 2000 is a naphthalene sulfate polymer that has been shown to bind to CD4 (Rusconi et al, 1996). Encouraging reports on safety and tolerance (Mayer et al, 2003) led to preclinical studies on vaginal explants (Keller et al, 2006) as well as clinical trials.…”

Section: Nonspecific Microbicidesmentioning

confidence: 97%

Vaccines and Microbicides Preventing HIV-1, HSV-2, and HPV Mucosal Transmission

Nikolic

Piguet

2010

Journal of Investigative Dermatology

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HIV-1, herpes simplex virus type 2 (HSV-2), and human papillomavirus (HPV), among other sexually transmitted infections, represent a major burden for global health. Initial insights into the mucosal transmission of these viral pathogens have raised optimism with regard to the rapid generation of protective vaccines. Nevertheless, setbacks for HIV-1 and HSV-2 vaccines have seriously challenged the initial enthusiasm. Recently, two new vaccines that efficiently prevented HPV infection have renewed the hope that vaccinal prevention of viral mucosal sexually transmitted infections is possible. HIV-1 and HSV-2 differ from HPV, and each virus needs to be tackled with a distinct approach. However, vaccines are not the only possible answer. Topically applied agents (microbicides) are an attractive alternative in the prevention of HIV-1 and HSV-2 mucosal transmission. Progress in understanding the mechanisms of genital transmission of HIV-1 and HSV-2 is required for successful vaccine or microbicide candidates to emerge from current approaches.

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Naphthalene sulfonate polymers with CD4-blocking and anti-human immunodeficiency virus type 1 activities

Cited by 143 publications

References 18 publications

Structural features and anti-HIV-1 activity of novel polysaccharides from red algae Grateloupia longifolia and Grateloupia filicina

Structural features and anti-HIV-1 activity of novel polysaccharides from red algae Grateloupia longifolia and Grateloupia filicina

A Comprehensive Murine Model to Evaluate Topical Vaginal Microbicides: Mucosal Inflammation and Susceptibility to Genital Herpes as Surrogate Markers of Safety

Vaccines and Microbicides Preventing HIV-1, HSV-2, and HPV Mucosal Transmission

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