Indolizine Derivatives as <scp>HIV</scp>‐1 <scp>VIF</scp>–Elongin<scp>C</scp> Interaction Inhibitors

Huang, Wenlin; Zuo, Tao; Luo, Xiaoling; Jin, Hongwei; Liu, Zhenming; Yang, Zhenjun; Yu, Xianghui; Zhang, Liangren

doi:10.1111/cbdd.12119

Cited by 48 publications

(30 citation statements)

References 28 publications

(28 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Independent lead compounds have also been identified based on predicted fit into the Vif-binding pocket in ELOC, which would effectively outcompete the SLQ motif of Vif (Huang et al 2013a; Huang et al 2013b). However, the best of these indolizine type compounds has a modest IC50 value of 11 μM.…”

Section: Possible Avenues To Apobec3-based Therapeuticsmentioning

confidence: 99%

The APOBEC3 Family of Retroelement Restriction Factors

Refsland

Harris

2013

Current Topics in Microbiology and Immunology

171

219

View full text Add to dashboard Cite

The ability to regulate and even target mutagenesis is an extremely valuable cellular asset. Enzyme-catalyzed DNA cytosine deamination is a molecular strategy employed by vertebrates to promote antibody diversity and defend against foreign nucleic acids. Ten years ago, a family of cellular enzymes was first described with several proving capable of deaminating DNA and inhibiting HIV-1 replication. Ensuing studies on the apolipoprotein B mRNA-editing enzyme catalytic polypeptide-like 3 (APOBEC3) restriction factors have uncovered a broad-spectrum innate defense network that suppresses the replication of numerous endogenous and exogenous DNA-based parasites. Although many viruses possess equally elaborate counter-defense mechanisms, the APOBEC3 enzymes offer a tantalizing possibility of leveraging innate immunity to fend off viral infection. Here we focus on mechanisms of retroelement restriction by the APOBEC3 family of restriction enzymes and we consider the therapeutic benefits, as well as the possible pathological consequences, of arming cells with active DNA deaminases.

show abstract

Section: Possible Avenues To Apobec3-based Therapeuticsmentioning

confidence: 99%

The APOBEC3 Family of Retroelement Restriction Factors

Refsland

Harris

2013

Current Topics in Microbiology and Immunology

171

219

View full text Add to dashboard Cite

show abstract

“…The HIV genome also encodes four accessory factors (Vpr, Vpu, Vif, and Nef) essential for viral pathogenicity that represent alternative targets for drug discovery [2–4]. HIV-1 Nef is particularly attractive in this regard, because it is critical to the HIV life cycle in vivo and also promotes immune escape of HIV-infected cells.…”

Section: Introductionmentioning

confidence: 99%

Small molecule inhibitors of the HIV-1 virulence factor, Nef

Smithgall

Thomas

2013

Drug Discovery Today: Technologies

View full text Add to dashboard Cite

Summary Although antiretroviral therapy has revolutionized the clinical management of AIDS, life-long treatment is required because these drugs do not eradicate HIV-infected cells. Chronic antiretroviral therapy may not protect AIDS patients from cognitive impairment, raising important quality of life issues. Because of the rise of HIV strains resistant to current drugs and uncertain vaccine prospects, an urgent need exists for the discovery and development of new therapeutic approaches. This review is focused on one such approach, which involves targeting HIV-1 Nef, a viral accessory protein essential for AIDS pathogenesis.

show abstract

“…Following a SAR study, 49 indolizine derivatives were obtained and tested as potential HIV-1 infectivity factor inhibitors, one of which was found to exhibit an IC 50 value of 11 µM [67].…”

Section: Natural and Synthetic Indolizinesmentioning

confidence: 99%

Breakthroughs in Indole and Indolizine Chemistry – New Synthetic Pathways, New Applications

Ghinea¹,

Dinică²

2016

Scope of Selective Heterocycles From Organic and Pharmaceutical Perspective

View full text Add to dashboard Cite

Indole and indolizines heterocyclic aromatic compounds structurally and chemically isomeric with indoles are an important class of N-fused heterocyclic compounds due to their interesting biological and optical properties. Different strategies for generating diverse collections of small molecules with indole and indolizine moieties have been developed. They can be synthesized by means of classical and nonclassical pathways. The present study discusses the versatile nature of indole/indolizine derivatives, new green methods for their synthesis, their possible mechanism of action and also provides information about current/future prospects of the topics and different indole/indolizine derivatives in pharmaceutical/clinical trials. With the remarkable number of approved indole-containing drugs as well as the importance of the indolizine moiety, it can be easily concluded that indole and indolizine derivatives offer perspectives on how pyrrole scaffolds might be exploited in the future as bioactive molecules against a broad range of diseases.

show abstract

Indolizine Derivatives as HIV‐1 VIF–ElonginC Interaction Inhibitors

Cited by 48 publications

References 28 publications

The APOBEC3 Family of Retroelement Restriction Factors

The APOBEC3 Family of Retroelement Restriction Factors

Small molecule inhibitors of the HIV-1 virulence factor, Nef

Breakthroughs in Indole and Indolizine Chemistry – New Synthetic Pathways, New Applications

Contact Info

Product

Resources

About