HIV-1
HIV-1 is a retrovirus whose replication relies on reverse transcription of viral RNA into DNA, integrating into host genomes to produce progeny virions[1]. Viral entry is mediated by interactions between the envelope glycoprotein gp120 and the host CD4 receptor, along with chemokine co-receptors CXCR4 or CCR5, triggering membrane fusion and infection of target cells[2][3]. Post-entry, reverse transcription and integration involve complex protein-nucleic acid interactions, with viral integrase and nucleocapsid proteins directing efficient DNA synthesis[4]. The viral replication cycle engages host signaling pathways, including calcium-dependent activation cascades, nitric oxide signaling, and protein kinase C isoforms, which modulate viral transcription and assembly[5][6]. HIV-1 accessory proteins, such as Nef and Vif, interact with host factors to enhance replication and evade immune detection, establishing persistent infection[7]. Compared with related retroviruses, HIV-1 exhibits unique isoform-specific interactions of its envelope and regulatory proteins with host pathways, enabling differential cellular tropism and pathogenicity[1]. Small molecule inhibitors and peptide agonists targeting gp120-CD4 binding, integrase activity, or host signaling components have been employed to dissect viral replication mechanisms in vitro and in vivo, providing tools for experimental modulation of viral processes[8][9]. Mechanistically, selective modulation of these pathways has been used to evaluate antiviral efficacy and to define host determinants of infection, highlighting the functional distinctions among viral isoforms and their cellular interactions[10][11].
References:
- [1]. Downey GP, et al. Chemotactic peptide-induced activation of MEK-2, the predominant isoform in human neutrophils. Inhibition by wortmannin. J Biol Chem. 1996 Aug 30;271(35):21005-1011. [Content Brief]
- [2]. Boyé K, et al. Ligand activation induces different conformational changes in CXCR3 receptor isoforms as evidenced by plasmon waveguide resonance (PWR). Sci Rep. 2017 Sep 6;7(1):10703. [Content Brief]
- [3]. Karaś K, et al. The Dichotomous Nature of AZ5104 (an EGFR Inhibitor) Towards RORγ and RORγT. Int J Mol Sci. 2019 Nov 17;20(22):5780. [Content Brief]
- [4]. Maroney SA, et al. New insights into the biology of tissue factor pathway inhibitor. J Thromb Haemost. 2015 Jun;13 Suppl 1(0 1):S200-7. [Content Brief]
- [5]. Mourelle M, et al. The arginine/nitric oxide pathway modulates sphincter of Oddi motor activity in guinea pigs and rabbits. Gastroenterology. 1993 Nov;105(5):1299-305. [Content Brief]
- [6]. Liang C, et al. Rosiglitazone via upregulation of Akt/eNOS pathways attenuates dysfunction of endothelial progenitor cells, induced by advanced glycation end products. Br J Pharmacol. 2009 Dec;158(8):1865-73. [Content Brief]
- [7]. Kampa M, et al. Opioids are non-competitive inhibitors of nitric oxide synthase in T47D human breast cancer cells. Cell Death Differ. 2001 Sep;8(9):943-52. [Content Brief]
- [8]. Jing Q, et al. In search of potent and selective inhibitors of neuronal nitric oxide synthase with more simple structures. Bioorg Med Chem. 2013 Sep 1;21(17):5323-31. [Content Brief]
- [9]. Courilleau D, et al. The (R)-enantiomer of CE3F4 is a preferential inhibitor of human exchange protein directly activated by cyclic AMP isoform 1 (Epac1). Biochem Biophys Res Commun. 2013 Oct 25;440(3):443-8. [Content Brief]
- [10]. Shih CD. Activation of estrogen receptor beta-dependent nitric oxide signaling mediates the hypotensive effects of estrogen in the rostral ventrolateral medulla of anesthetized rats. J Biomed Sci. 2009 Jul 7;16(1):60. doi: 10.1186/1423-0127-16-60. PMID: 19583861; PMCID: PMC2717931. et al. Activation of estrogen receptor beta-dependent nitric oxide signaling mediates the hypotensive effects of estrogen in the rostral ventrolateral medulla of anesthetized rats. J Biomed Sci. 2009 Jul 7;16(1):60. [Content Brief]
- [11]. Larivière S, et al. Gonadotropin-releasing hormone inhibits pituitary adenylyl cyclase-activating polypeptide coupling to 3',5'-cyclic adenosine-5'-monophosphate pathway in LbetaT2 gonadotrope cells through novel protein kinase C isoforms and phosphorylation of pituitary adenylyl cyclase-activating polypeptide type I receptor. Endocrinology. 2008 Dec;149(12):6389-98. [Content Brief]
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HIV-1 Related Products (414)
Related Products (414)
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Elvitegravir
0 ImagesSynonyms: GS-9137; JTK-303; D06677Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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Atazanavir
0 ImagesSynonyms: BMS-232632Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
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Tat-beclin 1
0 ImagesTat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
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Sparstolonin B
0 ImagesSparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.
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Darunavir
0 ImagesSynonyms: TMC114; UIC-94017Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity.
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Fangchinoline
0 ImagesFangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
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Mavorixafor trihydrochloride
0 ImagesSynonyms: AMD-070 trihydrochloride; AMD-11070 trihydrochlorideMavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome.
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BRD3308
0 ImagesBRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
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5-(N,N-Hexamethylene)-amiloride
0 Images5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
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Nelfinavir Mesylate
0 ImagesSynonyms: AG 1343 MesylateNelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
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BRD-6929
0 ImagesBRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.
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L-α-Phosphatidylinositol
0 ImagesCat. No.: HY-W020658CAS No.: 97281-52-2
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Indinavir sulfate
0 ImagesSynonyms: MK-639; L735524Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor.
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Doravirine
0 ImagesSynonyms: MK-1439Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
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Tenofovir alafenamide fumarate
0 ImagesSynonyms: GS-7340 fumarateTenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
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Tizoxanide
0 ImagesSynonyms: TIZTizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.
