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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Apricitabine
0 ImagesSynonyms: SPD754; AVX754Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection.
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EFdA-TP tetraammonium
0 ImagesCat. No.: HY-138561AEFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms. EFdA-TP (tetraammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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EFdA-TP tetrasodium
0 ImagesCat. No.: HY-138561BCAS No.: 2883783-00-2EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1 RT with multiple mechanisms. EFdA-TP (tetrasodium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Pentosan Polysulfate
0 ImagesCat. No.: HY-A0203CAS No.: 37300-21-3
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ICeD-2
0 ImagesCat. No.: HY-151871CAS No.: 3050598-72-3ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs.
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HIV-1 integrase inhibitor
0 ImagesCat. No.: HY-13025CAS No.: 544467-07-4HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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3'-Azido-3'-deoxy-5-methylcytidine
0 Images3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells. 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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NBD-557
0 ImagesNBD-557 is a potentially HIV-1 inhibitor.
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Azt-pmap
0 ImagesAzt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection. Azt-pmap is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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(Z)-9-Propenyladenine
0 ImagesCat. No.: HY-100079ACAS No.: 1464851-21-5Synonyms: (Z)-Mutagenic Impurity of Tenofovir Disoproxil(Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
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FGI-106
0 ImagesCat. No.: HY-124618CAS No.: 501081-38-5FGI-106 is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively.
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Methyl-Hesperidin (Standard)
0 ImagesCat. No.: HY-N0165RCAS No.: 11013-97-1Methyl-Hesperidin (Standard) is the analytical standard of Methyl-Hesperidin (HY-N0165). This product is intended for research and analytical applications. Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs.
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Efavirenz-13C6
0 ImagesSynonyms: DMP 266-13C6; EFV-13C6; L-743726-13C6Efavirenz-13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
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Raltegravir sodium
0 ImagesCat. No.: HY-10353BCAS No.: 1292804-07-9Synonyms: MK 0518 sodiumRaltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
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NBD-14189
0 ImagesNBD-14189 is a potent HIV-1 entry antagonist with an IC50 of 89 nM against the HIV-1HXB2 pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC50<200 nM).
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Orthosporin
0 ImagesCat. No.: HY-W751002CAS No.: 118063-79-9Synonyms: (+)-OrthosporinOrthosporin ((+)-Orthosporin), a phytotoxic isocoumarin compound, is a microbial secondary metabolite. Orthosporin can be isolated from the endophytic fungus Lasiodiplodia tbeobromae. Orthosporin has potent antibacterial activity against B. subtilis, E. coli and P. aeruginosa. Orthosporin also has antioxidant activity against DPPH radical and antiviral activities with inhibition of HIV-1 reverse transcriptase activity.
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DPC 684
0 ImagesCat. No.: HY-171835CAS No.: 284661-73-0DPC 684 is a potent and selective HIV-1 protease inhibitor (IC90 = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC90 = 1.9-6.3 nM). DPC 684 has research significance for HIV.
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HIV-1 inhibitor-51
0 ImagesCat. No.: HY-152161CAS No.: 2834087-82-8HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056).
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Wikstrol A
0 ImagesCat. No.: HY-N10958CAS No.: 159736-35-3Wikstrol A is a potent antifungal, antimitotic and anti-HIV-1 Agent. Wikstrol A induces morphological deformation of P. oryzae mycelia with an MMDC value of 70.1 µM. Wikstrol A shows activity against microtubule polymerization with an IC50 value of 131 µM. Wikstrol A shows anti-HIV-1 activity with an IC50 value of 67.8 µM.
