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  • peptide
  • A gp41-derived peptide, T-20, efficiently inhibits HIV fusion and is currently approved for treatment of HIV-infected individuals. (asm.org)
  • To elucidate the mechanism in detail, we generated variants resistant to C34, a peptide derived from the gp41 carboxyl terminus heptad repeat (C-HR) in vitro. (asm.org)
  • Peptide inhibitors that block human immunodeficiency virus type 1 (HIV-1) fusion were first reported by Wild et al. (asm.org)
  • 30 ). Recently, a peptide fusion inhibitor (T-20 or enfuvirtide) has been approved in the United States and Europe for treatment of HIV-infected individuals. (asm.org)
  • The peptide sequence of T-20 is derived from the gp41 C terminus heptad repeat (C-HR) sequence, which corresponds to a linear region of 36 amino acids, and T-20 inhibits fusion by binding to the N-terminal heptad repeat (N-HR) of gp41 and preventing 6-helix bundle formation ( 4 , 30 ). (asm.org)
  • To elucidate the mechanism of resistance to the peptide fusion inhibitors, we generated and characterized HIV-1 variants resistant to C34, a gp41 C-HR-derived peptide ( 2 , 22 ) (Fig. 1A ). (asm.org)
  • The formyl peptide receptor 2 (FPR2) is a remarkably versatile transmembrane protein belonging to the G-protein coupled receptor (GPCR) family. (mdpi.com)
  • FPR2 is activated by an array of ligands, which include structurally unrelated lipids and peptide/proteins agonists, resulting in different intracellular responses in a ligand-specific fashion. (mdpi.com)
  • Formyl-peptide receptors 1, 2 and 3 (FPR1, FPR2 and FPR3) form a subgroup of receptors linked to inhibitory G-proteins (G i ). (mdpi.com)
  • We previously showed that a gp41 peptide (3S) induces expression of a natural killer (NK) ligand (NKp44L) on CD4+ T cells during HIV-1 infection and that those cells are highly sensitive to NK lysis. (natap.org)
  • In this study, it is shown that a classic chemotactic factor, the bacterial chemotactic peptide N-formyl-methionyl-leucylphenyl-alanine (fMLF), rapidly induced a protein-kinase-C-mediated serine phosphorylation and down-regulation of the chemokine receptor CCR5, which serves as a major human immunodeficiency virus (HIV)-1 coreceptor. (bloodjournal.org)
  • The fMLF binding to its receptor, formyl peptide receptor (FPR), resulted in significant attenuation of cell responses to CCR5 ligands and in inhibition of HIV-1-envelope-glycoprotein-mediated fusion and infection of cells expressing CD4, CCR5, and FPR. (bloodjournal.org)
  • 6-10 Human monocytes express a wide variety of 7-transmembrane (STM), G-protein-coupled chemoattractant receptors including chemokine receptors and the receptors for classic chemotactic factors such as the bacterial chemotactic peptide N-formyl-methionyl-leucyl-phenylalanine (fMLF), activated complement component 5 (C5a), and leukotriene B4 (LTB4). (bloodjournal.org)
  • This study shows that CCR5 in monocytes can be rapidly phosphorylated and subsequently desensitized by stimulation of the cells with the bacterial chemotactic peptide fMLF, causing reduced cell susceptibility to HIV-1 entry and infection. (bloodjournal.org)
  • We used X-ray crystallography to determine the structure of the protease-resistant part of a gp41 ectodomain solubilized with a trimeric GCN4 coiled coil in place of the amino-terminal fusion peptide. (nih.gov)
  • Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells. (nih.gov)
  • Researchers combined adnectins targeting the CD4 cell surface receptor and HIV's gp41 protein subunit, along with a peptide fusion inhibitor, to build a so-called 'combinectin' inhibitor which uses independent mechanisms to interfere with three routes of HIV entry. (nhivna.org)
  • The EC50, or 50% effective concentration, of the anti-CD4 adnectin, the anti-gp41 adnectin and the fusion inhibitor peptide were 8.5, 5.4 and 0.4 nM (nanoMolar), respectively. (nhivna.org)
  • Gallaher, W.R. (1987) Detection of a fusion peptide se-quence in the transmembrane protein of human immu-nodeficiency virus. (scirp.org)
  • We show for the first time that two trimeric forms of glycosylated gp41 released from transfected human cells modulated expression of cytokines and other genes in human PBMCs in the same manner, but at least seven hundred-fold stronger compared to that induced by the isu peptide. (biomedcentral.com)
  • Humans
  • Many of those studies demonstrate that neutralizing Abs can protect against HIV-1 infection in vitro and in animal models, but in vivo proof of their activity in infected humans remains circumstantial (9, 10). (natap.org)
  • Researchers concluded that the first transmission of SIV to HIV in humans took place around 1920 in Kinshasa in the Democratic Republic of Congo, Central Africa. (slideshare.net)
  • The human immunodeficiency virus (HIV) is a lentivirus (slowly replicating retrovirus) that causes the acquired immunodeficiency syndrome (AIDS), a condition in humans in which progressive failure of the immune system allows life-threatening opportunistic infections and cancers to thrive. (creative-diagnostics.com)
  • required to induce
  • This conformation is due to an connection of the C-terminal helical region (CHR) with the N-terminal Hematoxylin helical region (NHR) in an antiparallel manner forming a six-helix package.5-7 The conformation of gp41 required to induce bnAbs is still unfamiliar although either prehairpin or six-helix bundle formation is most likely to be targeted. (exposed-skin-care.net)
  • sequence
  • Alignments of gp41 and p15E showed a sequence homology within the MPER (F/YEGWFN in the case of gammaretroviruses and NWFNIT, the 4E10 epitope, in case of HIV-1) despite the evolutionary distance between PERV and HIV-1. (fu-berlin.de)
  • membranes
  • Interaction of the intermembrane space domain of Tim23 protein with mitochondrial membranes. (mpg.de)
  • Water penetration profile at the protein-lipid interface in Na,K-ATPase membranes. (mpg.de)
  • fusion inhibitors
  • Current research includes the development of assays for the detection, evaluation and development of fusion inhibitors against HIV. (tu.edu)
  • epitope
  • Despite the precise recognition of the 2F5 epitope no or very fragile neutralization of HIV-1NL4-3 from the immune sera was shown. (exposed-skin-care.net)
  • Based on these findings, both epitope regions of p15E recognized by neutralizing sera were substituted by corresponding sequences derived from gp41 of HIV-1. (fu-berlin.de)
  • Immunization
  • The fourth and fifth supernatant fractions comprising purified proteins N1 or N2 were dialyzed against double distilled water (ddH2O) and utilized for immunization. (exposed-skin-care.net)
  • Weak MPER-specific antibody responses were observed in rat sera after immunization with N2, these immune sera did not inhibit HIV-1NL4-3 infection. (fu-berlin.de)
  • inhibition
  • revealed that three continuous amino acids in the N-HR (GIV at positions 36 to 38 of gp41) were crucial for the inhibition of HIV-1 entry by T-20 and for efficient association between N-HR and T-20 in vitro ( 26 ). (asm.org)
  • membrane fusion
  • Cleavage mediated by a cellular furin protease during the protein transport through the cis or medial Golgi appears to be mandatory for membrane fusion ( 18 , 29 , 42 , 57 , 66 ). (asm.org)
  • Infections
  • A long-acting bio-engineered molecule with a triple mechanism of action demonstrated potent antiviral activity and worked against HIV that developed resistance to any one of the three mechanisms in a laboratory study, and lowered viral load in humanised mice, according to research presented at the Conference on Retroviruses and Opportunistic Infections (CROI 2016) last month in Boston. (nhivna.org)
  • prevention
  • Colostrum is a rich source of readily accessible mucosal B cells that may help define the mucosal antibody response contributing to prevention of postnatal HIV-1 transmission. (nih.gov)
  • mucosal
  • However, shortly after induction, these initial mucosal gp41 Env IgA Abs rapidly declined with a t(1/2) of ∼2.7 days. (biomedsearch.com)
  • cellular
  • The interaction of Vpr with the cellular protein UNG2 is a key event in various stages of retroviral replication and its role remains to be defined. (springer.com)
  • functional
  • Envelopes that contained residues with bulky hydrophobic side chains instead of cysteines retained their association with heavy rafts and were nearly fully functional for incorporation into virions and infectivity. (umassmed.edu)
  • Toward the functional oligomerization state of tryptophan-rich sensory proteins. (mpg.de)
  • Functional domains of gp41 of HIV-1, location and alignment of the immunosuppressive (isu) domains of different retroviruses. (biomedcentral.com)
  • retroviruses
  • 10 , 11 ] demonstrated that the TM proteins of different retroviruses, including MuLV and the human endogenous virus HERV-FRD (syncytin 2, that is expressed in the human placenta), are immunosuppressive in vivo . (biomedcentral.com)