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ENTITY | POTENCY | SAFETY INFORMATION | EVIDENCE | PMID |
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C20-Jp-Hp, Antiviral peptides generated by conjugating two known short antiviral peptides: part-1 (named Jp with the sequence of ARLPR) and part-2 (named Hp with the sequence of KKWK) | The anti-IAV screening results identified that C20-Jp-Hp was the most potent peptide with IC50 value of 0.53 microM against A/Puerto Rico/8/34 (H1N1) strain. | Herein, we show a new class of antiviral peptides generated by conjugating two known short antiviral peptides: part-1 (named Jp with the sequence of ARLPR) and part-2 (named Hp with the sequence of KKWK). | 26952867 | |
Tripeptide GPG-NH2 | Inhibits the replication of HIV-1, 50% inhibitory concentrations values were 2.7 to 37 microM | CONCLUSIONS: The tripeptide GPG-NH2 is a nontoxic compound that inhibits the replication of HIV-1 by an apparently new mode of action. Glycyl-prolyl-glycine-NH2 might prove useful by itself or as a lead compound for the treatment of drug-resistant HIV-1. | 11213928 | |
P-1946 | Specific HIV-1 protease inhibitor that has potent and selective in vitro antiviral activity (EC50 152 nM) against a range of isolates resistant to commercially available protease inhibitors. | Antiviral activity and cross-resistance profile of P-1946, a novel human immunodeficiency virus type 1 protease inhibitor. The HIV protease inhibitor P-1946 is a member of a novel family of l-Lysine derivatives. | 16473417 | |
T-20EK - T-20 (enfuvirtide) through engineered electrostatic interactions between glutamic acid (E) and lysine (K) substitutions. | Anti-HIV-1 | HIV-1 resistance mechanism to an electrostatically constrained peptide fusion inhibitor that is active against T-20-resistant strains. T-20EK is a novel fusion inhibitor designed to have enhanced ?-helicity over T-20 (enfuvirtide) through engineered electrostatic interactions between glutamic acid (E) and lysine (K) substitutions. | 23689710 | |
King cobra cathelicidin (OH-CATH) | Both L- and D-OH-CATH30 showed higher efficacy against (toward) Gram-positive bacteria and stronger antibacterial activity against nearly all Gram-negative bacteria tested compare with antibiotics. | King cobra peptide OH-CATH30 as a potential candidate drug through clinic drug-resistant isolates. Cationic antimicrobial peptides (AMPs) are considered as important candidate therapeutic agents, which exert potent microbicidal properties against bacteria, fungi and some viruses. | 29515090 | |
PIE12-trimer | First D-peptide HIV entry inhibitor with the breadth and potency required for clinical use. | D-peptides (peptides composed of D-amino acids) are promising therapeutic agents due to their insensitivity to protease degradation. PIE12-trimer was designed using structure-guided mirror-image phage display and linker optimization and is the first D-peptide HIV entry inhibitor with the breadth and potency required for clinical use. | 20719956 | |
Series of oligomeric HR2 peptides with increased helical structure and with exceptionally high HR1/HR2 bundle stability | The engineered peptides are found to be as much as 3,600-fold more active than ENF against viruses that are resistant to the HR2 peptides ENF, T-1249, or T-651. | Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus. Enfuvirtide (ENF), the first approved fusion inhibitor (FI) for HIV, is a 36-aa peptide that acts by binding to the heptad repeat 1 (HR1) region of gp41 and preventing the interaction of the HR1 and HR2 domains, which is required for virus-cell fusion. | 17640899 | |
Muramyl dipeptide (MDP) | MDP exhibited an inhibitory activity against HIV infection of CD4+ H9 lymphocytes and U937 monocytoid cells. | Muramyl dipeptide inhibits replication of human immunodeficiency virus in vitro. An inhibitor of viral reverse transcriptase, 2', 3'-dideoxyadenosine, produced potent inhibition in cultures which were similarly infected with HIV. | 2111159 | |
SC34EK | Demonstrates remarkably potent inhibition of membrane fusion by the resistant HIV-1 variants as well as wild-type viruses. | Electrostatically constrained alpha-helical peptide inhibits replication of HIV-1 resistant to enfuvirtide. In particular, the modified peptide, SC34EK, demonstrates remarkably potent inhibition of membrane fusion by the resistant HIV-1 variants as well as wild-type viruses. | 18834950 | |
Fatty acid-conjugated lipopeptide named LP-11 | Showed potent and broad inhibitory activity against diverse primary HIV-1 isolates and clinically drug-resistant mutants, and it had dramatically increased ex-vivo antiviral activity and extended half-life. | DESIGN: On the basis of the M-T hook structure, we recently developed a short-peptide named HP23, which mainly targets the deep pocket site of gp41 and possesses highly potent antiviral activity. | 26919736 | |
Aza-dipeptide analogues [8 aza-dipeptide analogues carrying N-(bis-aryl-methyl) substituents on the (hydroxethyl)hydrazine moiety] | Potent and orally absorbed HIV-1 protease inhibitors, candidates for clinical development | New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development. | 9719591 | |
Albuvirtide (ABT), a 3-maleimimidopropionic acid-modified peptide fusion inhibitor | ABT had potent inhibitory activity against the subtypes A, B and C that predominate the worldwide AIDS epidemics, and subtype B', CRF07_BC and CRF01_AE recombinants that are currently circulating in China. | The results showed that ABT had potent inhibitory activity against the subtypes A, B and C that predominate the worldwide AIDS epidemics, and subtype B', CRF07_BC and CRF01_AE recombinants that are currently circulating in China. | 22403678 | |
Ancestral peptide (named P3) | mean IC50, 63.8 nmol/l | CONCLUSION: P3 is an HIV-2/SIV ancestral peptide with low antigenicity, high stability, and potent activity against both HIV-1, including variants resistant to T-20, and HIV-2. | 23324659 | |
Artificial peptides containing four heptad repeats (m4HR) conjugated with a pocket-specific small molecule (pssm) or pssm and cholesterol (chol) [pssm-m4HR or pssm-m4HR-chol] | pssm-m4HR conjugates exhibited promising inhibitory activity against HIV-1 Env-mediated cell-cell fusion and laboratory-adapted HIV-1 replication with IC50 values at the low micromolar level, whereas the pssm-m4HR-chol conjugates exhibited dramatically increased anti-HIV-1 activities with IC50 values at the low nanomolar level. Some of the pssm-m4HR-chol conjugates (e.g. 5a and 5b) showed highly potent antiviral activity against infection by primary HIV-1 isolates and enfuvirtide-resistant HIV-1 strains. | No or low cytotoxicity towards MT-2 cells | These results suggest this scaffold design is a promising strategy for developing novel peptide conjugates with improved antiviral activity against a broad spectrum of HIV-1 strains, including those highly resistant to enfuvirtide. | 24500189 |
p5RD(D-form of heparan sulfate binding peptide) | Reduce HCMV infectivity in vitro including GCV resistant HCMVs and MCMV infection | In an effort to develop novel CMV treatments, we tested the effectiveness of the D-form of a novel heparan sulfate binding peptide, p5RD, at reducing infection of ganciclovir (GCV) resistant HCMVs in vitro and MCMV in vivo. | 27678155 | |
SK&F 107647 | Increase natural host resistance to infections caused by both gram-negative and gram-positive bacteria. | Treatment of experimental gram-negative and gram-positive bacterial sepsis with the hematoregulatory peptide SK&F 107647. SK&F 107647, a novel synthetic low-molecular-weight peptide, has demonstrated potent antiinfective activities in murine models of fungal and viral infection. | 8537660 | |
P3 and an arginine-substituted analog, JH-3 | Potent antimicrobial activities against drug-resistant strains by disrupting and penetrating the bacterial cytoplasmic membrane | P3, a novel hemoglobin peptide derived from bovine erythrocytes, exhibited modest antimicrobial activity in vitro. | 25753638 | |
Labyrinthopeptin A1 (LabyA1) | LabyA1 exhibited a consistent and broad anti-HIV activity (EC50s: 0.70-3.3 microM) and anti-HSV activity (EC50s: 0.29-2.8 microM) in cell cultures. LabyA1 also inhibited viral cell-cell transmission between persistently HIV-infected T cells and uninfected CD4(+) T cells (EC50?2.5 microM) and inhibited the transmission of HIV captured by DC-SIGN(+)-cells to uninfected CD4(+) T cells (EC50?4.1 microM). | LabyA1 can be considered as a novel lead peptide as it had profound antiviral activity against HIV and HSV. | 23724015 | |
Peptide (6a) | Among the peptides synthesized and evaluated, a lead peptide (6a) with potent activity (IC50: 4.4nM) was identified against the MDR769 HIV-1 protease. | Design, synthesis and evaluation of a potent substrate analog inhibitor identified by scanning Ala/Phe mutagenesis, mimicking substrate co-evolution, against multidrug-resistant HIV-1 protease. | 23921229 |