• DRAMP ID

    • DRAMP21540
    • Peptide Name

    • Pleu(i+4)1,15(A9K)
    • Sequence

    • GⓍGSFⓍKKKAHVGKHⓍGKAⓍLTHYL
    • Sequence Length

    • 25
    • Original Sequence

    • GWGSFFKKAAHVGKHVGKAALTHYL
    • Source

    • Synthetic construct
    • SMILES

    • O=C(NC(C(=O)NC(C(=O)NC(C=O)CC(C)C)Cc1ccc(O)cc1)Cc1nc[nH]c1)C(NC(=O)C(NC(=O)C1(C)NC(=O)C(C)NC(=O)C(CCCC[NH3+])NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(C)NC(=O)C(Cc3ccccc3)NC(=O)C(CO)NC(=O)CNC(=O)C(NC(=O)C[NH3+])(C)CCCC=CCCC2)CCCC[NH3+])CCCC[NH3+])CCCC[NH3+])C)Cc2[nH]cnc2)C(C)C)CCCC[NH3+])Cc2nc[nH]c2)(C)CCCC=CCCC1)CC(C)C)C(O)C
    • Biological Activity

    • Antimicrobial, Antibacterial, Anti-Gram+, Anti-Gram-
    • Comments

    • Function: Antibacterial activity against Gram-positive and Gram-negative bacteria.
    • Target Organism

      • [Ref.31427820] Gram-positive bacteria: Staphyolococcus aureus ATCC 25923 (MIC = 3.13 μg/mL), Bacillus cereus ATCC 14579 (MIC = 3.13 μg/mL);
      • Gram-negative bacteria: Escherichia coli ATCC 25922 (MIC = 1.56 μg/mL), Pseudomonas aeruginosa ATCC 27853 (MIC = 1.56 μg/mL)
    • Hemolytic Activity

      • [Ref.31427820] It has 17.1% hemolysis against human red blood cells at 25 μg/mL.
    • Cytotoxicity

    • No cytotoxicity information found in the reference(s) presented
    • Linear/Cyclic

    • Cyclic (Stapled)
    • N-terminal Modification

    • Free
    • C-terminal Modification

    • Amidation
    • Special Amino Acid and Stapling Position

    • ①The Ⓧ (position: 2, 6, 16 and 20) in sequence indicates S5 stapling amino acid. Note: S5 is (S)-pentenyl alanine. ②Ⓧ (2) and Ⓧ (6), Ⓧ (16) and Ⓧ (20) are cross-linked by hydrocarbon stapling respectively.
    • Stereochemistry

    • L
    • Secondary Structure

    • α-helix in potassium phosphate buffer.
    • Structure Description

    • No other descriptive information about the structure found in the literature
  • There is no predicted structure for DRAMP21540.
  • Literature 1
    • Title

    • Design of stapled antimicrobial peptides that are stable, nontoxic and kill antibiotic-resistant bacteria in mice
    • Reference

    • Nat Biotechnol. 2019 Oct;37(10):1186-1197. doi: 10.1038/s41587-019-0222-z. Epub 2019 Aug 19.
    • Author

    • Rida Mourtada, Henry D Herce, Daniel J Yin, Jamie A Moroco, Thomas E Wales, John R Engen, Loren D Walensky