Antibody–Bactericidal Macrocyclic Peptide Conjugates To Target Gram‐Negative Bacteria
Sign Up to like & getrecommendations! Published in 2018 at "ChemBioChem"
DOI: 10.1002/cbic.201800295
Abstract: To combat antimicrobial infections, new active molecules are needed. Antimicrobial peptides, ever abundant in nature, are a fertile starting point to develop new antimicrobial agents but suffer from low stability, low specificity, and off‐target toxicity.… read more here.
Keywords: peptide conjugates; macrocyclic peptide; antibody; antibody bactericidal ... See more keywords
Evaluation of a Radiolabeled Macrocyclic Peptide as Potential PET Imaging Probe for PD−L1
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200091
Abstract: The interaction between the immune checkpoint PD‐1 and PD−L1 promotes T‐cell deactivation and cancer proliferation. Therefore, immune checkpoint inhibition therapy, which relies on prior assessment of the target, has been widely used for many cancers.… read more here.
Keywords: peptide potential; radiolabeled macrocyclic; potential pet; macrocyclic peptide ... See more keywords
Macrocyclic peptide construction through C–H activation strategy
Sign Up to like & getrecommendations! Published in 2018 at "Science Bulletin"
DOI: 10.1016/j.scib.2018.09.008
Abstract: Peptides are biomolecules that commonly engage in biological activities of native bio-systems, and have also been inspiringly investigated, synthesized and utilized by human beings for clinical purposes. The function of a peptide is typically dependent… read more here.
Keywords: activation strategy; macrocyclic peptide; peptide construction; construction activation ... See more keywords
Identification of Macrocyclic Peptide Families from Combinatorial Libraries Containing Noncanonical Amino Acids Using Cheminformatics and Bioinformatics Inspired Clustering.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical biology"
DOI: 10.1021/acschembio.3c00159
Abstract: In the past decade, macrocyclic peptides gained increasing interest as a new therapeutic modality to tackle intracellular and extracellular therapeutic targets that had been previously classified as "undruggable". Several technological advances have made discovering macrocyclic… read more here.
Keywords: amino acids; identification; peptide; macrocyclic peptide ... See more keywords
Design and Evolution of a Macrocyclic Peptide Inhibitor of the Sonic Hedgehog/Patched Interaction.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.7b06087
Abstract: The hedgehog (Hh) signaling pathway plays a central role during embryonic development, and its aberrant activation has been implicated in the development and progression of several human cancers. Major efforts toward the identification of chemical… read more here.
Keywords: peptide; patched interaction; macrocyclic peptide; hedgehog ... See more keywords
A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation
Sign Up to like & getrecommendations! Published in 2023 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2220012120
Abstract: Significance We have used an established in vitro cyclic peptide selection strategy to generate a novel inhibitor of multidrug resistance protein 1 (MRP1), an ABC transporter implicated in cancer drug resistance. Multiple small-molecule MRP1 inhibitors… read more here.
Keywords: inhibitor traps; inhibitor; peptide; peptide inhibitor ... See more keywords
Abstract B018: The development of macrocyclic peptide Ras inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Molecular Cancer Research"
DOI: 10.1158/1557-3125.ras23-b018
Abstract: While there has been tremendous progress developing small molecule covalent K-Ras G12C inhibitors that bind Ras-off (GDP) and inhibit nucleotide exchange, there remains a need for additional K-Ras inhibitors with different Ras isoform/mutant selectivity profiles… read more here.
Keywords: ras inhibitors; peptide; macrocyclic peptide; ras ... See more keywords
Structural Characterization of a Macrocyclic Peptide Modulator of the PD-1/PD-L1 Immune Checkpoint Axis
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26164848
Abstract: The clinical success of PD-1/PD-L1 immune checkpoint targeting antibodies in cancer is followed by efforts to develop small molecule inhibitors with better penetration into solid tumors and more favorable pharmacokinetics. Here we report the crystal… read more here.
Keywords: structural characterization; immune checkpoint; macrocyclic peptide; characterization macrocyclic ... See more keywords