Results 21 to 30 of about 10,137 (233)

Nano-G<sub>s</sub> Protein Peptidomimetics: Rational Design of Gα C-Terminus-Derived Peptides Mimicking Key Components of G<sub>s</sub>-β<sub>2</sub>AR Interactions. [PDF]

open access: yesAngew Chem Int Ed Engl
G protein‐coupled receptors (GPCRs) are major therapeutic targets. Modulating GPCR activity through intracellular sites is evolving. A structure‐ and computation‐assisted approach generated small G protein‐derived peptidomimetics targeting the intracellular binding crevice of the β2 adrenergic receptor mimicking features of the full G protein.
Tran PT   +11 more
europepmc   +2 more sources

Universal Peptidomimetics [PDF]

open access: yesJournal of the American Chemical Society, 2010
This paper concerns peptidomimetic scaffolds that can present side chains in conformations resembling those of amino acids in secondary structures without incurring excessive entropic or enthalpic penalties. Compounds of this type are referred to here as minimalist mimics.
Eunhwa, Ko   +5 more
openaire   +2 more sources

Synthesis of Isopeptide Epoxide Peptidomimetics

open access: yes, 2016
Two epoxide-containing peptidomimetics of the isopeptide, glutamyl-γ-glutamate, have been synthesized via a route that should be generally applicable to the synthesis of isopeptide analogues in which an oxirane replaces the scissile peptide bond. Enzymes
Matthew D. Alexander (1444090)   +2 more
core   +6 more sources

Pharmacological targeting of Sam68 functions in colorectal cancer stem cells

open access: yesiScience, 2021
Summary: Cancer stem cells (CSCs) are documented to play a key role in tumorigenesis and therapy resistance. Despite significant progress in clinical oncology, CSC reservoirs remain elusive and difficult to eliminate.
Angelique N. Masibag   +9 more
doaj   +1 more source

Non-Canonical Amino Acids as Building Blocks for Peptidomimetics: Structure, Function, and Applications

open access: yesBiomolecules, 2023
This review provides a fresh overview of non-canonical amino acids and their applications in the design of peptidomimetics. Non-canonical amino acids appear widely distributed in nature and are known to enhance the stability of specific secondary ...
Tarsila G. Castro   +4 more
doaj   +1 more source

Rational design, synthesis and structural characterization of peptides and peptidomimetics to target Hsp90/Cdc37 interaction for treating hepatocellular carcinoma

open access: yesComputational and Structural Biotechnology Journal, 2023
Heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) work together as a molecular chaperone complex to regulate the activity of a multitude of client protein kinases.
Surya Sukumaran   +7 more
doaj   +1 more source

Peptides and peptidomimetics as prototypes [PDF]

open access: yesCurrent Opinion in Chemical Biology, 2008
Since the unraveling of the structure of the α-helix [1] and β-sheet [2] by smart modeling, the use of peptides and their mimetics has been a highly fruitful approach that continues to attract natural scientists. These molecules occupy a privileged place in chemical biology, being both readily accessible via chemical synthesis and directly relevant to ...
Helma, Wennemers, Ronald T, Raines
openaire   +2 more sources

Repurposing Azithromycin and Rifampicin Against Gram-Negative Pathogens by Combination With Peptidomimetics

open access: yesFrontiers in Cellular and Infection Microbiology, 2019
Synthetic peptidomimetics may be designed to mimic functions of antimicrobial peptides, including potentiation of antibiotics, yet possessing improved pharmacological properties.
Kristin R. Baker   +8 more
doaj   +1 more source

Peptides and Peptidomimetics as Immunomodulators [PDF]

open access: yesImmunotherapy, 2014
Peptides and peptidomimetics can function as immunomodulating agents by either blocking the immune response or stimulating the immune response to generate tolerance. Knowledge of B- or T-cell epitopes along with conformational constraints is important in the design of peptide-based immunomodulating agents. Work on the conformational aspects of peptides,
Ameya S, Gokhale   +1 more
openaire   +2 more sources

Combinatorial assembly of small molecules into bivalent antagonists of TrkC or TrkA receptors.

open access: yesPLoS ONE, 2014
A library of peptidomimetics was assembled combinatorially into dimers on a triazine-based core. The pharmacophore corresponds to β-turns of the neurotrophin polypeptides neurotrophin-3 (NT-3), nerve growth factor (NGF), or brain-derived neurotrophic ...
Fouad Brahimi   +4 more
doaj   +1 more source

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