Making Blank Faces Expressive: Chemical Approaches to the Modification of Chemically Inert Peptides
As an alternative to the conventional approach, which combines amino acid monomers in a one‐by‐one fashion to peptide derivatives, the chemical modification of existing peptides has attracted significant attention in recent years. However, such approaches generally target the reactive functional groups in cysteine and lysine residues, particularly in ...
Yoshitaka Moriyama +2 more
wiley +1 more source
A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission.
Swapna Bhagwanth +2 more
doaj +1 more source
Proapoptotic activity of new glutathione S-transferase inhibitors [PDF]
Selected 7-nitro-2,1,3-benzoxadiazole derivatives have been recently found very efficient inhibitors of glutathione S-transferase (GST) PI-1,(5) an enzyme which displays antiapoptotic activity and is also involved in the cellular resistance to anticancer
Bullo, A +11 more
core +2 more sources
Discovery, evolution and potential future applications of bismuth bicycle molecules—a novel class of therapeutics with unique properties. ABSTRACT Bicyclic peptides are emerging as next generation therapeutics by combining the affinity and specificity of antibodies with the synthetic convenience of small molecules.
Saan Voss +8 more
wiley +1 more source
Diastereodivergent synthesis of chiral tetrahydropyrrolodiazepinediones via a one-pot intramolecular aza-Michael/lactamization sequence [PDF]
A modular and diastereodivergent synthesis of tetrahydro-1H-pyrrolo[1,2d]diazepine-(2,5)-diones is presented. The tetrahydropyrrolodiazepinedione scaffold is obtained via a base-mediated three-step isomerization/tandem cyclization of amino acid-coupled ...
Brown, Lauren E. +3 more
core +1 more source
A user-friendly Matlab program and GUI for the pseudorotation analysis of saturated five-membered ring systems based on scalar coupling constants [PDF]
Background: The advent of combinatorial chemistry has revived the interest in five-membered heterocyclic rings as scaffolds in pharmaceutical research. They are also the target of modifications in nucleic acid chemistry.
Hendrickx, Pieter, Martins, José
core +4 more sources
Dimeric peroxiredoxins are druggable targets in human Burkitt lymphoma [PDF]
Burkitt lymphoma is a fast-growing tumor derived from germinal center B cells. It is mainly treated with aggressive chemotherapy, therefore novel therapeutic approaches are needed due to treatment toxicity and developing resistance. Disturbance of red-ox
Bajor, Małgorzata +17 more
core +2 more sources
Molecular determinants of signal transduction in tropomyosin receptor kinases
Tropomyosin receptor kinases control critical neuronal functions, but how do the same receptors produce diverse cellular responses? This review explores the structural mechanisms behind Trk signaling diversity, focusing on allosteric modulation and ligand bias.
Giray Enkavi
wiley +1 more source
Nanoparticles and cars : analysis of potential sources [PDF]
Urban health is potentially affected by particle emissions. The potential toxicity of nanoparticles is heavily debated and there is an enormous global increase in research activity in this field.
Groneberg, Jan David Alexander +5 more
core
Rational Design of Selective and Bioactive Inhibitors of the Mycobacterium Tuberculosis Proteasome [PDF]
The 20S core particle of the proteasome in Mycobacterium tuberculosis (Mtb) is a promising, yet unconventional, drug target. This multimeric peptidase is not essential, yet degrades proteins that have become damaged and toxic via reactions with nitric ...
Barthelme, Dominik +7 more
core +1 more source

