Category: amides-buliding-blocksOn March 5, 2021, Aizpurua, Jesus M.; Miranda, Jose I.; Irastorza, Aitziber; Torres, Endika; Eceiza, Maite; Sagartzazu-Aizpurua, Maialen; Ferron, Pablo; Aldanondo, Garazi; Lasa-Fernandez, Haizpea; Marco-Moreno, Pablo; Dadie, Naroa; Lopez de Munain, Adolfo; Vallejo-Illarramendi, Ainara published an article in European Journal of Medicinal Chemistry. The article was 《Discovery of a novel family of FKBP12 “”reshapers”” and their use as calcium modulators in skeletal muscle under nitro-oxidative stress》. The article mentions the following:
The hypothesis of rescuing FKBP12/RyR1 interaction and intracellular calcium homeostasis through mol. “”reshaping”” of FKBP12 was investigated. To this end, novel 4-arylthioalkyl-1-carboxyalkyl-1,2,3-triazoles were designed and synthesized, and their efficacy was tested in human myotubes. A library of 17 compounds (10a-n) designed to dock the FKBP12/RyR1 hot-spot interface contact residues, was readily prepared from free α-amino acids and arylthioalkynes using CuAAC “”click”” protocols amenable to one-pot transformations in high overall yields and total configurational integrity. To model nitro-oxidative stress, human myotubes were treated with the peroxynitrite donor SIN1, and evidence was found that some triazoles 10 were able to normalize calcium levels, as well as FKBP12/RyR1 interaction. For example, compound 10 b at 150 nM rescued 46% of FKBP12/RyR1 interaction and up to 70% of resting cytosolic calcium levels in human myotubes under nitro-oxidative stress. All compounds 10 analyzed showed target engagement to FKBP12 and low levels of cytotoxicity in vitro. Compounds 10b, 10c, 10h, and 10iR were identified as potential therapeutic candidates to protect myotubes in muscle disorders with underlying nitro-oxidative stress, FKBP12/RyR1 dysfunction and calcium dysregulation. After reading the article, we found that the author used H-Lys(Boc)-OH(cas: 2418-95-3Category: amides-buliding-blocks)
H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. These amino acids may be present in low concentrations and play a vital part as an intermediate in a biosynthetic pathway, e.g., ornithine, homoserine, or cystathionine. In contrast they may act as a major storage form of nitrogen, e.g., canavanine in the seed of Canavalia ensiformis, or may be formed in high amounts in response to an external stress, e.g., γ-aminobutyrate.Category: amides-buliding-blocks It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics