2418-95-3 Archives - Page 9 of 16 - Amides-buliding-blocks

Bryson, David I.’s team published research in Nature Chemical Biology in 13 | CAS: 2418-95-3

Nature Chemical Biology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

Bryson, David I. published the artcileContinuous directed evolution of aminoacyl-tRNA synthetases, Name: H-Lys(Boc)-OH, the publication is Nature Chemical Biology (2017), 13(12), 1253-1260, database is CAplus and MEDLINE.

Directed evolution of orthogonal aminoacyl-tRNA synthetases (AARSs) enables site-specific installation of noncanonical amino acids (ncAAs) into proteins. Traditional evolution techniques typically produce AARSs with greatly reduced activity and selectivity compared to their wild-type counterparts. We designed phage-assisted continuous evolution (PACE) selections to rapidly produce highly active and selective orthogonal AARSs through hundreds of generations of evolution. PACE of a chimeric Methanosarcina spp. pyrrolysyl-tRNA synthetase (PylRS) improved its enzymic efficiency (k_cat/K_M^tRNA) 45-fold compared to the parent enzyme. Transplantation of the evolved mutations into other PylRS-derived synthetases improved yields of proteins containing noncanonical residues up to 9.7-fold. Simultaneous pos. and neg. selection PACE over 48 h greatly improved the selectivity of a promiscuous Methanocaldococcus jannaschii tyrosyl-tRNA synthetase variant for site-specific incorporation of p-iodo-L-phenylalanine. These findings offer new AARSs that increase the utility of orthogonal translation systems and establish the capability of PACE to efficiently evolve orthogonal AARSs with high activity and amino acid specificity.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Li, Yue’s team published research in Journal of Chromatography A in 1591 | CAS: 2418-95-3

Journal of Chromatography A published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Safety of H-Lys(Boc)-OH.

Li, Yue published the artcileAn in-line capillary electrophoresis assay for the high-throughput screening of histone deacetylase inhibitors, Safety of H-Lys(Boc)-OH, the publication is Journal of Chromatography A (2019), 171-177, database is CAplus and MEDLINE.

Histone deacetylases (HDACs) are important enzymes that cause chromatin structure contraction and transcription repression, which can downregulate some cancer-suppression genes and lead to the occurrence of cancer. HDAC-specific inhibition is an effective approach to cancer therapy. Hence, a method with which to investigate HDAC activity is needed. We developed an in-line capillary electrophoresis method based on electrophoretically mediated microanal. The optimized conditions were thoroughly validated, and the method was applied to determine the enzyme’s kinetic parameters and the inhibition characteristics of three potent probe inhibitors. The obtained values were comparable to the literature data. Hence, the presented method, with its advantages of miniaturization and full automation, could be used for kinetic and inhibition studies of HDACs, which are targets for drug discovery, in the early stages of new drug development.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Giliomee, Johnel’s team published research in Polymers (Basel, Switzerland) in 13 | CAS: 2418-95-3

Polymers (Basel, Switzerland) published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Recommanded Product: H-Lys(Boc)-OH.

Giliomee, Johnel published the artcileEvaluation of composition effects on the physicochemical and biological properties of polypeptide-based hydrogels for potential application in wound healing, Recommanded Product: H-Lys(Boc)-OH, the publication is Polymers (Basel, Switzerland) (2021), 13(11), 1828, database is CAplus and MEDLINE.

In this study, the effect of crosslinking and concentration on the properties of a new library of low-concentration poly(Lys₆₀-ran-Ala₄₀)-based hydrogels for potential application in wound healing was investigated in order to correlate the hydrogel composition with the desired physicochem. and biofunctional properties to expand the assortment of poly-L-lysine (PLL)-based hydrogels suitable for wound healing. Controlled ring-opening polymerization (ROP) and precise hydrogel compositions were used to customize the physicochem. and biofunctional properties of a library of new hydrogels comprising poly(L-lysine-ran-L-alanine) and four-arm poly(ethylene glycol) (P(KA)/4-PEG). The chem. composition and degree of crosslinking via free amine quantification were analyzed for the P(KA)/4-PEG hydrogels. In addition, the rheol. properties, pore morphol., swelling behavior and degradation time were characterized. Subsequently, in vitro cell studies for evaluation of the cytotoxicity and cell adhesion were performed. The 4 wt% 1:1 functional molar ratio hydrogel with P(KA) concentrations as low as 0.65 wt% demonstrated low cytotoxicity and desirable cell adhesion towards fibroblasts and thus displayed a desirable combination of properties for wound healing application.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Morgan, Charles W.’s team published research in Journal of the American Chemical Society in 143 | CAS: 2418-95-3

Journal of the American Chemical Society published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Product Details of C11H22N2O4.

Morgan, Charles W. published the artcileSelective CRAF Inhibition Elicits Transactivation, Product Details of C11H22N2O4, the publication is Journal of the American Chemical Society (2021), 143(12), 4600-4606, database is CAplus and MEDLINE.

Discovering mols. that regulate closely related protein isoforms is challenging, and in many cases the consequences of isoform-specific pharmacol. regulation remains unknown. RAF isoforms are commonly mutated oncogenes that serve as effector kinases in MAP kinase signaling. BRAF/CRAF heterodimers are believed to be the primary RAF signaling species, and many RAF inhibitors lead to a “paradoxical activation” of RAF kinase activity through transactivation of the CRAF protomer; this leads to resistance mechanisms and secondary tumors. It has been hypothesized that CRAF-selective inhibition might bypass paradoxical activation, but no CRAF-selective inhibitor has been reported and the consequences of pharmacol. inhibiting CRAF have remained unknown. Here, we use bio-orthogonal ligand tethering (BOLT) to selectively target inhibitors to CRAF. Our results suggest that selective CRAF inhibition promotes paradoxical activation and exemplify how BOLT may be used to triage potential targets for drug discovery before any target-selective small mols. are known.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Willis, Julian C. W.’s team published research in Nature Chemistry in 10 | CAS: 2418-95-3

Nature Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C18H15N3O3, Formula: C11H22N2O4.

Willis, Julian C. W. published the artcileMutually orthogonal pyrrolysyl-tRNA synthetase/tRNA pairs, Formula: C11H22N2O4, the publication is Nature Chemistry (2018), 10(8), 831-837, database is CAplus and MEDLINE.

Genetically encoding distinct non-canonical amino acids (ncAAs) into proteins synthesized in cells requires mutually orthogonal aminoacyl-tRNA synthetase (aaRS)/tRNA pairs. The pyrrolysyl-tRNA synthetase/^PyltRNA pair from Methanosarcina mazei (Mm) has been engineered to incorporate diverse ncAAs and is commonly considered an ideal pair for genetic code expansion. However, finding new aaRS/tRNA pairs that share the advantages of the MmPylRS/Mm^PyltRNA pair and are orthogonal to both endogenous aaRS/tRNA pairs and the MmPylRS/Mm^PyltRNA pair has proved challenging. Here we demonstrate that several ΔNPylRS/^PyltRNA_CUA pairs, in which PylRS lacks an N-terminal domain, are active, orthogonal and efficiently incorporate ncAAs in Escherichia coli. We create new PylRS/^PyltRNA pairs that are mutually orthogonal to the MmPylRS/Mm^PyltRNA pair and show that transplanting mutations that reprogram the ncAA specificity of MmPylRS into the new PylRS reprograms its substrate specificity. Finally, we show that distinct PylRS/^PyltRNA-derived pairs can function in the same cell, decode distinct codons and incorporate distinct ncAAs.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Willis, Julian C. W.’s team published research in Nature Chemistry in 10 | CAS: 2418-95-3

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhou, Min’s team published research in iScience in 2021 | CAS: 2418-95-3

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.Quality Control of H-Lys(Boc)-OH It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.

Quality Control of H-Lys(Boc)-OHOn October 22, 2021 ,《Synthesis of poly-α/β-peptides with tunable sequence via the copolymerization on N-carboxyanhydride and N-thiocarboxyanhydride》 was published in iScience. The article was written by Zhou, Min; Zou, Jingcheng; Liu, Longqiang; Xiao, Ximian; Deng, Shuai; Wu, Yueming; Xie, Jiayang; Cong, Zihao; Ji, Zhemin; Liu, Runhui. The article contains the following contents:

The fascinating functions of proteins and peptides in biol. systems have attracted intense interest to explore their mimics using polymers, including polypeptides synthesized from polymerization The folding, structures and functions of proteins and polypeptides are largely dependent on their sequence. However, sequence-tunable polymerization for polypeptide synthesis is a long-lasting challenge. The application of polypeptides is also greatly hindered by their susceptibility to enzymic degradation Although poly-α/β-peptide has proven to be an effective strategy to address the stability issue, the synthesis of poly-α/β-peptide from polymerization is not available yet. Hereby, we demonstrate a living and controlled copolymerization on α-NCA and β-NTA to prepare sequence-tunable poly-α/β-peptides. This polymerization strategy shows a prominent solvent-driven characteristic, providing random-like copolymers of poly-α/β-peptides in THF and block-like copolymers of poly-α/β-peptides in a mixed solvent of CHCl3/H2O (95/5, volume/volume), and opens new avenues for sequence-tunable polymerization and enables facile synthesis of proteolysis tunable poly-α/β-peptides for diverse applications. The experimental process involved the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Quality Control of H-Lys(Boc)-OH)

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Fang, Danxuan’s team published research in ACS Omega in 2019 | CAS: 2418-95-3

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Recommanded Product: H-Lys(Boc)-OH

Recommanded Product: H-Lys(Boc)-OHOn October 8, 2019 ,《Stable, Bioresponsive, and Macrophage-Evading Polyurethane Micelles Containing an Anionic Tripeptide Chain Extender》 was published in ACS Omega. The article was written by Fang, Danxuan; Pi, Menghan; Pan, Zhicheng; Song, Nijia; He, Xueling; Li, Jiehua; Luo, Feng; Tan, Hong; Li, Zhen. The article contains the following contents:

Polymeric nanocarriers have been extensively used in medicinal applications for drug delivery. However, i.v. nanocarriers circulating in the blood will be rapidly cleared from the mononuclear macrophage system. The surface physicochem. characterizations of nanocarriers are the primary factors to determine their fate in vivo, such as evading the reticuloendothelial system, exhibiting long blood circulation times, and accumulating in the targeted site. In this work, we develop a series of polyurethane micelles containing segments of an anionic tripeptide, hydrophilic mPEG, and disulfide bonds. It is found that the long hydrophilic mPEG can shield the micellar surface and have a synergistic effect with the neg. charged tripeptide to minimize macrophage phagocytosis. Meanwhile, the disulfide bond can rapidly respond to the intracellular reduction environment, leading to the acceleration of drug release and improvement of the therapeutic effect. Our results verify that these anionic polyurethane micelles hold great potential in the development of the stealth immune system and controllable intracellular drug transporters. In the experimental materials used by the author, we found H-Lys(Boc)-OH(cas: 2418-95-3Recommanded Product: H-Lys(Boc)-OH)

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zheng, Yiwu’s team published research in ChemMedChem in 2019 | CAS: 2418-95-3

《Stabilizing p-Dithiobenzyl Urethane Linkers without Rate-Limiting Self-Immolation for Traceless Drug Release》 was published in ChemMedChem in 2019. These research results belong to Zheng, Yiwu; Shen, Yang; Meng, Xiaoting; Wu, Yaqi; Zhao, Yibing; Wu, Chuanliu. Category: amides-buliding-blocks The article mentions the following:

Exploiting the redox sensitivity of disulfide bonds is a prevalent strategy in targeted prodrug designs. In contrast to aliphatic disulfides, p-thiobenzyl-based disulfides have rarely been used for prodrug designs, given their intrinsic instability caused by the low pKa of aromatic thiols. Here, we examined the interplay between steric hindrance and the low-pKa effect on thiol-disulfide exchange reactions and uncovered a new thiol-disulfide exchange process for the self-immolation of p-thiobenzyl-based disulfides. We observed a central leaving group shifting effect in the α,α-dimethyl-substituted p-dithiobenzyl urethane linkers (DMTB linkers), which leads to increased disulfide stability by more than two orders of magnitude, an extent that is significantly greater than that observed with typical aliphatic disulfides. In particular, the DMTB linkers display not only high stability, but also rapid self-immolation kinetics due to the low pKa of the aromatic thiol, which can be used as a general and robust linkage between targeting reagents and cytotoxic drugs for targeted prodrug designs. The unique and promising stability characteristics of the present DMTB linker will likely inspire the development of novel targeted prodrugs to achieve traceless release of drugs into cells. In the experiment, the researchers used H-Lys(Boc)-OH(cas: 2418-95-3Category: amides-buliding-blocks)

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Ma, Chunying’s team published research in Molecules in 2019 | CAS: 2418-95-3

《A practical and total synthesis of pasireotide: Synthesis of cyclic hexapeptide via a three-component condensation》 was published in Molecules in 2019. These research results belong to Ma, Chunying; Chen, Miao; Chu, Weiming; Tao, Jiayi; Kong, Delong; Zhang, Mengmeng; Feng, Wenhua. Application In Synthesis of H-Lys(Boc)-OH The article mentions the following:

Pasireotide is a multi-receptor ligand somatostatin analog approved for medical treatment of Cushing’s disease and acromegaly. The liquid-phase total synthesis of pasireotide-a 18-membered cyclic hexapeptide-was achieved by the 3 + 2 + 1 strategy, and the Pro1 -Phe6 peptide bond was selected as the final cyclization position. Two key fragments were simply synthesized using N,O-bis(trimethylsilyl)acetamide/N-hydroxysuccinimide ester (BSA/NHS) as coupling agents, and processes of the two key fragments were simple without any chromatog. purification The current synthesis method is easily scalable and produces the target peptide with an overall yield of 15%. In the experiment, the researchers used many compounds, for example, H-Lys(Boc)-OH(cas: 2418-95-3Application In Synthesis of H-Lys(Boc)-OH)

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics