Category: 42074-68-0

Yuan, Dan published the artcileThe enzyme-instructed assembly of the core of yeast prion Sup35 to form supramolecular hydrogels, Name: 2-Chlorotrityl chloride, the publication is Journal of Materials Chemistry B: Materials for Biology and Medicine (2016), 4(7), 1318-1323, database is CAplus and MEDLINE.

Based on the self-assembly capability of the core segment (GNNQQNY) of yeast prion Sup35, we design and synthesize a series of structurally related precursors for the enzymic formation of hydrogels. We found that, with the catalysis of alk. phosphatase, the precursor becomes a hydrogelator that self-assembles in water to form nanofibers with an average width less than ten nanometers. Interestingly, the introduction of an amyloid segment into a cytotoxic precursor (N’ffyp: D-1P) is able to abrogate the cytotoxicity of the precursor, making the resulting peptide cell compatible. This work contributes a new insight into the use of enzymes to form cell compatible hydrogels of peptide cross-β spine.

Journal of Materials Chemistry B: Materials for Biology and Medicine published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C17H18N2O6, Name: 2-Chlorotrityl chloride.

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

Mohamed, Heba A. published the artcileSilver(I) N-Heterocyclic Carbene Complexes Derived from Clotrimazole: Antiproliferative Activity and Interaction with an Artificial Membrane-Based Biosensor, Formula: C19H14Cl2, the publication is Organometallics (2020), 39(8), 1318-1331, database is CAplus.

With the aim of combining the potential anticancer properties of both clotrimazole, an imidazole based antifungal agent, and Ag(I) N-heterocyclic carbenes, 13 novel Ag(I) N-heterocyclic carbene complexes derived from clotrimazole were synthesized. The complexes were fully characterized, and the partition coefficient of each provides a measure of hydrophobicity. The antiproliferative properties of the complexes against cancerous and noncancerous cell lines found optimum cytotoxicity when the complex displays an intermediate lipophilicity, which describes a complex that possesses both water-soluble groups and lipophilic aromatic groups. The Ag complexes were screened on a synthetic biomembrane-like device using a chip-based phospholipid-coated Pt/Hg electrode embedded in a flow cell system. The results are recorded as rapid cyclic voltammograms (RCVs), which give insight into the interactions of the complexes with a cell membrane. The principle of intermediate lipophilicity also applies to the monolayer interaction to which the Ag atom significantly implements an irreversibility.

Organometallics published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Formula: C19H14Cl2.

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

Hirabayashi, Ayumi published the artcilePhotodegradation of amyloid β and reduction of its cytotoxicity to PC12 cells using porphyrin derivatives, Recommanded Product: 2-Chlorotrityl chloride, the publication is Chemical Communications (Cambridge, United Kingdom) (2014), 50(67), 9543-9546, database is CAplus and MEDLINE.

A purpose-designed porphyrin-peptide hybrid effectively degraded amyloid β monomer and oligomers associated with Alzheimer’s disease. Degradation was achieved using light irradiation in the absence of any additives and under neutral conditions. Moreover, the hybrid effectively neutralized the cytotoxicity of amyloid β in PC12 cells upon photoirradiation

Chemical Communications (Cambridge, United Kingdom) published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.

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

Wodtke, Robert published the artcileSynthesis and kinetic characterization of water-soluble fluorogenic acyl donors for transglutaminase 2, Application of 2-Chlorotrityl chloride, the publication is ChemBioChem (2016), 17(13), 1263-1281, database is CAplus and MEDLINE.

Small Glu-containing peptides bearing coumarin derivatives as fluorescent leaving groups attached to the γ-carboxylic acid group of the Glu residue were synthesized and investigated with regard to their potential to act as substrates for transglutaminase 2 (TGase 2). Their synthesis was accomplished by an efficient solid-phase approach. The excellent water solubility of the compounds enabled their extensive kinetic characterization in the context of TGase 2-catalyzed hydrolysis and aminolysis. The influence of the coumarin skeleton’s substitution pattern on the kinetic properties was studied. Derivatives containing 7-hydroxy-4-methylcoumarin (HMC) revealed properties superior to those of their 7-hydroxycoumarin counterparts; analogous amides were not accepted as substrates. Z-Glu(HMC)-Gly-OH, which exhibited the best substrate properties out of the investigated derivatives, was selected for representative kinetic characterization of acyl acceptor substrates and irreversible inhibitors.

ChemBioChem published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C7H13BrSi, Application of 2-Chlorotrityl chloride.

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

Kato, Naoya published the artcileSynthesis and evaluation of a novel adapter lipid derivative for preparation of cyclic peptide-modified PEGylated liposomes: Application of cyclic RGD peptide, Formula: C19H14Cl2, the publication is European Journal of Pharmaceutical Sciences (2022), 106239, database is CAplus and MEDLINE.

Peptide ligand modified nanoparticles can simply prepared by post-insertion method to mix pre-formed nanoparticles with peptide-lipid conjugates in an aqueous solution at an optimal temperature Therefore, water dispersibility of peptide-lipid conjugates is a very important factor for implementing the post-insertion method. We proposed that highly water dispersible peptide-lipid conjugates can be easily synthesized by sep. designing novel adapter lipids with different water dispersibility and reacting them with ligands in a highly efficient manner. Adapter lipids have three critical roles; as spacers of ligand-conjugated lipids for efficient ligand presentation, as structures that form discrete mol. weight distributions, and as providing water dispersibility. In this study, we developed a novel adapter-lipid derivative that enables a variety of cyclic peptide modifications using the click reaction. The integrin αvβ3-targeted cyclic RGDfK (cRGD) peptide was selected as the cyclic peptide ligand. We designed a novel alkyne-tagged lipid with a discrete peptide spacer and bound the cRGD peptide using a click reaction to synthesize a cRGD-conjugated lipid with good water dispersibility for the preparation of cRGD-modified PEGylated liposomes using the post-insertion method. We also revealed that cRGD-modified PEGylated liposomes are efficiently associated with integrin αvβ3-expressing murine colon carcinoma (Colon-26) cells in a modification amount- and peptide sequence-dependent manner, showing high cytotoxicity upon loading with doxorubicin. This novel adapter lipid derivative can be used to synthesize various cyclic peptides by click reactions and will provide useful insights for the future development of cyclic peptide-modified PEGylated liposomes.

European Journal of Pharmaceutical Sciences published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Formula: C19H14Cl2.

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

Bodendiek, Silke B. published the artcileTriarylmethanes, a new class of Cx50 inhibitors, Category: chlorides-buliding-blocks, the publication is Frontiers in Pharmacology of Ion Channels and Channelopathies (2012), 3(June), 106, database is CAplus and MEDLINE.

The paucity of specific pharmacol. agents has been a major impediment for delineating the roles of gap junction (GJ) channels formed by connexin proteins in physiol. and pathophysiol. Here, we used the selective optimization of side activities (SOSA) approach, which has led to the design of high affinity inhibitors of other ion channels, to identify a specific inhibitor for channels formed by Cx50, a connexin subtype that is primarily expressed in the lens. We initially screened a library of common ion channel modulating pharmacophores for their inhibitory effects on Cx50 GJ channels and identified four new classes of compounds The triarlymethane (TRAM) clotrimazole was the most potent Cx50 inhibitor and we therefore used it as a template to explore the structure activity relationship (SAR) of the TRAMs for Cx50 inhibition. We describe the design of T122 (N-[(2-methoxyphenyl)diphenylmethyl]-1,3-thiazol-2-amine) and T136 (N-[(2-iodophenyl)diphenylmethyl]-1,3-thiazol-2-amine), which inhibit Cx50 with IC₅₀s of 1.2 and 2.4 μM. Both compounds exhibit at least 10-fold selectivity over other connexins as well as major neuronal and cardiac voltage-gated K⁺ and Na⁺ channels. The SAR studies also indicated that the TRAM pharmacophore required for connexin inhibition is significantly different from the pharmacophore required for blocking the calcium-activated KCa3.1 channel. Both T122 and T136 selectively inhibited Cx50 GJ channels in lens epithelial cells, suggesting that they could be used to further explore the role of Cx50 in the lens. In addition, our results indicate that a similar approach may be used to find specific inhibitors of other connexin subtypes.

Frontiers in Pharmacology of Ion Channels and Channelopathies published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Category: chlorides-buliding-blocks.

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

Grassi, Luigi published the artcileAn explorative study towards the chemical synthesis of the immunoglobulin G1 Fc CH3 domain, Formula: C19H14Cl2, the publication is Journal of Peptide Science (2018), 24(12), n/a, database is CAplus and MEDLINE.

Monoclonal antibodies, fusion proteins including Ig fragment c (Ig Fc) CH2-CH3 domains, and engineered antibodies are prominent representatives of an important class of drugs and drug candidates, which are referred to as biotherapeutics or biopharmaceuticals. These recombinant proteins are highly heterogeneous due to their glycosylation pattern. In addition, enzyme-independent reactions, like deamidation, dehydration, and oxidation of sensitive side chains, may contribute to their heterogeneity in a minor amount To investigate the biol. impact of a spontaneous chem. modification, especially if found to be recurrent in a biotherapeutic, it would be necessary to reproduce it in a homogeneous manner. Here, we undertook an explorative study toward the chem. synthesis of the IgG1 Fc CH3 domain, which has been shown to undergo spontaneous changes like succinimide formation and methionine oxidation We used Fmoc-solid-phase peptide synthesis (SPPS) and native chem. ligation (NCL) to test the accessibility of large fragments of the IgG1 Fc CH3 domain. In general, the incorporation of pseudoproline dipeptides improved the quality of the crude peptide precursors; however, sequences larger than 44 residues could not be achieved by standard stepwise elongation with Fmoc-SPPS. In contrast, the application of NCL with Cys residues, which were either native or introduced ad hoc, allowed the assembly of the C-terminal IgG1 Fc CH3 sequence 371 to 450. The syntheses reported here show advantages and limitations of the chem. approaches chosen for the preparation of the synthetic IgG1 Fc CH3 domain and will guide future plans toward the synthesis of both the native and selectively modified full-length domain.

Journal of Peptide Science published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Formula: C19H14Cl2.

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

Chen, Xingchen published the artcilePotent, multi-target serine protease inhibition achieved by a simplified β-sheet motif, Application In Synthesis of 42074-68-0, the publication is PLoS One (2019), 14(1), e0210842, database is CAplus and MEDLINE.

Engagement of an extended β-sheet is a common substrate/inhibitor interaction at the active site of serine proteases and is an important feature of Laskowski mechanism inhibitors that present a substrate-like loop to a target protease. This loop is cleaved but subsequently relegated forming a stable inhibitor/protease complex. Laskowski inhibitors are ubiquitous in nature and are used extensively in serine protease inhibitor design. However, most studies concentrate on introducing new sidechain interactions rather than the direct contributions of the substrate-like β-sheet to enzyme inhibition. Here we report the crystal structure of an simplified β-sheet inhibitory motif within the Sunflower Trypsin Inhibitor (SFTI) in complex with trypsin. We show that the intramol. hydrogen bond network of this SFTI variant (SFTI-TCTR) engages the inhibitor sidechains that would normally interact with a target protease, giving mainchain interactions a more prominent role in complex formation. Despite having reduced sidechain interactions, this SFTI variant is remarkably potent and inhibits a diverse range of serine proteases. Crystal structural anal. and mol. modeling of SFTI-TCTR complexes again indicates an interface dominated by β-sheet interactions, highlighting the importance of this motif and the adaptability of SFTI as a scaffold for inhibitor design.

PLoS One published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Application In Synthesis of 42074-68-0.

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

Nielsen, Alexander L. published the artcileMechanism-based inhibitors of SIRT2: structure-activity relationship, X-ray structures, target engagement, regulation of α-tubulin acetylation and inhibition of breast cancer cell migration, Quality Control of 42074-68-0, the publication is RSC Chemical Biology (2021), 2(2), 612-626, database is CAplus and MEDLINE.

Sirtuin 2 (SIRT2) is a protein deacylase enzyme that removes acetyl groups and longer chain acyl groups from post-translationally modified lysine residues. It affects diverse biol. functions in the cell and has been considered a drug target in relation to both neurodegenerative diseases and cancer. Therefore, access to well-characterized and robust tool compounds is essential for the continued investigation of the complex functions of this enzyme. Here, we report a collection of chem. probes that are potent, selective, stable in serum, water-soluble, and inhibit SIRT2-mediated deacetylation and demyristoylation in cells. Compared to the current landscape of SIRT2 inhibitors, this is a unique ensemble of features built into a single compound We expect the developed chemotypes to find broad application in the interrogation of SIRT2 functions in both healthy and diseased cells, and to provide a foundation for the development of future therapeutics.

RSC Chemical Biology published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Quality Control of 42074-68-0.

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

Kalola, Anirudhdha G. published the artcileReduction of aliphatic, aromatic and heteroaromatic carboxylic acid derivatives to alcohol promoted by trityl resin under presence of copper sulphate and sodium borohydride catalytic system, COA of Formula: C19H14Cl2, the publication is Heterocyclic Letters (2022), 12(1), 87-99, database is CAplus.

An efficient, eco-friendly, mild protocol for the acid-alc. transformation is developed. Varied aliphatic, aromatic and heteroaromatic carboxylic acid derivatives RC(O)OH [R = n-heptadecan-1-yl, 1-naphthyl, furan-2-yl, etc.] loaded on to the 2-chloro trityl chloride resin under perseverance of DIPEA base followed by subsequent reduction into corresponding alcs. ROH using CuSO₄-NaBH₄ catalytic system have been achieved in excellent yield with easy product isolation technique. Facile recycling of the recovered resin is also associated to this methodol.

Heterocyclic Letters published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, COA of Formula: C19H14Cl2.

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