Category: 1395786-30-7

Xiao, Wu-Yi published the artcileClick Reaction-Assisted Peptide Immune Checkpoint Blockade for Solid Tumor Treatment, Name: Dbco-maleimide, the publication is ACS Applied Materials & Interfaces (2020), 12(36), 40042-40051, database is CAplus and MEDLINE.

One of the major challenges of immune checkpoint blockade (ICB) is the poor penetration of antibody for solid tumor treatment. Herein, peptides with deeper penetration capability are used to develop a click reaction-assisted peptide immune checkpoint blockade (CRICB) strategy that could in situ construct assemblies, enabling enhanced accumulation and prolonged PD-L1 occupancy, ultimately realizing high-performance tumor inhibition. First, the free DBCO-modified targeting peptide (TP) efficiently recognizes and binds PD-L1 in a deep solid tumor. Upon a reagent-free click reaction with a subsequently introduced azide-tethered assembled peptide (AP), the click reaction results in spontaneous self-aggregation in situ with enhanced accumulation and prolonged occupancy. In addition, the penetration of TP-AP (121.2 ¡À 15.5¦Ìm) is significantly enhanced compared with that of an antibody (19.9 ¡À 5.6¦Ìm) in a solid tumor tissue. More importantly, significant immunotherapy effects and negligible side effects are observed in 4T1 and CT26 tumor-bearing mice models treated with TP-AP, suggesting the high-performance tumor inhibition attributed to the CRICB strategy. In summary, this CRICB strategy manifest the preferable effects of immune checkpoint blockade, thereby extending the biomedical application of assembling peptides.

ACS Applied Materials & Interfaces published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C18H26ClN3O, Name: Dbco-maleimide.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Henning, Ryan K. published the artcileDegradation of Akt using protein-catalyzed capture agents, Safety of Dbco-maleimide, the publication is Journal of Peptide Science (2016), 22(4), 196-200, database is CAplus and MEDLINE.

Abnormal signaling of the protein kinase Akt has been shown to contribute to human diseases such as diabetes and cancer, but Akt has proven to be a challenging target for drugging. Using iterative in situ click chem., we recently developed multiple protein-catalyzed capture (PCC) agents that allosterically modulate Akt enzymic activity in a protein-based assay. Here, we utilize similar PCCs to exploit endogenous protein degradation pathways. We use the modularity of the anti-Akt PCCs to prepare proteolysis targeting chimeric mols. that are shown to promote the rapid degradation of Akt in live cancer cells. These novel proteolysis targeting chimeric mols. demonstrate that the epitope targeting selectivity of PCCs can be coupled with non-traditional drugging moieties to inhibit challenging targets.

Journal of Peptide Science published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, Safety of Dbco-maleimide.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Masuya, Takahiro published the artcilePinpoint Dual Chemical Cross-Linking Explores the Structural Dynamics of the Ubiquinone Reaction Site in Mitochondrial Complex I, Recommanded Product: Dbco-maleimide, the publication is Biochemistry (2021), 60(10), 813-824, database is CAplus and MEDLINE.

The ubiquinone reduction step in NADH-ubiquinone oxidoreductase (complex I) is the key to triggering proton translocation in its membrane part. Although the existence of a long and narrow quinone-access channel was identified, it remains debatable whether the channel model can account for binding of various ligands (ubiquinones and inhibitors) to the enzyme. The authors previously proposed that the matrix-side interfacial region of the 49 kDa, ND1, PSST, and 39 kDa subunits, which is covered by a loop connecting transmembrane helixes (TMHs) 1 and 2 of ND3, may be the area for entry of some bulky ligands into the quinone reaction cavity. However, this proposition lacks direct evidence that the cavity is accessible from the putative matrix-side region, which allows ligands to pass. To address this, the authors examined whether Cys³⁹ of ND3 and Asp¹⁶⁰ of 49 kDa can be specifically crosslinked by bifunctional crosslinkers (tetrazine-maleimide hybrid, named TMBC). On the basis of the structural models of complex I, such dual crosslinking is unexpected because ND3 Cys³⁹ and 49 kDa Asp¹⁶⁰ are located on the TMH1-2 loop and deep inside the channel, resp., and hence, they are phys. separated by peptide chains forming the channel wall. However, three TMBCs with different spacer lengths did crosslink the two residues, giving new crosslinked ND3/49 kDa subunits. Chem. modification of either ND3 Cys³⁹ or 49 kDa Asp¹⁶⁰ blocked the dual crosslinking, ensuring the specificity of the crosslinking. Altogether, this study provides direct evidence that the quinone reaction cavity is indeed accessible from the proposed matrix-side region covered by the ND3 TMH1-2 loop.

Biochemistry published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, Recommanded Product: Dbco-maleimide.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Yao, Xiyuan published the artcileCysteine-Directed Bioconjugation of a Platinum(II)-Acridine Anticancer Agent, HPLC of Formula: 1395786-30-7, the publication is Inorganic Chemistry (2019), 58(1), 43-46, database is CAplus and MEDLINE.

Classical maleimide Michael addition chem. in conjunction with copper-free click chem. was investigated as a synthetic strategy to attach cytotoxic platinum-acridine hybrid agents to carrier proteins. The structural integrity and selectivity of the model payloads, which were validated in human serum albumin (HSA) using mass spectrometric anal. and heteronuclear 2D ¹H-¹⁵N HSQC NMR experiments, may have broad utility for the targeted delivery of highly cytotoxic platinum acridines and other nonclassical platinum containing anticancer agents.

Inorganic Chemistry published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C2H2N4O2, HPLC of Formula: 1395786-30-7.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Cal, Pedro M. S. D. published the artcileSite-selective installation of BASHY fluorescent dyes to Annexin V for targeted detection of apoptotic cells, Application In Synthesis of 1395786-30-7, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(2), 368-371, database is CAplus and MEDLINE.

Fluorophores are indispensable for imaging biol. processes. The authors report the design and synthesis of azide-tagged boronic acid salicylidenehydrazone (BASHY) dyes and their use for site-selective labeling of Annexin V. The Annexin V-BASHY conjugate maintained function and fluorescence as demonstrated by the targeted detection of apoptotic cells.

Chemical Communications (Cambridge, United Kingdom) published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, Application In Synthesis of 1395786-30-7.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Mukhortava, Ann published the artcileEfficient Formation of Site-Specific Protein-DNA Hybrids Using Copper-Free Click Chemistry, SDS of cas: 1395786-30-7, the publication is Bioconjugate Chemistry (2016), 27(7), 1559-1563, database is CAplus and MEDLINE.

Protein-DNA hybrids have become increasingly popular mol. building blocks in bionanotechnol. and single-mol. studies to synergistically combine the programmability of DNA with the chem. diversity of proteins. The growing demand for protein-DNA hybrids requires powerful strategies for their conjugation. Here, we present an efficient two-step method for protein-DNA assembly based on copper-free click chem. The method allows site-specificity and high coupling efficiency, while maintaining the conservation of protein activity. We compare our method to a commonly used protocol of direct linkage of maleimide-modified oligos. We demonstrate the significantly higher yield with a protein-DNA conjugate, which is analyzed using single-mol. force spectroscopy.

Bioconjugate Chemistry published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, SDS of cas: 1395786-30-7.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Stejskalova, Anna published the artcileBiologically Inspired, Cell-Selective Release of Aptamer-Trapped Growth Factors by Traction Forces, Computed Properties of 1395786-30-7, the publication is Advanced Materials (Weinheim, Germany) (2019), 31(7), n/a, database is CAplus and MEDLINE.

Biomaterial scaffolds that are designed to incorporate dynamic, spatiotemporal information have the potential to interface with cells and tissues to direct behavior. Here, a bioinspired, programmable nanotechnol.-based platform is described that harnesses cellular traction forces to activate growth factors, eliminating the need for exogenous triggers (e.g., light), spatially diffuse triggers (e.g., enzymes, pH changes), or passive activation (e.g., hydrolysis). Flexible aptamer technol. is used to create modular, synthetic mimics of the Large Latent Complex that restrains transforming growth factor-¦Â1 (TGF-¦Â1). This flexible nanotechnol.-based approach is shown here to work with both platelet-derived growth factor-BB (PDGF-BB) and vascular endothelial growth factor (VEGF-165), integrate with glass coverslips, polyacrylamide gels, and collagen scaffolds, enable activation by various cells (e.g., primary human dermal fibroblasts, HMEC-1 endothelial cells), and unlock fundamentally new capabilities such as selective activation of growth factors by differing cell types (e.g., activation by smooth muscle cells but not fibroblasts) within clin. relevant collagen sponges.

Advanced Materials (Weinheim, Germany) published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is 0, Computed Properties of 1395786-30-7.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Tachihara, Yoshihiro published the artcileMechanically interlocked molecular architectures of valinomycin as cancer targeted prodrugs, Category: catalysis-chemistry, the publication is Nano Select (2022), 3(8), 1242-1251, database is CAplus.

Macrocyclic drugs are promising agents for treating a variety of diseases. However, these compounds usually present delivery limitations, such as low tissue selectivity and poor cellular uptake, which may impair efficacy and clin. translation. Here, we propose a mol. machine approach for delivering macrocyclic drugs based on their assembly into bioactive rotaxanes. To prove this concept, we use the extremely toxic macrocycle valinomycin (Val) as the host mol., and identify dihydralazine (Dihyd) as a guest mol. after screening several guest compounds The Val-Dihyd complex is mech. interlocked by capping one hydrazide group in Dihyd with fluorescein isothiocyanate (FITC) and the other with a Y-shape branched poly(ethylene glycol) (PEG) via a pH-sensitive hydrazone bond. Thus, the Val-loaded rotaxanes (Vrot) are stable at physiol. pH, but release Val at mild acidic conditions mimicking intratumoral and endosomal environments. In vitro studies revealed Vrot is less cytotoxic than free Val in pancreatic cancer cells, while modifying Vrot with cyclic arginine-glycine-aspartic acid (cRGD) peptides promotes the cytotoxicity by enhancing cellular uptake. These results indicate the potential of rotaxanes of macrocyclic drugs for generating cancer targeted prodrugs.

Nano Select published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C4Br2N2O4S, Category: catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Zhou, Qianghui published the artcileBioconjugation by Native Chemical Tagging of C-H Bonds, COA of Formula: C25H21N3O4, the publication is Journal of the American Chemical Society (2013), 135(35), 12994-12997, database is CAplus and MEDLINE.

A general C-H functionalization method for the tagging of natural products and pharmaceuticals is described. An azide-containing sulfinate reagent allows the appendage of azidoalkyl chains onto heteroaromatics, the product of which can then be attached to a monoclonal antibody by a “click” reaction. This strategy expands the breadth of bioactive small mols. that can be linked to macromols. in a manner that is beyond the scope of existing methods in bioconjugation to permit tagging of the “seemingly untaggable”.

Journal of the American Chemical Society published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C38H24F4O4P2, COA of Formula: C25H21N3O4.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Kelemen, Rachel E. published the artcileA Precise Chemical Strategy To Alter the Receptor Specificity of the Adeno-Associated Virus, Computed Properties of 1395786-30-7, the publication is Angewandte Chemie, International Edition (2016), 55(36), 10645-10649, database is CAplus and MEDLINE.

The ability to target the adeno-associated virus (AAV) to specific types of cells, by altering the cell-surface receptor it binds, is desirable to generate safe and efficient therapeutic vectors. Chem. attachment of receptor-targeting agents onto the AAV capsid holds potential to alter its tropism, but is limited by the lack of site specificity of available conjugation strategies. The development of an AAV production platform is reported that enables incorporation of unnatural amino acids (UAAs) into specific sites on the virus capsid. Incorporation of an azido-UAA enabled site-specific attachment of a cyclic-RGD peptide onto the capsid, retargeting the virus to the ¦Á_v¦Â₃ integrin receptors, which are overexpressed in tumor vasculature. Retargeting ability was site-dependent, underscoring the importance of achieving site-selective capsid modification. This work provides a general chem. approach to introduce various receptor binding agents onto the AAV capsid with site selectivity to generate optimized vectors with engineered infectivity.

Angewandte Chemie, International Edition published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, Computed Properties of 1395786-30-7.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia