Search results for: Conjugates
#34522599 2021/04/29 To Up
Delivery strategies of amphotericin B for invasive fungal infections.Invasive fungal infections (IFIs) represent a growing public concern for clinicians to manage in many medical settings, with substantial associated morbidities and mortalities. Among many current therapeutic options for the treatment of IFIs, amphotericin B (AmB) is the most frequently used drug. AmB is considered as a first-line drug in the clinic that has strong antifungal activity and less resistance. In this review, we summarized the most promising research efforts on nanocarriers for AmB delivery and highlighted their efficacy and safety for treating IFIs. We have also discussed the mechanism of actions of AmB, rationale for treating IFIs, and recent advances in formulating AmB for clinical use. Finally, this review discusses some practical considerations and provides recommendations for future studies in applying AmB for combating IFIs.
Xiaochun Wang, Imran Shair Mohammad, Lifang Fan, Zongmin Zhao, Md Nurunnabi, Marwa A Sallam, Jun Wu, Zhongjian Chen, Lifang Yin, Wei He1,000 tests 1 G1 LITRE100 ml
#34522229 2021/08/27 To Up
Synthesis of precision antibody conjugates using proximity-induced chemistry.Therapeutic antibody conjugates allow for the specific delivery of cytotoxic agents or immune cells to tumors, thus enhancing the antitumor activity of these agents and minimizing adverse systemic effects. Most current antibody conjugates are prepared by nonspecific modification of antibody cysteine or lysine residues, inevitably resulting in the generation of heterogeneous conjugates with limited therapeutic efficacies. Traditional strategies to prepare homogeneous antibody conjugates require antibody engineering or chemical/enzymatic treatments, processes that often affect antibody folding and stability, as well as yield and cost. Developing a simple and cost-effective way to precisely couple functional payloads to native antibodies is of great importance. We describe a simple proximity-induced antibody conjugation method (pClick) that enables the synthesis of homogeneous antibody conjugates from native antibodies without requiring additional antibody engineering or post-synthesis treatments. A proximity-activated crosslinker is introduced into a chemically synthesized affinity peptide modified with a bioorthogonal handle. Upon binding to a specific antibody site, the affinity peptide covalently attaches to the antibody via spontaneous crosslinking, yielding an antibody molecule ready for bioorthogonal conjugation with payloads. We have prepared well-defined antibody-drug conjugates and bispecific small molecule-antibody conjugates using pClick technology. The resulting conjugates exhibit excellent cytotoxic activity against cancer cells and, in the case of bispecific conjugates, superb antitumor activity in mouse xenograft models. Our pClick technology enables efficient, simple, and site-specific conjugation of various moieties to the existing native antibodies. This technology does not require antibody engineering or additional UV/chemical/enzymatic treatments, therefore providing a general, convenient strategy for developing novel antibody conjugates.
Yu J Cao, Chenfei Yu, Kuan-Lin Wu, Xuechun Wang, Dong Liu, Zeru Tian, Lijun Zhao, Xuexiu Qi, Axel Loredo, Anna Chung, Han Xiao
1442 related Products with: Synthesis of precision antibody conjugates using proximity-induced chemistry.100ug100ug100ul 100ul100μg100 ul100 ul50 ul100μg100μg50 ul100ug Lyophilized
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#34519765 2021/09/14 To Up
HER2-Low Breast Cancers.Recent clinical trials have demonstrated significant clinical benefits from novel therapeutic compounds in breast cancer patient with human epidermal growth factor receptor 2 (HER2) immunohistochemical (IHC) score of 1+ or 2+ and negative in situ hybridization (ISH) result. A new concept of "HER2-low" breast cancer has been proposed and applied in the recent and ongoing clinical trials. In this article, we review the literature on the topic of HER2-low breast cancer.
Huina Zhang, Hani Katerji, Bradley M Turner, David G Hicks100ul50 ug
#34519610 2021/09/14 To Up
An approach to assessing the contribution of the high LET effect in strategies for Auger endoradiotherapy.The interest in exploiting Auger emitters in cancer therapy stems from their high linear energy transfer (LET) - type radiation damage. However, the design of Auger-emitter labelled vehicles, that target the Auger cascade specifically to tumour cells, is challenging, especially to bring the decay event close enough to DNA to inflict high LET- type damage in DNA. Here we suggest a possible approach to evaluate tumour-targeting Auger-labelled conjugates by assessing the impact of a radioprotector known to be effective in protecting low LET radiation, but ineffective in protecting against high LET-type radiation. However, the efficacy of the radioprotector is not known in the context of irradiation by low energy electrons from randomly distributed Auger emitters. Given some similarity between the energy spectrum of Auger electrons and that of secondary electrons from soft X-rays, we report the results of radioprotection experiments with 25 kVp X-rays. Clonogenic survival curves for cultured human keratinocytes were established for three different irradiation conditions: Cs Î³-rays, 25âkeV X-rays (effective energy 15.5âkeV) and 320 kVp X-rays, and the effect of including a new methylproamine analogue, denoted "2PH", before and during irradiation, was investigated. The extent of radioprotection by 2PH was essentially the same for all radiation conditions, although RBE was higher (about 1.7) for soft X-rays. This suggests that the effects of randomly distributed Auger emitters will be largely subject to radioprotection. It is reasonable to expect that use of methylproamine analogues will help to ascertain the relative contributions of the high-LET effects (not protected), compared to other components, including bystander effects, that are subject to radioprotection. This could be a useful tool in evaluating Auger endoradiotherapy strategies.
Pavel Lobachevsky, Colin Skene, Laura Munforte, Andrea Smith, Jonathan White, Roger F Martin
1783 related Products with: An approach to assessing the contribution of the high LET effect in strategies for Auger endoradiotherapy.4 Arrays/Slide4 Membranes/Box2 Pieces/Box4 Membranes/Box
#34519496 2021/09/14 To Up
Drug-to-Antibody Ratio Estimation via Proteoform Peak Integration in the Analysis of Antibody-Oligonucleotide Conjugates with Orbitrap Fourier Transform Mass Spectrometry.The therapeutic efficacy and pharmacokinetics of antibody-drug conjugates (ADCs) in general, and antibody-oligonucleotide conjugates (AOCs) in particular, depend on the drug-to-antibody ratio (DAR) distribution and average value. The DAR is considered a critical quality attribute, and information pertaining to it needs to be gathered during ADC/AOC development, production, and storage. However, because of the high structural complexity of ADC/AOC samples, particularly in the initial drug-development stages, the application of the current state-of-the-art mass spectrometric approaches can be limited for DAR analysis. Here, we demonstrate a novel approach for the analysis of complex ADC/AOC samples, following native size-exclusion chromatography Orbitrap Fourier transform mass spectrometry (FTMS). The approach is based on the integration of the proteoform-level mass spectral peaks in order to provide an estimate of the DAR distribution and its average value with less than 10% error. The peak integration is performed via a truncation of the Orbitrap's unreduced time-domain ion signals (transients) before mass spectra generation via FT processing. Transient recording and processing are undertaken using an external data acquisition system, FTMS Booster X2, coupled to a Q Exactive HF Orbitrap FTMS instrument. This approach has been applied to the analysis of whole and subunit-level trastuzumab conjugates with oligonucleotides. The obtained results indicate that ADC/AOC sample purification or simplification procedures, for example, deglycosylation, could be omitted or minimized prior to the DAR analysis, streamlining the drug-development process.
Konstantin O Nagornov, Natalia Gasilova, Anton N Kozhinov, Pasi Virta, Patrik Holm, Laure Menin, Victor J Nesatyy, Yury O Tsybin
2611 related Products with: Drug-to-Antibody Ratio Estimation via Proteoform Peak Integration in the Analysis of Antibody-Oligonucleotide Conjugates with Orbitrap Fourier Transform Mass Spectrometry.1 Set100ug Lyophilized1 Set1 Set100ug Lyophilized1 Set
#34519477 2021/09/14 To Up
Non-Genetic Generation of Antibody Conjugates Based on Chemoenzymatic Tyrosine Click Chemistry.The availability of tools to generate homogeneous and stable antibody conjugates without recombinant DNA technology is a valuable asset in fields spanning from diagnostics to imaging and therapeutics. We present here a general approach for the conjugation to human IgG1 antibodies, by employing a straightforward two-stage protocol based on antibody deglycosylation followed by tyrosinase-mediated -quinone strain-promoted click chemistry. The technology is validated by the efficient and clean generation of highly potent DAR2 and DAR4 antibody-drug conjugates (ADCs) with cytotoxic payloads MMAE or PBD dimer, and their evaluation.
Jorick J Bruins, Johannes A M Damen, Marloes A Wijdeven, Lianne P W M Lelieveldt, Floris L van Delft, Bauke Albada
2981 related Products with: Non-Genetic Generation of Antibody Conjugates Based on Chemoenzymatic Tyrosine Click Chemistry.100μg20 micro gram100ug Lyophilized100ug20 micro gram100ug100ul100ug Lyophilized100ug100μg100ug100μg
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#34517609 2021/07/24 To Up
Sensing nanoparticle-protein corona using nanoparticle enhanced Laser Induced Breakdown Spectroscopy signal enhancement.Recently nanoparticle enhanced Laser Induced Breakdown Spectroscopy (NELIBS) is getting a growing interest as an effective alternative method for improving the analytical performance of LIBS. On the other hand, the plasmonic effect during laser ablation can be used for a different task rather than elemental analysis. In this paper, the dependence of NELIBS emission signal enhancement on nanoparticle-protein solutions dried on a reference substrate (metallic titanium) was investigated. Two proteins were studied: Human Serum Albumin (HSA) and Cytochrome C (CytC). Both proteins have a strong affinity for the gold nanoparticles (AuNPs) due to the bonding between the single free exterior thiol (associated with a cysteine residue) and the gold surface to form a stable protein corona. Then, since the protein sizes are vastly different, a different number of protein units is needed to cover AuNP surface to form a protein layer. The NP-protein solution was dropped and dried onto the titanium substrate. Then the NELIBS signal enhancement of Ti emission lines was correlated to the solution characteristics as determined with Dynamic Light Scattering (DLS), Surface Plasmon Resonance (SPR) spectroscopy and Laser Doppler Electrophoresis (LDE) for Î¶-potential determination. Moreover, the dried solutions were studied with TEM (Transmission Electron Microscopy) for the inspection of the inter-particle distance. The structural effect of the NP-protein conjugates on the NELIBS signal reveals that NELIBS can be used to determine the number of protein units required to form the nanoparticle-protein corona with good accuracy. Although the investigated NP-protein systems are simple cases in biological applications, this work demonstrates, for the first time, a different use of NELIBS that is beyond elemental analysis and it opens the way for sensing the nanoparticle protein corona.
Marcella Dell'Aglio, Zita SalajkovÃ¡, Antonia Mallardi, Maria Chiara Sportelli, Jozef Kaiser, Nicola Cioffi, Alessandro De Giacomo
2765 related Products with: Sensing nanoparticle-protein corona using nanoparticle enhanced Laser Induced Breakdown Spectroscopy signal enhancement.300 300 200 200 100 5 mg96T100 1 mg200 100 μg
#34515791 2021/09/13 To Up
The blood-brain barrier limits the therapeutic efficacy of antibody drug conjugates in glioblastoma.
Roger Abounader, David Schiff
1689 related Products with: The blood-brain barrier limits the therapeutic efficacy of antibody drug conjugates in glioblastoma.
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