54930-24-4Relevant academic research and scientific papers
Conjugation between maleimide-containing Pt(IV) prodrugs and furan or furan-containing drug delivery vectors via Diels-Alder cycloaddition
Gabano, Elisabetta,Perin, Elena,Bonzani, Diego,Ravera, Mauro
, p. 195 - 200 (2019/01/30)
Pt(IV) complexes are considered to act as antitumor prodrugs and their in vivo activity can be improved exploiting drug targeting and delivery strategies. With a view to such applications, the maleimide-containing ligand 2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetic acid was used to produce the cisplatin-based Pt(IV) complexes (OC-6-44)-diamminedichlorido(ethanolato)(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetato)platinum(IV) and (OC-6-44)-acetatodiamminedichlorido(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetato)platinum(IV). These complexes underwent Diels-Alder reaction with furan, used as a model molecule to set up the experimental conditions, at ambient temperature up to 50 h, with limited decomposition. Finally, the reaction between the maleimide-containing Pt(IV) complexes and silica nanoparticles decorated with furan were successfully used as a proof-of-concept to demonstrate the clickability of functionalized vectors for drug delivery.
Incorporating 131I into a PAMAM (G5.0) dendrimer-conjugate: design of a theranostic nanosensor for medullary thyroid carcinoma
He,Wang,Su,Chen,Xie,Chen,Yu,Toledo,Abayaweera,Zhu,Bossmann
, p. 16181 - 16188 (2017/03/22)
We report the synthesis and purification of a targeting probe for Medullary Thyroid Carcinoma (MTC) by incorporating 131I into PAMAM (G5.0) dendrimers. Both the 131I labeled control dendrimer (131I-PAMAM (G5.0) without attached targeting peptide) and the MTC-targeting dendrimer (131I-PAMAM (G5.0) attached to VTP (vascular targeting peptide)) were labeled with the radioisotope 131I by applying the iodogen method. The resulting G5.0 dendrimers were purified by means of ultracentrifugation. The labelling efficiencies and radiochemical purities vs. time were determined by paper chromatography. The radiolabeling efficiencies of 131I-PAMAM (G5.0) and 131I-PAMAM (G5.0) were 93 ± 1% and 85 ± 2%, respectively. 131I-PAMAM (G5.0) did exhibit small, but significant changes in radiochemical purity as a function of time after labelling. The highest observed highest purity was 82 ± 2%. 131I-PAMAM (G5.0)-VTP did display larger changes in radiochemical purity as a function of time after labelling, maximally 80 ± 2%. The stability of the two probes and their binding behavior to the human medullary thyroid cancer cell line (TT) were observed in vitro. Compared to the negative control group (consisting of Na131I), the TT cell binding rate of 131I-PAMAM (G5.0)-VTP was significantly increased at 48 h and 72 h (P 131I-PAMAM (G5.0)-VTP at 48 h and 72 h was not significantly different when compared to the positive control group (131I-PAMAM (G5.0) group) (P > 0.05). These findings have been confirmed by performing MTT assays. These results confirm earlier findings, which demonstrated fast uptake of PAMAM (G5.0) by various cell types.
Synthesis and in vitro testing of new potent polyacridine-melittin gene delivery peptides
Baumhover, Nicholas J.,Anderson, Kevin,Fernandez, Christian A.,Rice, Kevin G.
experimental part, p. 74 - 83 (2010/11/04)
The combination of a polyacridine peptide modified with a melittin fusogenic peptide results in a potent gene transfer agent. Polyacridine peptides of the general formula (Acr-X)n-Cys were prepared by solid-phase peptide synthesis, where Acr is
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes
Brownlee, June M.,Carlson, Erik,Milne, Amy C.,Pape, Erika,Harrison, David H.T.
, p. 424 - 444 (2008/02/09)
The competitive inhibition constants of series of inhibitors related to phenylacetic acid against both wild-type and the doubly mutanted C298A/W219Y aldose reductase have been measured. Van't Hoff analysis shows that these acids bind with an enthalpy near -6.8 kcal/mol derived from the electrostatic interactions, while the 100-fold differences in binding affinity appear to be largely due to entropic factors that result from differences in conformational freedom in the unbound state. These temperature studies also point out the difference between substrate and inhibitor binding. X-ray crystallographic analysis of a few of these inhibitor complexes both confirms the importance of a previously described anion binding site and reveals the hydrophobic nature of the primary binding site and its general plasticity. Based on these results, N-glycylthiosuccinimides were synthesized to demonstrate their potential in studies that probe distal binding sites. Reduced α-lipoic acid, an anti-oxidant and therapeutic for diabetic complications, was shown to bind aldose reductase with a binding constant of 1 μM.
Probing structural effects on replication efficiency through comparative analyses of families of potential self-replicators
Kassianidis, Eleftherios,Pearson, Russell J.,Philp, Douglas
, p. 8798 - 8812 (2007/10/03)
A formidable synthetic apparatus for the creation of nanoscale molecular structures and supramolecular assemblies through molecular structures can potentially be created from systems that are capable of parallel automultiplication (self-replication). In order to achieve this goal, a detailed understanding of the relationship be tween molecular structure and replication efficiency is necessary. Diastereoisomeric templates that are capable of specific and simultaneous autocatalysis have been synthesised. A systematic experimental and theoretical evaluation of their behaviour and that of structurally-related systems reveals the key determinants that dictate the emergence of self-replicative function and defines the structural space within which this behaviour is observed.
Maleimidyl-containing material and production method thereof
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Page/Page column 6, (2010/11/08)
The invention provides a maleimidyl-containing material having a substituent group defined by the following structural formula (1) containing a maleimidyl group (maleimido group): wherein A denotes a spacer containing an amino acid or a peptide spacer P. Also, the invention provides a production method of the above-mentioned maleimidyl-containing material involving a step of reacting a material containing an amino acid or a peptide chain with a compound containing a maleimido group.
Systems chemistry: Kinetic and computational analysis of a nearly exponential organic replicator
Kindermann, Maik,Stahl, Insa,Reimold, Malte,Pankau, Wolf Matthias,Von Kiedrowski, Guenter
, p. 6750 - 6755 (2007/10/03)
Combining kinetic, structural, and computational studies on complex dynamic feedback systems may lead to the field of "systems chemistry". The approach is exemplified by the analysis of a simple organic self-replicating system that has the potential to ex
Self-replication vs. reactive binary complexes - Manipulating recognition-mediated cycloadditions by simple structural modifications
Pearson, Russell J.,Kassianidis, Eleftherios,Slawin, Alexandra M.Z.,Philp, Douglas
, p. 3434 - 3441 (2007/10/03)
The rate of reaction and the selectivity of a Diels - Alder cycloaddition between a furan and a maleimide can be enhanced by the introduction of complementary recognition sites on the reactant species. Subtle manipulation of other structural elements allows the generation of the observed rate enhancements and selectivities through either self-replication or formation of a pre-reactivc binary complex.
