Read Structure-Activity Studies of Polyamine Analogues as Antineoplastics (Classic Reprint) - Yang Feng | ePub
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Thus, this systematic sar study has provided new pharmacological tools for studies of iglu receptors.
Selective mammalian smo and pao inhibitors could represent important tools to study the involvement of this class of enzymes in polyamine homeostasis and in designing new antineoplastic drugs. Here, mpao and msmo inhibition by 1,8‐diaminooctane, 1,12‐diaminododecane, g3, guazatine and mdl72527 is reported.
Structure-activity studies showed a clear dependence of the acyl chain length on activity against lta in compounds with spermine and homospermine scaffolds.
Recent studies indicate that induction of polyamine catabolic enzymes ssat and spermine oxidase (smo) play key roles in the anti-proliferative and apoptotic effects of polyamine analogues and their combinations with chemotherapeutic agents such as 5-fluorouracil (5-fu) and paclitaxel.
10 jul 2014 blue waters symposium presentation:project pi: aleksei aksimentiev, university of illinois at urbana-champaignpresented by: jejoong yoo,.
15 jan 2002 several studies have shown the association of polyamines to dna to of polyamines under conditions of low water activity (18) and possibly.
15 dec 2009 the highly sensitive structure–activity relationships (sar's) that underlie and control polyamine function have been the target of intense research.
These studies were expanded to include ec 50 determinations as well as ec 90 to provide depth to our structure activity relationship analysis. Upon analysis, 37 individual polyamines were found to inhibit bacterial growth alone at or below the maximum concentration tested 25 μg ml-1.
Polyamine analogue regulation of nmda mk-801 binding: a structure-activity study. J med chem, 39(26):5257-5266, 01 dec 1996 cited by 12 articles pmid: 8978854.
The diversity of biological research in the polyamine field is the subject of an ( 1994) antiproliferative properties of polyamine analogues: a structure-activity.
Structure-activity studies of polyamine analogues as antineoplastics by yang feng a dissertation presented to the graduate school of the university of florida in partial fulfillment of the requirements for the degree of doctor of philosophy university of florida 1996 acknowledgments.
The nachr belongs to the superfamily of ligand‐gated ion channels and is a heteropentameric transmembrane protein with a subunit stoichiometry of α 2 βγδ[[1-3]]. The five receptor subunits are arranged around a central pore, which is permeable for cations upon agonist binding.
These measurements included formal acute and chronic toxicity trials, drug and metabolic tissue distribution studies, and assessment of the impact of these analogues on tissue polyamine pools. Finally, the remarkable activity of n n ‘ - bis[3-(ethylamino)propyl]- trans -1,4-cyclohexanediamine underscores the need to further explore this.
Structure activity relationship studies on the antimicrobial activity of novel edeine a and d analogues.
Amino acid residues) are actually considered as signal structures for the rapid and selective in the following experiments, therefore, the effects of putrescine were studied.
Mammalian polyamine catabolism is under the control of two enzymes, spermidine/spermine n 1-acetyltransferase and the flavin adenine dinucleotide-dependent polyamine oxidase (pao). In this study, the cloning and initial characterization of human pao is reported.
Structure-activity investigations of polyamine-anthracene conjugates and their uptake via the polyamine transporter. Targeting polyamine metabolism and function in cancer and other hyperproliferative diseases.
Fourteen polyamine analogues, asymmetric or symmetric substituted spermine (1-9) or methoctramine (10-14) analogues, were evaluated as potential inhibitors or substrates of two enzymes of the polyamine catabolic pathway, spermine oxidase (smox) and acetylpolyamine oxidase (paox).
Abstract: this review describes the recent developments in the field of polyamine toxins, with focus on structure activity relationship investigations, including studies of importance of the polyamine moiety for biological activity, photolabeling studies using polyamine toxins as templates, as well as use of solid phase methods for the synthesis of polyamine toxins.
We and others have performed extensive structure–activity relationship (sar) studies of polyamine toxins as iglu receptor ligands, 7 initially using the wasp polyamine toxin, philanthotoxin‐433, as a template. 9 more recently, we have used the structurally more complex and more potent spider polyamine toxins, such as argiotoxin‐636 (argtx.
Phanstiel o 4th, kaur n, delcros jg (2007) structure-activity investigations of polyamine-anthracene conjugates and their uptake via the polyamine transporter.
19 dec 2016 we studied the effect of branched-chain polyamines on the folding transition of polyamines induce a crosslinked meshwork structure in a giant dna an important role in maintaining genetic activities at high temperat.
2008, 51, 7308–7312 structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone.
Polyamine analogs have demonstrated considerable activity against many important solid tumor models including breast cancer. However, the precise mechanisms of antitumor activities of polyamine analogs are not entirely understood. The cytotoxicity of a newly developed polyamine analog compound, sl11144, against human breast cancer was assessed.
Knowing that the polyamine transport system is upregulated in cancers and that polyamines naturally bind to dna, a range of polyamine analogues and polyamine-like structures have been synthesised to target epigenetic regulators, with encouraging results.
Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine lsd1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures.
Selective mammalian smo and pao inhibitors could represent important tools to study the involve- ment of this class of enzymes in polyamine homeosta- sis and in designing new antineoplastic drugs. Here, mpao and msmo inhibition by 1,8-diaminooctane, 1,12-diaminododecane, g3, guazatine and mdl72527 is reported.
10 oct 2018 research output: contribution to journal › article › peer-review fingerprint dive into the research topics of 'investigating structure property.
The studies clearly indicate that polyamine length, charge, and terminal nitrogen substitution have a significant effect on how the tetraamine regulates mk-801 binding to the nmda receptor. Thus a structure-activity basis set on which future design of mk-801 agonists and antagonists can be based is now available.
The passmore laboratory uses a hybrid approach to study the structure and function of the main deadenylase activities are found within the evolutionarily.
2 structure–activity relationships of polyamine analogs as the second generation of chemotherapeutic agents, polyamine analogs have been a focus because their similarity to natural polyamines may interrupt the normal polyamine metabolic pathways, disrupt the polyamine pool, and ultimately cause damage to cancer cells.
They also found that diamine and polyamine analogues with chain lengths approaching that of spermidine and spermine were among the best inhibitors of polyamine uptake by l1210 cells (16). Studies with other uptake inhibitors indicated that n'jv@-dialkyl de rivatives were better inhibitors than n-acylspermidine derivatives (17).
We also include the recent structure–activity relationship studies and application of polyamine toxins as biological tools, including developing selective iglu subtype receptors and nach receptors antagonists, as well as templates to develop labeled and fluorescent polyamine toxin probes.
This structure-activity set makes it possible to establish the importance of charge, intercharge distance, and terminal nitrogen substitution on polyamine-regulated mk-801 binding in the nmda channel.
Finally, inclusion of reducible disulfide bonds to the polymer backbone increased transfection activity and reduced cytotoxicity.
In this study, the importance of the charged groups on the polyamine moiety for inhibition of mammalian nachr, nmdar and ampar has been addressed. When the polyamine chain of phtx-343 was reduced in length from phtx-343, through phtx-34, to phtx-3 antagonism potency declined for all three classes of ionotropic receptor.
The polyamine (pa) metabolism is involved in cell proliferation and differentiation. Increased cellular pa levels are observed in different types of cancers. These observations open a perspective to exploit the enzymes of pa catabolism as a target for anticancer drug design.
Preliminary structure/activity correlations, based only on data from the symmetrically alkylated polyamine analogs, suggested that monoalkylation at both terminal nitrogens of spermidine or spermine was important for optimal antiproliferative activity, and that alkylation at an internal nitrogen reduced in vitro activity (23).
The scope of mini-reviews in medicinal chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.
In vitro structure-activity relation study on the basis of our previous findings of effective hcc growth inhibition by the polyamine conjugates, two hcc cell lines (hepg2, smmc7721) were selected for the in vitro screen of novel flavonoid-polyamine conjugates.
As a part of our continuing studies on 'polyamines and their role in human disease' our considerations of structure–activity relationships (sar) within naturally.
Recent studies indicate that induction of polyamine catabolic enzymes ssat and spermine oxidase (smo) play key roles in the anti-proliferative and apoptotic effects of polyamine analogues and their combinations with chemotherapeutic agents such as 5-fluorouracil (5-fu) and paclitaxel.
Or spermidine, yet display substantially different structure activity relationships for polyamines that inhibit human carbonic anhydrases, biomed research.
Therefore, continuous structure–activity studies using there could be some uncharacterized oxidases present, rationally developed polyamine analogues are warranted. Which are capable of oxidizing polyamines, especially in moreover, similar studies with pathogens may reveal bovine serum used as a supplement in cell culture media.
The evaluation of a group of polyamine analogs as agents to ameliorate the activity of the compounds is very dependent on both the nature of the in addition to the subcutaneous studies, several compounds, n1,n11- diethylnorspermin.
The studies clearly indicate that polyamine length, charge, and terminal nitrogen substitution have a significant effect on how the tetraamine regulates mk-801 binding to the nmda receptor. Thus a structure−activity basis set on which future design of mk-801 agonists and antagonists can be based is now available.
The application of polyamine pharmacophores as vectors for intracellular transport of therapeutic agents by hua yao a dissertation presented to the graduate school.
4 dec 2018 (20) this led to the identification of functionalized polyamines as efficient rna conjugates for structure–affinity and structure–activity studies.
Increased synthesis of adomet but not of methionine during testosterone stimulation of polyamine studies on the oxidation state and biosynthesis of molybdopterin effect of limited proteolysis on structure and activity of phenylal.
The evaluation of a group of polyamine analogs as agents to ameliorate diarrhea-predominant irritable bowel syndrome is described. Each compound was assessed when administered subcutaneously in a psychological stress-induced model of irritable bowel syndrome in rodents for its ability to reduce stool output in a dose-dependent manner.
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