Lys linked cyclic peptides related to hypoglycaemic analogues of human growth hormone hGH [6-13] have been examined. (eurekamag.com)
The success of the cyclisation reaction with the corresponding resin-bound, partially protected linear peptides was found to be both reagent as well as sequence dependent, with competing inter-chain oligomerisation predominating in some cases. (eurekamag.com)
The unique conformational constraint of cyclic peptides provides a larger surface area to interact with the target at the same time, improving the membrane permeability and in vivo stability compared to their linear counterparts. (nih.gov)
Currently, cyclic peptides have been reported to possess various activities, such as antifungal, antiviral and antimicrobial activities. (nih.gov)
2. Hybrid Cyclic-Linear Cell-Penetrating Peptides Containing Alternative Positively Charged and Hydrophobic Residues as Molecular Transporters. (nih.gov)
3. Cyclic and Linear Peptides Containing Alternate WW and RR Residues as Molecular Cargo Delivery Tools. (nih.gov)
4. Comparative Molecular Transporter Efficiency of Cyclic Peptides Containing Tryptophan and Arginine Residues. (nih.gov)
5. Comparative Molecular Transporter Properties of Cyclic Peptides Containing Tryptophan and Arginine Residues Formed through Disulfide Cyclization. (nih.gov)
10. Enhanced cellular uptake of short polyarginine peptides through fatty acylation and cyclization. (nih.gov)
15. Surface decorated gold nanoparticles by linear and cyclic peptides as molecular transporters. (nih.gov)
Additional studies with other substrate-mimicking cyclic peptides revealed that EarP activity is sensitive to the method used to induce cyclization and in some cases is tolerant to amino acid sequence variation. (rsc.org)
Trypsin-digested globin peptides with mass shifts consistent with the presence of HMVK monoadducts and cyclic diadducts were detected by LC/electrospray-quadrupole time-of-flight/MS with all rats given BDD. (nih.gov)
In this study, the goal was to design cyclic peptides (ADTC1, ADTC5, and ADTC6) derived from linear ADT6 (Ac-ADTPPV-NH2) to improve their stability and biological activity in improving paracellular delivery of drugs into the brain. (ku.edu)
In conclusion, formation of cyclic peptides can maintain cadherin peptide ability to modulate intercellular junctions of the BBB, and the primary sequence of ADT peptides is important for their biological activity. (ku.edu)
Out of 20 peptide derivatives, three peptides, NCGC00857950, a cyclic analog, NCGC00857001, connecting a lysine-coupled palmitic acid tail, and NCGC00591015 carrying a 10-carbon acyl group, were found to be 5- to 10-fold more potent in cell-based assays than parent peptide RP-182. (nih.gov)
Cyclic peptides have been considered ideal by many experts as therapeutics. (proteogenix.science)
Cyclization can increase the stability of peptides, making them more resistant to proteolytic cleavage. (proteogenix.science)
Cyclic peptides can be produced in a few minutes by cyclization in a microfluidic system. (ciil.fr)
Peptide12
To date, there is emerging interest in cyclic peptide therapeutics, and increasing numbers of clinically approved cyclic peptide drugs are available on the market. (nih.gov)
7. Efficient delivery of cell impermeable phosphopeptides by a cyclic peptide amphiphile containing tryptophan and arginine. (nih.gov)
12. Cyclic Peptide-Gadolinium Nanoparticles for Enhanced Intracellular Delivery. (nih.gov)
18. Cyclic peptide-selenium nanoparticles as drug transporters. (nih.gov)
19. Cyclic peptide-capped gold nanoparticles as drug delivery systems. (nih.gov)
20. Cyclic Peptide-Gadolinium Nanocomplexes as siRNA Delivery Tools. (nih.gov)
I am trying to generate conformations for a 29 residue cyclic peptide with N-C terminal cyclisation. (rosettacommons.org)
The results showed that ADTC1 has activity in inhibiting the resealing of the intercellular junctions of the MDCK cell monolayers similar to that of the linear ADT6, indicating that cyclization can maintain the peptide activity. (ku.edu)
60. "1D alignment of proteins and other nanoparticles by using reversible covalent bonds on cyclic peptide nanotubes" Priegue , J.M. (javiermontenegrochemistry.com)
The cyclization with a single non-peptide bond can lead them to be incorrectly called DEPSIPEPTIDES , but the echinocandins lack ester links. (bvsalud.org)
Here, we report the evaluation and implementation of the common industrial enzyme, microbial transglutaminase (mTG), as a versatile biocatalyst for cyclization of mRNA display peptide libraries via lysine-to-glutamine isopeptide bonds. (unc.edu)
Stable cyclic2
Loss of a water molecule and autoxidation convert cyclic diadduct 1 to a more stable cyclic diadduct 2. (nih.gov)
This aldehyde was found to undergo reversible cyclization to form the more stable cyclic carbamate 4-hydroxy-5-phenyl-tetrahydro-1,3-oxazin-2-one or undergo elimination to form 2-phenylpropenal. (aspetjournals.org)
Reaction5
The results also indicated that protection with the bulky Fmoc group of the amino acid residues immediately adjacent to the side chain-deprotected Lys and Glu residues, which participate in the cyclisation reaction, enhanced the rate of lactam formation. (eurekamag.com)
Upon reaction with a heteroleptic copper complex in the presence of an amine and under visible light irradiation, a range of ynamides were shown to smoothly cyclize to the corresponding azetidines, useful building blocks in natural product synthesis and medicinal chemistry, with full control of the regioselectivity of the cyclization resulting from a unique and underrated radical 4-exo-dig pathway. (nature.com)
c Reaction design: radical 4-exo-dig cyclization of ynamides triggered by visible-light activation with a photoredox catalyst (PC). (nature.com)
Type I terpene synthases (TPSs) activate these acyclic molecules by the abstraction of diphosphate to produce a reactive allyl cation that can initiate a cascade reaction through typical carbocation chemistry, including cyclisation reactions by intramolecular attack of an olefinic double bond to the cationic centre Wagner-Meerwein rearrangements, and proton or hydride migrations [2] . (beilstein-journals.org)
The synthetic route adopted began with the Beckmann rearrangement reaction and/or the Schmidt reaction of cyclic ketones to make lactams, which were then thionated by Curphy or Brillon procedures. (wits.ac.za)
Radical cyclization2
A general 4-exo-dig radical cyclization therefore remains untapped and meeting this challenge would be of high significance in terms of synthetic chemistry and, from more fundamental points of view, especially in terms of reactivity. (nature.com)
Methods enabling straightforward and efficient syntheses of cyclic organic molecules are therefore of utmost importance and it is not surprising that intramolecular cyclizations have been extensively studied over the years, resulting in the development of remarkably efficient reactions for the synthesis of a broad range of carbo- and hetero- cycles. (nature.com)
Ethers6
Cyclic diaryl ethers are present in multiple natural compounds, organic pollutants as well as in π-conjugated organic molecular materials. (unamur.be)
Rossignon, A & BONIFAZI, D 2019, ' O-Annulation Leading to Five-, Six-, and Seven-Membered Cyclic Diaryl Ethers Involving C-H Cleavage ', Synthesis (Germany) , VOL. 51, Numéro 19, p. 3588-3599. (unamur.be)
Why do cyclic ethers have higher boiling points than their acyclic isomers? (stackexchange.com)
Here are some more data comparing cyclic ethers to their acyclic isomers (and some analogs). (stackexchange.com)
The data I could find suggests that cyclic ethers have higher dipole moments than their acyclic counterparts. (stackexchange.com)
This seems consistent with intuitive expectations based on conformational models where, in the cyclic ethers where the molecular geometry is constrained by the ring, the lone pairs are pointing in the opposite direction from the carbon skeleton. (stackexchange.com)
Synthesis1
An improved synthesis of cyclic polyether-esters by cyclization", Liebigs Ann. (wikipedia.org)
Hydrolysis2
Specific cases include site-selective cycloaddition and addition of arenes, reduction of epoxides, α,β-unsaturated aldehydes, azides, halides and alkenes, oxidation of remote C-H bonds and alkenes, and substitution reactions involving ring-opening cyclization of epoxides, nucleophilic substitution of allylic chlorides, and hydrolysis reactions. (beilstein-journals.org)
This involved hydrolysis of the tert-butyl ester and cyclisation via a mixed anhydride. (wits.ac.za)
Chemistry1
AU - Igarashi,Tomohiro, AU - Arai,Shigeru, AU - Nishida,Atsushi, Y1 - 2013/04/18/ PY - 2013/4/11/entrez PY - 2013/4/11/pubmed PY - 2013/12/18/medline SP - 4366 EP - 72 JF - The Journal of organic chemistry JO - J Org Chem VL - 78 IS - 9 N2 - Anti carbocyanative cyclization using 1,6-enynes under nickel catalysis is described. (unboundmedicine.com)
Acyclic1
This map shows a few examples of acyclic and cyclic sesquiterpenoids. (genome.jp)
The similarity of these transformations led us to consider 5-phenyl-1,3-oxazinane-2,4-dione, which could arise from an oxidation of the cyclic carbamate, as a potential metabolite of felbamate. (aspetjournals.org)
Alkynes1
A general anti-Baldwin radical 4-exo-dig cyclization from nitrogen-substituted alkynes is reported. (nature.com)
Analogues1
New synthetic approach towards avibactam analogues and hypervalent iodine(III)-mediated cyclizations of unsaturated N-alkoxyureas. (viaf.org)
Reactions2
One HMVK-NAL cyclic diadduct (cyclic diadduct 1) also formed by sequential Michael addition reactions of two HMVK molecules with the epsilon-amino group of NAL followed by enolization and cyclization. (nih.gov)
These multistep cascade reactions ultimately result in terpene hydrocarbons that are often (poly)cyclic and contain several stereogenic centres [3,4] . (beilstein-journals.org)
Centres1
The presence of the nitrogen atom in between the radical centre and the triple bond could facilitate the 4-exo-dig cyclization by bringing the reacting centres in proximity, polarizing the triple bond and stabilizing the resulting vinyl radical (Fig. 1c ). (nature.com)
Affinity2
Surface area plasmon resonance and differential checking fluorometry analysis Guanosine 5′-diphosphate exposed that neither the affinity for antigen nor the thermal balance was disrupted from the scFv cyclization. (lacbiosafety.org)
To demonstrate the potential benefits of mTG-mediated cyclization in ligand discovery, high diversity mTG-modified libraries were employed in two separate affinity selections: (1) one against the calcium and integrin binding protein, CIB1, and (2) the second against the immune checkpoint protein and emerging therapeutic target, B7-H3. (unc.edu)
Linear3
6-N-Methyl NAD(+) (6-N-methyl nicotinamide adenosine 5'-dinucleotide 10) hydrolyzes to give the linear 6-N-methyl ADPR (adenosine 5'-diphosphoribose, 11), whereas 6-thio NHD(+) (nicotinamide 6-mercaptopurine 5'-dinucleotide, 17) generates a cyclic dinucleotide. (ox.ac.uk)
In the design and development of therapeutic agents, macromolecules with restricted structures have stronger competitive edges than linear biological entities since cyclization can overcome the limitations of linear structures. (nih.gov)
Terpenoid synthases are responsible for the cyclization and/or rearrangement of linear isoprenoid diphosphates into cyclic terpenoids [ 12 , 13 ]. (biomedcentral.com)
Formation2
While most cyclization modes are well documented, some of them still remain rather elusive, notably for the formation of small ring systems such as four-membered ones. (nature.com)
Use of matrix-assisted laser desorption ionization/Fourier transform ion cyclotron resonance provided further evidence for the formation of HMVK monoadducts and cyclic diadducts, and use of LC/MS/MS provided unequivocal evidence for adduction of HMVK with Cys125 of globin beta chains. (nih.gov)
Biological1
Aberrant cyclization affords a C-6 modified cyclic adenosine 5'-diphosphoribose analogue with biological activity in Jurkat T cells. (ox.ac.uk)
Activity4
In Jurkat T cells, unlike the parent cyclic inosine 5'-diphosphoribose N1-cIDPR 2, 6-thio N1-cIDPR antagonizes both cADPR- and N1-cIDPR-induced Ca(2+) release but possesses weak agonist activity at higher concentration. (ox.ac.uk)
In this protocol, we describe the design and use of an engineered cyclic herpes simplex virus 1-thymidine kinase (HSV1-TK) PET reporter whose kinase activity is specifically switched on by apoptosis. (nih.gov)
The expression of cyclic TK (cTK) in healthy cells leads to inactive product, whereas the activation of apoptosis through the caspase-3 pathway cleaves cTK, thus restoring its activity and enabling PET imaging. (nih.gov)
Both selections resulted in the identification of potent, cyclic, low nanomolar binders, and subsequent structure-activity studies demonstrate the importance of the cyclization to the observed activity. (unc.edu)
Structure1
v) Decyclization : This is opening up of ring structure of the cyclic drug molecule, e.g. barbiturates, phenytoin. (slideshare.net)
High1
Open-closed dynamics and aggregation had been suppressed in the cyclic scFv markedly, as judged from powerful light scattering and high-speed atomic push microscopy analyses. (lacbiosafety.org)
Product1
Surprisingly, NMR correlation spectra confirm this compound to be the N1 cyclic product 6-thio N1-cIDPR (6-thio cyclic inosine 5'-diphosphoribose, 3), although the corresponding 6-oxo analogue is well-known to cyclize at N7. (ox.ac.uk)
We also anticipated that our cyclic cMO strategy could be adapted to accommodate enzyme-mediated activation. (cdc.gov)
Lead1
It seems likely that the higher dipole moments in the cyclic compounds would lead to greater alignment / ordering in the liquid phase, which in turn would lead to higher boiling points. (stackexchange.com)
Potential1
Among these, the 4-exo-dig cyclization is certainly the least-explored one, despite a strong potential. (nature.com)
Study1
11 The 4,5-dimethoxy-2-nitrobenzyl (DMNB)-containing linkers used in our previous study allowed optical MO uncaging, but cyclic cMOs could accommodate enzyme-cleavable linkers as well. (cdc.gov)
Examples2
However, examples of such cyclizations are still limited. (nature.com)
b Rare examples of radical 4-exo-dig and 5-endo-dig cyclizations. (nature.com)