scholarly journals Automated synthesis of backbone protected peptides

2014 ◽  
Vol 50 (61) ◽  
pp. 8316-8319 ◽  
Author(s):  
Abu-Baker M. Abdel-Aal ◽  
George Papageorgiou ◽  
Martin Quibell ◽  
John Offer
Keyword(s):  
Automated Synthesis ◽  
Peptide Backbone ◽  
Protected Peptides

The automated introduction of removable substitution along a peptide backbone prevents chain-association and synthesis failure.

Engineering “Antimicrobial Peptides” and Other Peptides to Modulate Protein-Protein Interactions in Cancer

2020 ◽  
Vol 20 (32) ◽  
pp. 2970-2983
Author(s):  
Samuel J.S. Rubin ◽  
Nir Qvit
Keyword(s):  
Antimicrobial Peptides ◽  
Protein Interactions ◽  
Anticancer Agents ◽  
Cancer Therapeutics ◽  
Target Cells ◽  
Protein Protein Interactions ◽  
Peptide Backbone ◽  
Modified Peptides ◽  
Selective Death ◽  
Drug Leads

Antimicrobial peptides (AMPs) are a class of peptides found across a wide array of organisms that play key roles in host defense. AMPs induce selective death in target cells and orchestrate specific or nonspecific immune responses. Many AMPs exhibit native anticancer activity in addition to antibacterial activity, and others have been engineered as antineoplastic agents. We discuss the use of AMPs in the detection and treatment of cancer as well as mechanisms of AMP-induced cell death. We present key examples of cathelicidins and transferrins, which are major AMP families. Further, we discuss the critical roles of protein-protein interactions (PPIs) in cancer and how AMPs are well-suited to target PPIs based on their unique drug-like properties not exhibited by small molecules or antibodies. While peptides, including AMPs, can have limited stability and bioavailability, these issues can be overcome by peptide backbone modification or cyclization (e.g., stapling) and by the use of delivery systems such as cellpenetrating peptides (CPPs), respectively. We discuss approaches for optimizing drug properties of peptide and peptidomimetic leads (modified peptides), providing examples of promising techniques that may be applied to AMPs. These molecules represent an exciting resource as anticancer agents with unique therapeutic advantages that can target challenging mechanisms involving PPIs. Indeed, AMPs are suitable drug leads for further development of cancer therapeutics, and many studies to this end are underway.

Automated synthesis of PEG-coupled antisense-oligonucleotides

1993 ◽  
Vol 58 (s1) ◽  
pp. 204-208 ◽  
Author(s):  
Andres Jäschke ◽  
Jens P. Fürste ◽  
Dieter Cech ◽  
Volker A. Erdmann
Keyword(s):  
Antisense Oligonucleotides ◽  
Automated Synthesis

Modification of an Anion-Exchange Procedure for 68Ga Preconcentration and Automated Synthesis of [68Ga]Ga-PSMA-11

2019 ◽  
Vol 61 (6) ◽  
pp. 748-753
Author(s):  
D. O. Antuganov ◽  
D. V. Ryzhkova ◽  
V. V. Timofeev ◽  
T. A. Zykova ◽  
Yu. O. Antuganova ◽  
...  
Keyword(s):  
Anion Exchange ◽  
Automated Synthesis

scholarly journals Hybrid Cyclobutane/Proline-Containing Peptidomimetics: The Conformational Constraint Influences Their Cell-Penetration Ability

2021 ◽  
Vol 22 (10) ◽  
pp. 5092
Author(s):  
Ona Illa ◽  
Jimena Ospina ◽  
José-Emilio Sánchez-Aparicio ◽  
Ximena Pulido ◽  
María Ángeles Abengozar ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cell Penetrating Peptides ◽  
Cell Uptake ◽  
Relevant Parameter ◽  
Intracellular Accumulation ◽  
Peptide Backbone ◽  
New Family ◽  
Cell Line Hela ◽  
Penetration Ability ◽  
Tumoral Cell

A new family of hybrid β,γ-peptidomimetics consisting of a repetitive unit formed by a chiral cyclobutane-containing trans-β-amino acid plus a Nα-functionalized trans-γ-amino-l-proline joined in alternation were synthesized and evaluated as cell penetrating peptides (CPP). They lack toxicity on the human tumoral cell line HeLa, with an almost negligible cell uptake. The dodecapeptide showed a substantial microbicidal activity on Leishmania parasites at 50 µM but with a modest intracellular accumulation. Their previously published γ,γ-homologues, with a cyclobutane γ-amino acid, showed a well-defined secondary structure with an average inter-guanidinium distance of 8–10 Å, a higher leishmanicidal activity as well as a significant intracellular accumulation. The presence of a very rigid cyclobutane β-amino acid in the peptide backbone precludes the acquisition of a defined conformation suitable for their cell uptake ability. Our results unveiled the preorganized charge-display as a relevant parameter, additional to the separation among the charged groups as previously described. The data herein reinforce the relevance of these descriptors in the design of CPPs with improved properties.

Automated Synthesis of Comprehensive Memory Model Litmus Test Suites

2017 ◽  
Vol 45 (1) ◽  
pp. 661-675
Author(s):  
Daniel Lustig ◽  
Andrew Wright ◽  
Alexandros Papakonstantinou ◽  
Olivier Giroux
Keyword(s):  
Memory Model ◽  
Automated Synthesis ◽  
Litmus Test ◽  
Test Suites

Automated synthesis of custom networks-on-chip for real world applications

2020 ◽  
Author(s):  
Anup Gangwar ◽  
Nitin Kumar Agarwal ◽  
Ravishankar Sreedharan ◽  
Ambica Prasad ◽  
Sri Harsha Gade ◽  
...  
Keyword(s):  
Real World ◽  
Automated Synthesis ◽  
Networks On Chip ◽  
Real World Applications ◽  
On Chip

Automated Synthesis Modules for PET Radiochemistry

2020 ◽  
pp. 437-456
Author(s):  
Laura Bruton ◽  
Peter J.H. Scott
Keyword(s):  
Automated Synthesis

scholarly journals Clinically Applicable Cyclotron-Produced Gallium-68 Gives High-Yield Radiolabeling of DOTA-Based Tracers

Biomolecules ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1118
Author(s):  
Emma Jussing ◽  
Stefan Milton ◽  
Erik Samén ◽  
Mohammad Mahdi Moein ◽  
Lovisa Bylund ◽  
...  
Keyword(s):  
Metal Ion ◽  
Metal Content ◽  
Gamma Spectroscopy ◽  
Radiochemical Yield ◽  
High Yield ◽  
Automated Synthesis ◽  
Molar Activity ◽  
Icp Ms ◽  
Gallium 68 ◽  
Fe Impurities

By using solid targets in medical cyclotrons, it is possible to produce large amounts of 68GaCl3. Purification of Ga3+ from metal ion impurities is a critical step, as these metals compete with Ga3+ in the complexation with different chelators, which negatively affects the radiolabeling yields. In this work, we significantly lowered the level of iron (Fe) impurities by adding ascorbate in the purification, and the resulting 68GaCl3could be utilized for high-yield radiolabeling of clinically relevant DOTA-based tracers. 68GaCl3 was cyclotron-produced and purified with ascorbate added in the wash solutions through the UTEVA resins. The 68Ga eluate was analyzed for radionuclidic purity (RNP) by gamma spectroscopy, metal content by ICP-MS, and by titrations with the chelators DOTA, NOTA, and HBED. The 68GaCl3eluate was utilized for GMP-radiolabeling of the DOTA-based tracers DOTATOC and FAPI-46 using an automated synthesis module. DOTA chelator titrations gave an apparent molar activity (AMA) of 491 ± 204 GBq/µmol. GMP-compliant syntheses yielded up to 7 GBq/batch [68Ga]Ga-DOTATOC and [68Ga]Ga-FAPI-46 (radiochemical yield, RCY ~ 60%, corresponding to ten times higher compared to generator-based productions). Full quality control (QC) of 68Ga-labelled tracers showed radiochemically pure and stable products at least four hours from end-of-synthesis.

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