Introduction: Radioimmunotherapy (RIT) is a very promising new therapy for the treatment of recurrent B-Cell non-Hodgkin's lymphoma (NHL). Iodine-131 is the most frequently used nuclide in clinical RIT, but its usefulness has been limited by dehalogenation of monoclonal antibodies labeled via conventional methods. To circumvent this problem, we have synthesized a tr...

introduction: radioimmunotherapy (rit) is a very promising new therapy for the treatment of recurrent b-cell non-hodgkin's lymphoma (nhl). iodine-131 is the most frequently used nuclide in clinical rit, but its usefulness has been limited by dehalogenation of monoclonal antibodies labeled via conventional methods. to circumvent this problem, we have synthesized a tri-peptide consisting of non-m...

Background: UBI 29-41 (a derivative of antimicrobial peptide ubiquicidin) labelled with 99mTc is reported to discriminate between bacterial infections and sterile inflammatory processes. In this study, three lyophilized kit were performed, one of them based on the direct labelling with only SnCl2 as reducing agent , and other two based on 6- hydrazinopyridine-3-carboxylic acid (HYNIC) and trici...

Introduction During an evaluation of azido-α-amino acids and their utility in solid-phase peptide chemistry, the octapeptide angiotensin II and a tripeptide thyrotropin-releasing hormone (TRH) analog have been prepared using Meldal’s procedure [1]. A necessary novel step was the reduction of the azido moiety of L-proline, a secondary amine constrained by a ring, to the corresponding free amine ...

Solid Phase Peptide Synthesis (SPPS) is a key technology for the production of pharmaceutical grade peptides and replacement piperidine with alternative bases piece puzzle moving toward greener technology.

Heptapeptides containing residues with terminal olefin-derivatized side chains (3 and 4) have been treated with ruthenium alkylidene 1 and undergone facile ring-closing olefin metathesis (RCM) to give 21- and 23-membered macrocyclic peptides (5 and 6). The primary structures of peptides 3 and 4 were based upon a previously studied heptapeptide (2), which was shown to adopt a predominantly 3(10)...

Abstract The conversion of C?H bonds to C?N offers a sustainable and economical strategy for the synthesis nitrogen-containing compounds. However, challenges regarding control regio- stereoselectivity currently limit broad applicability intermolecular C( sp 3 )?H amination reactions. We address these restrictions by directed nitrene-mediated insertion using metal-coordinating functional group. ...

Recombinant peptide synthesis allows for large-scale production of peptides with therapeutic potential. However, access to dicarba peptidomimetics via sidechain-deprotected sequences becomes challenging exposed Lewis basicity presented by amine and sulfur-containing residues. Presented here is a combination strategies which can be used deactivate coordinative residues achieve high-yielding Ru-c...