125238-99-5Relevant articles and documents
COMPOUND FOR PREPARATION OF ANTIBODY-PAYLOAD CONJUGATE AND USE THEREOF
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, (2022/03/15)
The present application relates to a novel linker for use in bioconjugation, comprising two or more electrophilic carbon atoms of a carbonyl group, and a click chemistry functional group and, more specifically, to a linker through which a compound, a peptide, and/or a protein can be directly and/or indirectly linked by a substitution reaction to a desired target molecule, that is, a target molecule.
Practical and efficient synthesis of orthogonally protected α-2,3-diaminopropionic acid (2,3-Dap), 2,4-diaminobutanoic acid (2,4-Dab), and their N-methylated derivatives
Rao, R. V. Ramana,Tantry, Subramanyam J.,Babu, Vommina V. Suresh
, p. 2901 - 2912 (2007/10/03)
The synthesis of orthogonally protected Fmoc-Dap/Dab (Boc/Z/Alloc)-OH starting from Fmoc-Asp/Glu has been described. The salient features of our synthetic strategy involved formation of Fmoc-Asp/Glu-5-oxazolidinone acids, conversion of acid function to acyl azides, Curtius rearrangement, and hydrolysis of the oxazolidinone group. Copyright Taylor & Francis Group, LLC.
A new somatostatin analog with optimized ring size inhibits neointima formation induced by balloon injury in rats without altering growth hormone release
Thurieau,Janiak,Krantic,Guyard,Pillon,Kucharczyk,Vilaine,Fauchere
, p. 115 - 122 (2007/10/02)
We report on the synthesis and pharmacological properties of a new series of somatostatin analogs. Two lower homologs of lysine, 2,3-diaminopropanoic acid and 2,4-diaminobutyric acid, were prepared and used for cyclization via amide formation with the side chain of aspartic or glutamic acid in place of natural cystine present in many somatostatin analogs. One resulting compound, although having low binding affinities for somatostatin receptors, displayed a strong potency in inhibiting neointima formation induced by balloon injury in rats at the dose of 100 μg·kg-1·d-1. This dissociation of the antiproliferative effect from the endocrine effect seems to indicate that myointimal growth is not related to a change in growth hormone secretion.