- Synthesis and structural characterization of triple-helical peptided which mimic the ligand binding site of the human macrophage scavenger receptor
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A synthetic method for triple-helical peptides was developed. Peptides with and without glutamic acid a-thioester at their N-termini are prepared by the solid-phase method. These peptides are crosslinked at their N-termini one by one to generate trimeric peptides using the activation of the thioester group by silver ions. This method was applied to the synthesis of model peptides, which mimic the binding site of modified low density lipoprotein (LDL) in the human scavenger receptor (SR). These models possessed different spacers, which connect the peptide chains and the crosslinking site. CD and DSC analysis of the peptides revealed that spacer length has a critical effect on the stability of the triple helix.
- Hojo, Hironobu,Akamatsu, Yoshiko,Yamauchi, Kiyoshi,Kinoshita, Masayoshi,Miki, Shunji,Nakamura, Yu
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- Site-Specific Incorporation of Multiple Thioamide Substitutions into a Peptide Backbone via Solid Phase Peptide Synthesis
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Among various peptide modification strategies, thioamide substitution by replacing the carbonyl oxygen atom of an amide bond with a sulfur atom constitutes an invaluable tool for chemical biology, for use in peptide drug discovery and protein structure-fu
- Yang, Jinhua,Wang, Changliu,Yao, Chaochao,Chen, Chunqiu,Hu, Yafang,He, Guifeng,Zhao, Junfeng
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p. 1484 - 1494
(2020/01/02)
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- ANTI-CD40 ANTIBODY DRUG CONJUGATES
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Provided herein are anti-CD40 antibody drug conjugates comprising a radical of Formula (I), wherein R1, R2, and R3 are as defined herein. Further provided are anti-CD40 antibody drug conjugates of Formula (II), wherein Z, R, AA1, AA2, AA3, m, p, q, n, w, R1, R2, and R3 are as defined herein. Further provided are pharmaceutical compositions and kits thereof, and methods of using same.
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Paragraph 00191
(2019/06/17)
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- ANTI-MSR1 ANTIBODIES AND METHODS OF USE THEREOF
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Provided herein are antibodies and antigen-binding fragments that bind MSR1 and methods of use thereof. According to certain embodiments, the antibodies bind human MSR1 with high affinity. In certain embodiments, the antibodies bind MSR1 without blocking, or blocking less than 90%, of modified LDL binding to MSR1. In some embodiments, the antibodies bind cell surface expressed-MSR1 and are internalized. The antibodies of the invention may be fully human antibodies. The invention includes anti-MSR1 antibodies, or antigen-binding fragments thereof, conjugated to drugs or therapeutic compounds.
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Paragraph 0585; 0586
(2019/11/28)
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