专利号:US-2024066133-A1 优先权日:2020-03-06 标 题 :Therapeutic agents and conjugates thereof 发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.
专利号:US-12102685-B2 优先权日:2020-03-26 标 题:Immodulator peptides covalently modified with small molecules 发明人:MASCARENHAS DESMOND 权利人:MASCARENHAS DESMOND 摘要:This invention provides modified IGFBP-derived peptides—collectively termed “immodulator peptidesâ€?—and related compositions and methods. Chemical modifications to peptides using small molecules, and sequence extensions to immodulator core sequences exhibit new and surprising biological activities. The invention builds the combinatorial power of the immodulator peptide class further by demonstrating which core sequences bind metal or glycosaminoglycans such as heparin. The invention discloses some surprising biological properties of compositions derived from these modifications, including a host of new therapeutic and diagnostic utilities (e.g. immune modulation of TLR signaling, enhanced collagen synthesis by skin fibroblasts, and synergy with a RIG-I agonist in killing melanoma cells). The invention also teaches methods for enhancing previously disclosed uses of immodulator peptides by showing how the modifications of the invention can boost the efficacy of immodulator peptides in a model of burn trauma.
专利号:US-11674950-B2 优先权日:2017-10-31 标题 :Methods determining and treating cellular resistance to ADP-rtbosylating toxin 发明人:LANE ANDREW; ASTER JON 权利人:DANA FARBER CANCER INST INC; BRIGHAM & WOMENS HOSPITAL INC 摘要:The present invention is based in part on the identification of DPH1 and other members of the diphthamide synthesis pathway as biomarkers of resistance to an ADP-ribosylating toxin in a cell, and methods for identification, assessment, and treatment of a condition that is resistant to an ADP-ribosylating toxin.
1: Kong FX, Liu H, Xu T, Li SJ, Li W, Lu H, Ma NN, Wang YL, Shi JH, Yang YR, Wang FL. RG108 attenuates acute kidney injury by inhibiting P38 MAPK/FOS and JNK/JUN pathways. Int Immunopharmacol. 2024 Sep 11;142(Pt A):113077. doi: 10.1016/j.intimp.2024.113077. Epub ahead of print. 22(2):e3863. doi: 10.30498/ijb.2024.435096.3863. 3: Li L, Pang W, Xu L, Zhang Y, Zhang H, Zhu L, Li Y, Lin H, Mo L, Liu Y, Wang L, Yang P. Inhibition of DNMT1 attenuates experimental food allergy. Mol Immunol. 2024 Sep;173:71-79. doi: 10.1016/j.molimm.2024.07.009. Epub 2024 Jul 26. 5(7):e652. doi: 10.1002/mco2.652. 5: Tang YW, Jiang MY, Cao JW, Wan F. Triptolide decreases podocytes permeability by regulating TET2-mediated hydroxymethylation of ZO-1. Exp Biol Med (Maywood). 2024 May 31;249:10051. doi: 10.3389/ebm.2024.10051.
合成参考文献
参考文献:10.1007/s00726-004-0109-1 摘要:Zeng Q, Liu Z, Li B, Wang F. Mild and effective N-phthaloylation of amino acids. Amino Acids. 2004 Oct;27(2):183–6. doi: 10.1007/s00726-004-0109-1.