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tumour necrosis factor shed form

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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
rp175336-500μg 500μg 期货 Stock Image
rp175336-1mg 1mg 期货 Stock Image

基本描述

产品名称 tumour necrosis factor shed form

产品规格参数

CAS编号和信息 rp175336

靶标

Target ID 1870
名称 tumor necrosis factor receptor 1
缩写名 TNFR1
家族 Tumour necrosis factor (TNF) receptor family
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 455 12p13.31 TNFRSF1A TNF receptor superfamily member 1A
Mouse 1 454 6 59.32 cM Tnfrsf1a tumor necrosis factor receptor superfamily, member 1a
Rat 1 461 4q42 Tnfrsf1a TNF receptor superfamily member 1A
Ensembl Gene ENSG00000067182 (Hs) , ENSMUSG00000030341 (Mm) , ENSRNOG00000031312 (Rn)
Entrez Gene 21937 (Mm) , 25625 (Rn) , 7132 (Hs)
OMIM 191190 (Hs)
Protein GI 4507575 (Hs) , 31560799 (Mm) , 6981664 (Rn)
UniProtKB P19438 (Hs) , P25118 (Mm) , P22934 (Rn)
ChEMBL Target CHEMBL3378 (Hs)

关联配体

Ligand ID 5074
名称 tumour necrosis factor shed form
别名 cachectin
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 TNFα is a pro-inflammatory, acute phase cytokine involved in systemic inflammation.
The TNF precursor is expressed as a membrane-bound ligand, which is cleaved by TACE/ADAM17 to form this shed (or 'soluble') bioactive cytokine containing just the extracellular domain, and that circulates predominantly as a homotrimer. Recombinant TNF is used as an immunostimulant under the INN tasonermin.

Circulating active TNF-α is the principal molecular target of the anti-TNF therapeutics and . A smaller and longer acting and orally deliverable anti-TNF biologic called V565 is in early stage clinical development . Considering alternative modes of administration, V565 is a heavy chain only variable domain anti-TNF nanobody generated in Ilama that is further modified to enhance resistance to protease-mediated degradation. It binds shed TNF-α with similar affinity to infliximab and adalimumab, and also inhibits biological responses mediated by membrane-bound TNF-α . If this design strategy proves successful, V565 will be the first orally active anti-TNF therapy. V565 is being evaluated for potential to treat Crohn's disease (see Phase 2 study NCT02976129).
配体家族 Tumor necrosis factor superfamily ligands
基因/前体
Gene symbol Gene name Precursor protein name Species 别名
TNF tumor necrosis factor prepro-tumor necrosis factor Human TNFA, TNFSF2, DIF, TNF-alpha, tumor necrosis factor (TNF superfamily, member 2), TNF superfamily, member 2
单字母多肽序列 VRSSSRTPSDKPVAHVVANPQAEGQLQWLNRRANALLANGVELRDNQLVVPSEGLYLIYSQVLFKGQGCPSTHVLLTHTISRIAVSYQTKVNLLSAIKSPCQRETPEGAEAKPWYEPIYLGGVFQLEKGDRLSAEINRPDYLDFAESGQVYFGIIAL
三字母多肽序列
翻译后修饰 O-linked glycosylation of serine residue at position 4; disulphide bond formation between cysteine residues at positions 69 and 101
化学修饰

参考文献

1. Tracey D, Klareskog L, Sasso EH, Salfeld JG, Tak PP.  (2008)  Tumor necrosis factor antagonist mechanisms of action: a comprehensive review..  Pharmacol Ther,  117  (2):  (244-79).  [PMID:18155297]
2. Crowe JS, Roberts KJ, Carlton TM, Maggiore L, Cubitt MF, Clare S, Harcourt K, Reckless J, MacDonald TT, Ray KP et al..  (2018)  Preclinical Development of a Novel, Orally-Administered Anti-Tumour Necrosis Factor Domain Antibody for the Treatment of Inflammatory Bowel Disease..  Sci Rep,  (1):  (4941).  [PMID:29563546]
3. Gahring LC, Carlson NG, Kulmar RA, Rogers SW.  (1996)  Neuronal expression of tumor necrosis factor alpha in the murine brain..  Neuroimmunomodulation,  (5):  (289-303).  [PMID:9218250]

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