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基本描述
| 产品名称 | TL1A |
|---|
产品规格参数
| CAS编号和信息 | rp175308 |
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数据库链接
| UniProtKB | O95150 |
|---|---|
| Wikipedia | TNFSF15 |
| RCSB PDB Structure | 2O0O |
| Ensembl Gene | ENSG00000181634 |
| CATH/Gene3D | 2.60.120.40 |
靶标
| Target ID | 1883 | ||||||||||||||||||||||||
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| 名称 | death receptor 3 | ||||||||||||||||||||||||
| 缩写名 | DR3 | ||||||||||||||||||||||||
| 家族 | Tumour necrosis factor (TNF) receptor family | ||||||||||||||||||||||||
| 基因和蛋白信息 |
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| Ensembl Gene | ENSMUSG00000024793 (Mm) , ENSRNOG00000021814 (Rn) , ENSG00000215788 (Hs) | ||||||||||||||||||||||||
| Entrez Gene | 85030 (Mm) , 500592 (Rn) , 8718 (Hs) | ||||||||||||||||||||||||
| OMIM | 603366 (Hs) | ||||||||||||||||||||||||
| Protein GI | 114145579 (Mm) , 212549637 (Rn) , 89142745 (Hs) | ||||||||||||||||||||||||
| UniProtKB | Q93038 (Hs) |
关联配体
| Ligand ID | 5071 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | TL1A | ||||||||||
| 别名 | Tumor necrosis factor ligand superfamily member 15, membrane form | ||||||||||
| 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 |
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| 评价 |
TL1A occurs as both membrane‐bound and soluble forms. It principally functions as a negative modulator of epithelial cell proliferation. Inhibiting the TL1A/death receptor 3 (TNFRSF25) pathway has been proposed as mechanism to treat inflammatory bowel disease |
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| 配体家族 | Tumor necrosis factor superfamily ligands | ||||||||||
| 基因/前体 |
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| 单字母多肽序列 | MAEDLGLSFGETASVEMLPEHGSCRPKARSSSARWALTCCLVLLPFLAGLTTYLLVSQLRAQGEACVQFQALKGQEFAPSHQQVYAPLRADGDKPRAHLTVVRQTPTQHFKNQFPALHWEHELGLAFTKNRMNYTNKFLLIPESGDYFIYSQVTFRGMTSECSEIRQAGRPNKPDSITVVITKVTDSYPEPTQLLMGTKSVCEVGSNWFQPIYLGAMFSLQEGDKLMVNVSDISLVDYTKEDKTFFGAFLL | ||||||||||
| 三字母多肽序列 | |||||||||||
| 翻译后修饰 | Predicted N-linked glycosylation of asparagine residues at positions 133 and 229; disulphide bond formation between cysteine residues at positions 162 and 202 | ||||||||||
| 化学修饰 | |||||||||||
| 临床描述 |
This phase 2b study is designed to have all subjects go into a 12 week induction period to compare different doses of study drug against placebo. After induction is complete all subjects will receive active therapy for 40 weeks, followed by a 12 week follow up period. |
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| 来源公司 |
Pfizer |
参考文献
| 1. Kakuta Y, Kinouchi Y, Negoro K, Takahashi S, Shimosegawa T. (2006) Association study of TNFSF15 polymorphisms in Japanese patients with inflammatory bowel disease.. Gut, 55 (10): (1527-8). [PMID:16966713] |
| 2. Picornell Y, Mei L, Taylor K, Yang H, Targan SR, Rotter JI. (2007) TNFSF15 is an ethnic-specific IBD gene.. Inflamm Bowel Dis, 13 (11): (1333-8). [PMID:17663424] |
| 3. Lagou S, Grapsa D, Syrigos N, Bamias G. (2022) The Role of Decoy Receptor DcR3 in Gastrointestinal Malignancy.. Cancer Diagn Progn, 2 (4): (411-421). [PMID:35813013] |
| 4. Danese S, Klopocka M, Scherl EJ, Romatowski J, Allegretti JR, Peeva E, Vincent MS, Schoenbeck U, Ye Z, Hassan-Zahraee M et al.. (2021) Anti-TL1A Antibody PF-06480605 Safety and Efficacy for Ulcerative Colitis: A Phase 2a Single-Arm Study.. Clin Gastroenterol Hepatol, 19 (11): (2324-2332.e6). [PMID:34126262] |
| 5. Zhang T, Ning WW, Zhang J, Xu FJ, Wang XQ, Li ZB, Xie M. (2022) Nonylphenol regulates TL1A through the AhR/HDAC2/HNF4α pathway in endothelial cells to promote the angiogenesis of colorectal cancer.. Toxicol Appl Pharmacol, 436 (13): (115854). [PMID:34974051] |
| 6. Gao Y, Wang Y, Wang X, Wang Y, Zhang X, Sun X. (2019) TNF-like ligand 1A is associated with progression and prognosis of human gastric cancer.. Onco Targets Ther, 12 (13): (7715-7723). [PMID:31571922] |
| 7. Banfield C, Rudin D, Bhattacharya I, Goteti K, Li G, Hassan-Zahraee M, Brown LS, Hung KE, Pawlak S, Lepsy C. (2020) First-in-human, randomized dose-escalation study of the safety, tolerability, pharmacokinetics, pharmacodynamics and immunogenicity of PF-06480605 in healthy subjects.. Br J Clin Pharmacol, 86 (4): (812-824). [PMID:31758576] |
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