fibroblast activation protein

FAPI-4 是一种成纤维细胞激活蛋白 (FAP) 抑制剂，是FAPI配体，在原发性肝癌肝细胞癌（HCC）的PET成像中显示出强烈的肝脏摄取作用，常用于 PET 成像，可用于研究癌症。

Trimethylamine N-oxide（TMAO）是肠道微生物依赖性代谢产物，由膳食胆碱、甜菜碱和肉碱转化而来，能通过激活ROS NLRP3炎症小体诱导炎症，并通过激活TGF-β Smad2信号通路促进成纤维细胞分化，常用于构建心脏纤维化模型。

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Talabostat mesylate (PT100) 是一种具有口服活性和非选择性的二肽基肽酶 IV 抑制剂(IC50< 4 nM;Ki= 0.18 nM)。Talabostat mesylate 是成纤维细胞活化蛋白的第一个临床抑制剂(IC50= 560 nM)，抑制 DPP8 9 (IC50= 4 11 nM;Ki= 1.5 0.76 nM)，静息细胞脯氨酸二肽酶(IC50= 310 nM)、DPP2 和一些其他 DASH 家族酶。Talabostat mesylate 具有抗肿瘤和造血刺激活性 。

FAP targeting peptide for FXX489是 FXX489的多肽组成部分。FXX489是一种能够特异性识别并结合成纤维细胞活化蛋白（FAP）的靶向性配体。

FAPI-2 是一种基于放射性示踪剂 FAP 标记的成纤维细胞活化蛋白特异性抑制剂，具有抗癌活性，可用于研究胰腺癌。

ML334 (LH601A) 是一种可穿过细胞膜且具有有效性的 NRF2 激活剂，抑制 Keap1-NRF2 蛋白质相互作用，抑制心脏成纤维细胞活化和增殖来改善心肌梗死诱导的心脏纤维化。

DOTAGA.(SA.FAPi)2 TFA 作为一种高效的二聚体成纤维细胞激活蛋白抑制剂 (FAPi)，展示出在癌症诊断研究中的应用潜力。

FAPI-mFS，作为一种不可逆的成纤维细胞活化蛋白 (FAP) 抑制剂，通过与FAP形成共价结合来提高在癌细胞中的摄取与滞留。此化合物在标记放射性68Ga或177Lu后，可应用于癌症的成像与治疗领域。

3BP-3580 是一种靶向成纤维细胞活化蛋白 (FAP) 的抑制剂 (pIC50: 8.6)，适用于癌症研究。

ARI-3099 inhibits fibroblast activation protein, alpha (FAP).

FAPI-46是一种基于喹啉的成纤维细胞激活蛋白（FAP）放射性示踪剂，属于FAP抑制剂（FAPi）,能够和68Ga或177Lu等标记物偶联，在正电子发射断层扫描（PET）中作为示踪剂表达FAP肿瘤。

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

NOTA-FAPI-4 is an analogue of FAPI-4 and a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI-4 is useful in the diagnosis or treatment of a disease characterized by overexpression of fibroblast activation protein (FAP). NOTA-FAPI-4 can be used as a PET tracer for detection of diseases or disorders related to fibroblast activation protein.

Suc-Gly-Pro-AMC 是一种成纤维细胞活化蛋白 (FAP) 特异性底物。Suc-Gly-Pro-AMC 可用于研究 FAP 的活性。

FSDD0I为一种与白蛋白结合的成纤维细胞活化蛋白(FAP)配体，能够与68Ga和177Lu标记，用于单光子发射计算机断层扫描(SPECT)成像。

FSDD1I为白蛋白结合成纤维细胞活化蛋白(FAP)配体，可68Ga和177Lu标记，用于单光子发射计算机断层扫描(SPECT)成像。

FSDD3I 是一种配体，特别是针对白蛋白结合成纤维细胞活化蛋白 (FAP) 的。它能够以68Ga 和177Lu 进行标记，进而应用于单光子发射计算机断层扫描 (SPECT) 成像技术。

FAP-2286，一种与放射性核素螯合剂 DOTA 偶联的 FAP 结合肽大环化合物。FAP-2286 对人 FAP 蛋白具有强亲和力，Kd 为 1.1 nM。FAP-2286 具有抗肿瘤活性。FAP-2286 可用放射性核素标记，用于治疗及诊断。

FAP-2286 acetate，一种与成纤维细胞活化蛋白(FAP)结合的肽偶联物，可通过放射性核素标记进行诊断应用，并展现出抗肿瘤活性。

FAP-IN-2 TFA为99mTc标记的异腈类FAP抑制剂衍生物，适用于肿瘤显像。

SP-13786 是成纤维细胞活化蛋白 (FAP)和脯氨酰寡肽酶 (PREP)的抑制剂，IC50值分别为3.2 nM和1.8μM。

FAP-IN-1，一种FAP (成纤维细胞激活蛋白)抑制剂，具有3.3 nM的IC50值，适用于癌症研究。

FAP-IN-2，一种标记有99mTc的含异腈FAPI（成纤维细胞活化蛋白）抑制剂衍生物，适用于肿瘤显像。