fibroblast activation protein (fap)

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。

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.

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。

SB03178是一种成纤维细胞活化蛋白-α (FAP) 的抑制剂，可通过与DOTA偶联，用于癌症研究。

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。

RO7122290 是一种双特异性抗体样融合蛋白，其结构由 T 细胞共刺激免疫受体 4-1BB (CD137) 的三聚体配体与靶向肿瘤相关成纤维细胞活化蛋白 (FAP) 的抗原结合片段 (Fab) 组成，展现出潜在的免疫调节和抗肿瘤活性。它可能用于治疗晚期实体瘤。分子量：177.78 KD。

3BP-3940是一种高效的成纤维细胞激活蛋白 (FAP) 靶向肽，常与放射性核素偶联用于肿瘤诊断和治疗。

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

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。

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。

FAPLigand 1（FL）为高亲和力小分子FAP配体，专用于将药物导向表达FAP的成纤维细胞，适用于癌症放射成像研究的靶向。

FAPI-2 TFA为一种针对成纤维细胞活化蛋白（FAP）的抑制剂，适用于癌症研究领域。

ARI-3144 是一种成纤维细胞激活蛋白 (FAP) 的优良底物，同时也是一种FAP激活的蛋白酶体抑制剂，适用于实体瘤研究。

DOTA.SA.FAPi TFA 是一种由方酸和 UAMC1110 构成的双功能性 DOTA 和 DATA5m 螯合剂.此化合物通过抑制成纤维细胞活化蛋白 (FAP),其 IC50 值达到 0.9 nM,并针对蛋白酶 PREP,展现出 5.4 μM 的 IC50 值.经68Ga标记的 DOTA.SA.FAPi TFA 可作为 PET 示踪剂,在癌症研究中发挥重要作用.

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。

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。

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-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。

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.

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。

TAM558intermediate-54 是 TAM558 合成过程中的一个中间体.TAM558 作为OMTX705合成的有效载荷分子.OMTX705为人源化抗成纤维细胞活化蛋白 (FAP) 抗体,通过结合 TAM470,展现出抗肿瘤活性.

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。

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.