fap-1

FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 of 3.3 nM, used for cancer research [1].

FAP Ligand 1 (FL), a high-affinity small molecule targeting fibroblast activation protein (FAP), facilitates the delivery of conjugated therapeutics to FAP-expressing fibroblasts and enables radiographic imaging of select tumors [1].

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.

Fas C-Terminal Tripeptide Acetate shows inhibitory activity of Fas FAP-1 binding.

FAP-PI3KI1, a fibroblast-activated protein (FAP)-targeted PI3K inhibitor, selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells. It effectively inhibits collagen synthesis and reduces collagen deposition [1].

Suc-Gly-Pro-AMC, a fibroblast activation protein (FAP)-specific substrate, facilitates the examination of FAP activity [1].

FSDD0I, an albumin-binding fibroblast activation protein (FAP) ligand, can be labeled with 68Ga and 177Lu for use in single photon emission computed tomography (SPECT) imaging [1].

FSDD1I, an albumin-binding fibroblast activation protein (FAP) ligand, can be tagged with 68 Ga and 177 Lu for use in single photon emission computed tomography (SPECT) imaging [1].

FSDD3I, an albumin-binding fibroblast activation protein (FAP) ligand, can be tagged with isotopes 68Ga and 177Lu for use in single photon emission computed tomography (SPECT) imaging [1].

FAP-2286 is a peptidic macrocycle that binds to the fibroblast activation protein (FAP) and is linked to the chelator DOTA, facilitating its role as a tumor imaging agent in positron emission tomography (PET) research. Exhibiting strong affinity for the human FAP protein with a dissociation constant (Kd) of 1.1 nM, FAP-2286 demonstrates significant antitumor activity, as referenced in [1] [2].

FAP-2286 acetate, a conjugate of a fibroblast activation protein (FAP)-binding peptide, exhibits antitumor activity [1]. It can be labeled with radionuclides for diagnostic purposes.

TAM470, a novel cytolysin, inhibits both tubulin polymerization and microtubule depolymerization. It serves as a precursor in the synthesis of OMTX705, a payload molecule. OMTX705 represents a new class of FAP-targeting antibody-drug conjugates (ADCs) exhibiting antitumor activity [1].

Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targeting Fibroblast Activating Protein (FAP) and is used in the study of colorectal cancer and non-small cell lung cancer.

Simlukafusp alfa (FAP-IL2v) is a tumor-targeting immune cytokine, a human IgG1 antibody, with antitumor activity and immunostimulatory properties that potentiate in vitro and in vivo activity of therapeutic antibodies mediating antibody-dependent or T-cell-independent cytotoxicity (TDCC) and programmed death ligand 1 (PD-L1) checkpoint inhibition.

TAM558 is a payload molecule utilized in the synthesis of OMTX705, which is a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470, exhibiting antitumor activity [1].

FAP-IN-2 TFA is a 99mTc-labeled, isonitrile-containing derivative inhibitor of fibroblast activation protein (FAP), used for tumor imaging [1].

FAP-IN-2 is a 99mTc-labeled, isonitrile-containing derivative of a fibroblast activation protein (FAPI) inhibitor suitable for tumor imaging [1].

FAPI-2 TFA, a fibroblast activation protein (FAP) inhibitor, is potentially applicable in cancer research [1].

ARI-3144, a substrate for fibroblast activation protein (FAP), serves as a FAP-activated proteasome inhibitor, making it valuable for solid tumor research [1].

SB03178 is an inhibitor of fibroblast activation protein-alpha (FAP) that can be conjugated with DOTA for use in cancer research [1].

BR102910 (4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-) is a selective inhibitor of fibroblast activated protein (FAP).

3BP-3940, a fibroblast activation protein (FAP)-targeting peptide, serves as a potent agent for theranostics. It is frequently conjugated with radionuclides to facilitate tumor diagnosis and therapy [1].