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Inhibitor Report for: Talabostat

inhibitors of the serine peptidases DPP8 and DPP9 (DPP8/9) induce pro-caspase-1-dependent pyroptosis in monocytes and macrophages. inhibition of DPP8 and/or DPP9 has been shown to cause severe toxicity in preclinical species


General
Type Peptide, Pyrrolidine, Boron compound
Chemical_Nomenclature [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid
Canonical SMILES B(C1CCCN1C(=O)C(C(C)C)N)(O)O
InChI InChI=1S/C9H19BN2O3/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15/h6-8,14-15H,3-5,11H2,1-2H3/t7-,8-/m0/s1
InChIKey FKCMADOPPWWGNZ-YUMQZZPRSA-N
Other name(s) Val-boro-pro ; Val-boroPro ; ValboroPro ; UNII-KZ1O2SH88Z ; Talabostat(PT100) ; VbP ; PT-100 ; DB06182
________________________________________________________________________________________________
MW|214.07
Formula|C9H19BN2O3
CAS_number|149682-77-9
PubChem|6918572
UniChem|FKCMADOPPWWGNZ-YUMQZZPRSA-N
IUPHAR|
Wikipedia|

Target
Families | Talabostat ligand of proteins in family: DPP4N_Peptidase_S9
Stucture | 2 structures: 6X6C, 6HP8
Protein | human-DPP8, human-DPP9, human-FAP

References:
Search PubMed for references concerning: Talabostat

11 more
    Title: Activation of the CARD8 Inflammasome Requires a Disordered Region
    Chui AJ, Griswold AR, Taabazuing CY, Orth EL, Gai K, Rao SD, Ball DP, Hsiao JC, Bachovchin DA
    Ref: Cell Rep, 33:108264, 2020 : PubMed

            

    Title: The NLRP1 and CARD8 inflammasomes
    Taabazuing CY, Griswold AR, Bachovchin DA
    Ref: Immunol Rev, 297:13, 2020 : PubMed

            

    Title: DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis
    Okondo MC, Johnson DC, Sridharan R, Go EB, Chui AJ, Wang MS, Poplawski SE, Wu W, Liu Y and Bachovchin DA <5 more author(s)>
    Ref: Nat Chemical Biology, 13:46, 2017 : PubMed