Lalistat-1
Apart from Lysosomal acid lipase human-LIPA, Lalistat-1 and -2 also inhibit major cytosolic lipid hydrolases responsible for lipid degradation in primary cells at neutral pH through off-target effects (ATGL not alpha/beta hydrolas; HSL hormone sensitive lipase); MGL Monoglyceride lipase). Lalistat also impairs Mycobacterium tuberculosis growth by targeting hydolases LipR Rv3084 Rv1984c Rv0183
General
Type : Piperidine,Lipase inhibitor,Sulfur Compound,Thiadiazol
Chemical_Nomenclature : (4-piperidin-1-yl-1,2,5-thiadiazol-3-yl) morpholine-4-carboxylate
Canonical SMILES : C1CCN(CC1)C2=NSN=C2OC(=O)N3CCOCC3
InChI : InChI=1S\/C12H18N4O3S\/c17-12(16-6-8-18-9-7-16)19-11-10(13-20-14-11)15-4-2-1-3-5-15\/h1-9H2
InChIKey : XAWUWPUYJUOUOF-UHFFFAOYSA-N
Other name(s) : 4-(piperidin-1-yl)-1,2,5-thiadiazol-3-yl morpholine-4-carboxylate,CHEMBL1085463,SCHEMBL17078235,ZINC795230
MW : 298.36
Formula : C12H18N4O3S
CAS_number : 501104-16-1
PubChem : 651937
UniChem : XAWUWPUYJUOUOF-UHFFFAOYSA-N
IUPHAR :
Wikipedia :
Target
Families : Lalistat-1 ligand of proteins in family: Acidic_Lipase || Hormone-sensitive_lipase_like || Monoglyceridelipase_lysophospholip || Cutinase || 6_AlphaBeta_hydrolase
Stucture :
Protein : human-LIPA || myctu-Rv3084 || myctu-rv0183 || myctu-cutas1 || myctu-RV0045C
References (4)
| Title : Off-target effects of the lysosomal acid lipase inhibitors Lalistat-1 and Lalistat-2 on neutral lipid hydrolases - Bradic_2022_Mol.Metab__101510 |
| Author(s) : Bradic I , Kuentzel KB , Honeder S , Grabner GF , Vujic N , Zimmermann R , Birner-Gruenberger R , Kratky D |
| Ref : Mol Metab , :101510 , 2022 |
| Abstract : Bradic_2022_Mol.Metab__101510 |
| ESTHER : Bradic_2022_Mol.Metab__101510 |
| PubMedSearch : Bradic_2022_Mol.Metab__101510 |
| PubMedID: 35504532 |
| Title : Loss of Function of Lysosomal Acid Lipase (LAL) Profoundly Impacts Osteoblastogenesis and Increases Fracture Risk in Humans - Helderman_2021_Bone__115946 |
| Author(s) : Helderman RC , Whitney DG , Duta-Mare M , Akhmetshina A , Vujic N , Jayapalan S , Nyman JS , Misra BB , Rosen CJ , Czech MP , Kratky D , Rendina-Ruedy E |
| Ref : Bone , :115946 , 2021 |
| Abstract : Helderman_2021_Bone__115946 |
| ESTHER : Helderman_2021_Bone__115946 |
| PubMedSearch : Helderman_2021_Bone__115946 |
| PubMedID: 33838322 |
| Gene_locus related to this paper: human-LIPA , mouse-1llip |
| Title : Human lysosomal acid lipase inhibitor lalistat impairs Mycobacterium tuberculosis growth by targeting bacterial hydrolases - Lehmann_2016_Medchemcomm_7_1797 |
| Author(s) : Lehmann J , Vomacka J , Esser K , Nodwell M , Kolbe K , Ramer P , Protzer U , Reiling N , Sieber SA |
| Ref : Medchemcomm , 7 :1797 , 2016 |
| Abstract : Lehmann_2016_Medchemcomm_7_1797 |
| ESTHER : Lehmann_2016_Medchemcomm_7_1797 |
| PubMedSearch : Lehmann_2016_Medchemcomm_7_1797 |
| PubMedID: |
| Gene_locus related to this paper: myctu-cutas1 , myctu-lipG , myctu-RV0045C , myctu-rv0183 , myctu-RV0293C , myctu-RV0840C , myctu-Rv1191 , myctu-RV1192 , myctu-Rv1399c , myctu-Rv1400c , myctu-Rv1426c , myctu-Rv2045c , myctu-Rv2284 , myctu-Rv2970c , myctu-Rv3084 , myctu-YR15 , larcr-a0a0f7ir14 |
| Title : Physiological difference in autophagic flux in macrophages from 2 mouse strains regulates cholesterol ester metabolism - Robinet_2013_Arterioscler.Thromb.Vasc.Biol_33_903 |
| Author(s) : Robinet P , Ritchey B , Smith JD |
| Ref : Arterioscler Thromb Vasc Biol , 33 :903 , 2013 |
| Abstract : Robinet_2013_Arterioscler.Thromb.Vasc.Biol_33_903 |
| ESTHER : Robinet_2013_Arterioscler.Thromb.Vasc.Biol_33_903 |
| PubMedSearch : Robinet_2013_Arterioscler.Thromb.Vasc.Biol_33_903 |
| PubMedID: 23493286 |