Key resources table.
| Reagent type (species) or resource |
Designation | Source or reference | Identifiers | Additional information |
|---|---|---|---|---|
| Cell line (Homo sapiens) | HEK293F | ThermoFisher | ThermoFisher: R79007 | |
| Cell line (H. sapiens) | HEK293F ∆N∆C-LCAT | this paper | polyclonal stable cell line | |
| Recombinant DNA reagent | pcDNA4 LCAT | (Glukhova et al., 2015) DOI:10.1038/ncomms7250 | ||
| Recombinant DNA reagent | pcDNA4 ∆N∆C-LCAT | (Glukhova et al., 2015) DOI:10.1038/ncomms7250 | ||
| Recombinant DNA reagent | pProEX HT-EndoH | other | D. J. Leahy, Johns Hopkins | |
| Peptide, recombinant protein | ESP24218 peptide | Genscript | PVLDLFRELLNELLEALKQKLK | |
| Commercial assay or kit | Index HT screen | Hampton Research | Hampton: HR2-134 | |
| Commercial assay or kit | Monolith His-Tag Labeling Kit RED-tris-NTA 2nd Generation | Nanotemper Technologies | Nanotemper: MO-L018 | |
| Chemical compound, drug | 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) |
Avanti Polar Lipids | Avanti: 850355 | |
| Chemical compound, drug | 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) | NOF America | NOF America: MC-6081 | |
| Chemical compound, drug |
16:0 Biotinyl Cap PE | Avanti Polar Lipids | Avanti: 870277 | |
| Chemical compound, drug | 4-Methylumbelliferyl phosphate | Cayman Chemical | Cayman: 16089 | |
| Chemical compound, drug | Bio-beads SM-2 | Bio-Rad | Bio-Rad: 1523920 | |
| Chemical compound, drug |
Bovine Serum Albumin (BSA), fatty acid free |
Sigma-Aldrich | Sigma: A8806 | |
| Chemical compound, drug | Cholesterol oxidase | Sigma-Aldrich | Sigma: C8649 | |
| Chemical compound, drug | Dehydroergosterol (DHE) | Sigma-Aldrich | Sigma: E2634 | |
| Chemical compound, drug |
DMEM high glucose with GlutaMAX and 1 mM pyruvate | ThermoFisher Scientific | ThermoFisher:10569 | |
| Chemical compound, drug |
Fetal bovine serum | Sigma-Aldrich | Sigma: F2442 | |
| Chemical compound, drug |
FreeStyle 293 Expression Medium | ThermoFisher Scientific | ThermoFisher: 12338026 | |
| Chemical compound, drug |
Isopropyl dodecyl fluorophosphonate |
Cayman Chemical | Cayman: 10215 | |
| Chemical compound, drug |
Kifunensine | Cayman Chemical |
Cayman: 10009437 |
|
| Chemical compound, drug |
Ni-NTA | Qiagen | Qiagen: 30230 | |
| Chemical compound, drug |
OptiMEM Reduced Serum Medium | ThermoFisher Scientific |
ThermoFisher:31985070 | |
| Chemical compound, drug |
Penicillin- Streptomycin |
ThermoFisher Scientific |
ThermoFisher: 15140122 | |
| Chemical compound, drug |
Polyethylenimine (PEI) |
Polysciences | Polysciences: 23966 | |
| Chemical compound, drug |
p-nitrophenyl butyrate (pNPB) | Sigma-Aldrich | Sigma: N9876 | |
| Chemical compound, drug |
SspI | New England Biolabs | New England Biolabs: R0132S |
|
| Chemical compound, drug |
SYPRO Orange | ThermoFisher Scientific | ThermoFisher: S6650 | |
| Chemical compound, drug |
6-(4-(4-Hydroxy-6-oxo-4- (trifluoromethyl)−4,5,6,7- tetrahydro-1H-pyrazolo[3,4- b]pyridin-3-yl)piperidin-1-yl) −4- (trifluoromethyl)nicotinonitrile, TFA (compound 1) |
example 95 in US patent 9150575 |
||
| Chemical compound, drug | 4-Hydroxy-4-(trifluoromethyl)−3- (1-(5-(trifluoromethyl)pyrazin-2- yl)piperidin-4-yl)−4,5-dihydro-1H- pyrazolo[3,4-b]pyridin-6(7H)-one (compound 2) |
example 46 in US patent 9150575 | ||
| Chemical compound, drug |
7-Hydroxy-7-(trifluoromethyl)−1- (1-(5-(trifluoromethyl)pyrazin-2- yl)piperidin-4-yl)−6,7-dihydro-1H- imidazo[4,5-b]pyridin-5(4H)-one (compound 3) |
example 3 in WO patent 2015087996A1 | ||
| Chemical compound, drug |
4-(trifluoromethyl)−3-(1-(5- (trifluoromethyl)pyrazin-2- yl)piperidin-4-yl)−1,4,5,7- tetrahydro-6H-pyrazolo[3,4- b]pyridin-6-one (compound 4) |
example 10 in WO patent 2015111545A1 | ||
| Chemical compound, drug |
4-Hydroxy-3-(piperidin-4-yl)−4- (trifluoromethyl)−4,5-dihydro-1H- pyrazolo[3,4-b]pyridin-6(7H)-one, HCl (compound 5) |
reference example 60 in US patent 9150575 | ||
| Chemical compound, drug | 7-Hydroxy-1-(piperidin-4-yl)−7- (trifluoromethyl)−6,7-dihydro-1H- imidazo[4,5-b]pyridin-5(4H)-one, HCl (compound 6) |
reference example 1 in WO patent 2015087996A1 | ||
| Chemical compound, drug |
4-Hydroxy-3-(piperidin-4-yl)−4- (trifluoromethyl)−4,5- dihydroisoxazolo[5,4-b]pyridin- 6(7H)-one, HCl (compound 7) |
this paper | Compound was synthesized by NCATS |
|
| Chemical compound, drug |
7-(trifluoromethyl)−1-(1-(5- (trifluoromethyl)pyrazin-2- yl)piperidin-4-yl)−1H-imidazo[4,5- b]pyridin-5(4H)-one (compound 8) |
this paper | Compound was synthesized by NCATS |
|
| Chemical compound, drug | 4-hydroxy-4-(trifluoromethyl)−3- (1-(5-(trifluoromethyl)pyrazin-2- yl)piperidin-4-yl)−4,5- dihydroisoxazolo[5,4-b]pyridin- 6(7H)-one (compound 9) |
this paper | Compound was synthesized by NCATS | |
| Software, algorithm | HKL-2000 | (Otwinowski and Minor, 1997) DOI:10.1016/S0076-6879(97)76066-X |
||
| Software, algorithm |
PHASER | (McCoy, 2007) DOI:10.1107/ S0907444906045975 |
||
| Software, algorithm |
REFMAC5 | (Murshudov et al., 2011) DOI:10.1107/ S0907444911001314 |
||
| Software, algorithm |
Phenix | (Adams et al., 2010) DOI:10.1107/ S0907444909052925 |
||
| Software, algorithm |
Coot | (Emsley et al., 2010) DOI:10.1107/S090 7444910007493 |
||
| Software, algorithm |
Molprobity | (Chen et al., 2010) DOI:10.1107/S0907 444909042073 |
||
| Software, algorithm |
Prism 7.0 c | Graphpad Software | ||
| Software, algorithm |
Octet Data Analysis 7.0 |
FortéBio | ||
| Software, algorithm | PyMOL Molecular Graphics System |
Schrödinger | ||
| Software, algorithm | Chimera | (Pettersen et al., 2004) DOI:10.1002/jcc.20084 |
||
| Software, algorithm |
Protein Thermal Shift |
ThermoFisher Scientific |
||
| Software, algorithm | MO.Affinity Analysis |
Nanotemper Technologies |
||