Title : Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity - Atkinson_2023_Eur.J.Med.Chem_251_115132 |
Author(s) : Atkinson BN , Willis NJ , Zhao Y , Patel C , Frew S , Costelloe K , Magno L , Svensson F , Jones EY , Fish PV |
Ref : Eur Journal of Medicinal Chemistry , 251 :115132 , 2023 |
Abstract : |
PubMedSearch : Atkinson_2023_Eur.J.Med.Chem_251_115132 |
PubMedID: 36934521 |
Gene_locus related to this paper: human-NOTUM |
Title : Structural Analysis and Development of Notum Fragment Screening Hits - Zhao_2022_ACS.Chem.Neurosci_13_2060 |
Author(s) : Zhao Y , Mahy W , Willis NJ , Woodward HL , Steadman D , Bayle ED , Atkinson BN , Sipthorp J , Vecchia L , Ruza RR , Harlos K , Jeganathan F , Constantinou S , Costa A , Kjaer S , Bictash M , Salinas PC , Whiting P , Vincent JP , Fish PV , Jones EY |
Ref : ACS Chem Neurosci , 13 :2060 , 2022 |
Abstract : |
PubMedSearch : Zhao_2022_ACS.Chem.Neurosci_13_2060 |
PubMedID: 35731924 |
Gene_locus related to this paper: human-NOTUM |
Title : Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity - Steadman_2022_J.Med.Chem_65_562 |
Author(s) : Steadman D , Atkinson BN , Zhao Y , Willis NJ , Frew S , Monaghan A , Patel C , Armstrong E , Costelloe K , Magno L , Bictash M , Jones EY , Fish PV , Svensson F |
Ref : Journal of Medicinal Chemistry , 65 :562 , 2022 |
Abstract : |
PubMedSearch : Steadman_2022_J.Med.Chem_65_562 |
PubMedID: 34939789 |
Gene_locus related to this paper: human-NOTUM |
Title : Design of a potent, selective and brain penetrant inhibitor of Wnt-deactivating enzyme Notum by optimization of a crystallographic fragment hit - Willis_2022_J.Med.Chem_65_7212 |
Author(s) : Willis NJ , Mahy W , Sipthorp J , Zhao Y , Woodward HL , Atkinson BN , Bayle ED , Svensson F , Frew S , Jeganathan F , Monaghan A , Benvegnu S , Jolly S , Vecchia L , Ruza RR , Kjaer S , Howell SA , Snidjers AP , Bictash M , Salinas PC , Vincent JP , Jones EY , Whiting P , Fish PV |
Ref : Journal of Medicinal Chemistry , 65 :7212 , 2022 |
Abstract : |
PubMedSearch : Willis_2022_J.Med.Chem_65_7212 |
PubMedID: 35536179 |
Gene_locus related to this paper: human-NOTUM |
Title : Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling - Bayle_2021_J.Med.Chem__ |
Author(s) : Bayle ED , Svensson F , Atkinson BN , Steadman D , Willis NJ , Woodward HL , Whiting P , Vincent JP , Fish PV |
Ref : Journal of Medicinal Chemistry , : , 2021 |
Abstract : |
PubMedSearch : Bayle_2021_J.Med.Chem__ |
PubMedID: 33783220 |
Gene_locus related to this paper: human-NOTUM |
Title : Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity - Mahy_2020_J.Med.Chem_63_9464 |
Author(s) : Mahy W , Patel M , Steadman D , Woodward HL , Atkinson BN , Svensson F , Willis NJ , Flint A , Papatheodorou D , Zhao Y , Vecchia L , Ruza RR , Hillier J , Frew S , Monaghan A , Costa A , Bictash M , Walter MW , Jones EY , Fish PV |
Ref : Journal of Medicinal Chemistry , 63 :9464 , 2020 |
Abstract : |
PubMedSearch : Mahy_2020_J.Med.Chem_63_9464 |
PubMedID: 32787107 |
Gene_locus related to this paper: human-NOTUM |
Title : Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen - Atkinson_2019_Medchemcomm_10_1361 |
Author(s) : Atkinson BN , Steadman D , Zhao YG , Sipthorp J , Vecchia L , Ruza RR , Jeganathan F , Lines G , Frew S , Monaghan A , Kjaer S , Bictash M , Jones Y , Fish PV , Zhao Y , Jones EY |
Ref : Medchemcomm , 10 :1361 , 2019 |
Abstract : |
PubMedSearch : Atkinson_2019_Medchemcomm_10_1361 |
PubMedID: 31534655 |
Gene_locus related to this paper: human-NOTUM |
Title : An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent - Willis_2019_Beilstein.J.Org.Chem_15_2790 |
Author(s) : Willis NJ , Bayle ED , Papageorgiou G , Steadman D , Atkinson BN , Mahy W , Fish PV |
Ref : Beilstein J Org Chem , 15 :2790 , 2019 |
Abstract : |
PubMedSearch : Willis_2019_Beilstein.J.Org.Chem_15_2790 |
PubMedID: 31807213 |
Gene_locus related to this paper: human-NOTUM |
Title : Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors - Atkinson_2019_Bioorg.Med.Chem.Lett__126751 |
Author(s) : Atkinson BN , Steadman D , Mahy W , Zhao Y , Sipthorp J , Bayle ED , Svensson F , Papageorgiou G , Jeganathan F , Frew S , Monaghan A , Bictash M , Jones EY , Fish PV |
Ref : Bioorganic & Medicinal Chemistry Lett , :126751 , 2019 |
Abstract : |
PubMedSearch : Atkinson_2019_Bioorg.Med.Chem.Lett__126751 |
PubMedID: 31862412 |
Gene_locus related to this paper: human-NOTUM |