PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33064187-9 2020 Strain with rAIP, GDH, DpkA, LysP, and DavB coexpression could produce delta-valerolactam. 2-piperidone 71-89 aryl-hydrocarbon receptor-interacting protein Rattus norvegicus 12-16 26046940-7 2015 25-fold affinity improvement of the piperidinone family of inhibitors for MDM2 constructs that include the full lid correlates with interactions between ligand hydrophobic groups and the C-terminal lid region that is already partially ordered in apo MDM2. 2-piperidone 36-48 MDM2 proto-oncogene Homo sapiens 74-78 28414905-6 2017 Upon coexpressing ORF26 with a metabolic pathway that produced 5-aminovaleric acid from lysine, we were able to demonstrate production of delta-valerolactam from lysine. 2-piperidone 138-156 hypothetical protein Escherichia coli 18-23 30253242-0 2018 The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. 2-piperidone 19-32 MDM2 proto-oncogene Homo sapiens 43-47 30253242-0 2018 The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. 2-piperidone 19-32 tumor protein p53 Homo sapiens 48-51 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 59-71 MDM2 proto-oncogene Homo sapiens 78-82 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 59-71 tumor protein p53 Homo sapiens 83-86 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 59-71 MDM2 proto-oncogene Homo sapiens 240-244 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 59-71 MDM2 proto-oncogene Homo sapiens 240-244 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 59-71 tumor protein p53 Homo sapiens 322-325 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 298-310 MDM2 proto-oncogene Homo sapiens 78-82 30253242-4 2018 This review is focused on the discovery and development of piperidinone-based MDM2-p53 inhibitors for cancer therapy, including the identification of hit compounds, hit-to-lead optimizations, binding models of ligands in the active site of MDM2, metabolic studies, and preclinical data of advanced piperidinone-based MDM2-p53 inhibitors. 2-piperidone 298-310 tumor protein p53 Homo sapiens 83-86 28669344-6 2018 Currently, nutlin, spirooxindole, isoquilinone and piperidinone analogues inhibiting p53-Mdm2 interaction are found to be promising in the treatment of cancer. 2-piperidone 51-63 transformation related protein 53, pseudogene Mus musculus 85-88 28669344-6 2018 Currently, nutlin, spirooxindole, isoquilinone and piperidinone analogues inhibiting p53-Mdm2 interaction are found to be promising in the treatment of cancer. 2-piperidone 51-63 transformed mouse 3T3 cell double minute 2 Mus musculus 89-93 27150473-0 2016 Design and Synthesis of a Piperidinone Scaffold as an Analgesic through Kappa-Opioid Receptor: Structure-Activity Relationship Study of Matrine Alkaloids. 2-piperidone 26-38 opioid receptor kappa 1 Homo sapiens 72-93 26046940-7 2015 25-fold affinity improvement of the piperidinone family of inhibitors for MDM2 constructs that include the full lid correlates with interactions between ligand hydrophobic groups and the C-terminal lid region that is already partially ordered in apo MDM2. 2-piperidone 36-48 MDM2 proto-oncogene Homo sapiens 250-254 25384157-1 2014 Structure-based rational design and extensive structure-activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of the MDM2-p53 association, which is currently being evaluated in human clinical trials for the treatment of cancer. 2-piperidone 132-144 MDM2 proto-oncogene Homo sapiens 162-166 25522111-3 2015 Herein, we describe the spontaneous rearrangement of 4-carboxy-2-oxoazepane alpha,alpha-amino acids to lead to 2"-oxopiperidine-containing beta(2,3,3) -amino acids, upon basic or acid hydrolysis of the 2-oxoazepane alpha,alpha-amino acid ester. 2-piperidone 111-127 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 139-149 25384157-1 2014 Structure-based rational design and extensive structure-activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of the MDM2-p53 association, which is currently being evaluated in human clinical trials for the treatment of cancer. 2-piperidone 132-144 tumor protein p53 Homo sapiens 167-170 24601644-1 2014 We previously reported the discovery of potent and selective morpholinone and piperidinone inhibitors of the MDM2-p53 interaction. 2-piperidone 78-90 MDM2 proto-oncogene Homo sapiens 109-113 25396040-5 2014 Soc., 2013, 135, 167 - 173) to a piperidinone-piperidine chemotype 1 indicated specific derivatives were candidates to perturb a protein-protein interface in the alpha-antithrombin dimer; those particular derivatives of 1 were prepared and tested. 2-piperidone 33-45 serpin family C member 1 Homo sapiens 168-180 25147610-0 2014 Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction. 2-piperidone 35-47 MDM2 proto-oncogene Rattus norvegicus 72-76 25147610-0 2014 Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction. 2-piperidone 35-47 Wistar clone pR53P1 p53 pseudogene Rattus norvegicus 77-80 24858256-0 2014 Group-based QSAR and molecular dynamics mechanistic analysis revealing the mode of action of novel piperidinone derived protein-protein inhibitors of p53-MDM2. 2-piperidone 99-111 transformation related protein 53, pseudogene Mus musculus 150-153 24858256-0 2014 Group-based QSAR and molecular dynamics mechanistic analysis revealing the mode of action of novel piperidinone derived protein-protein inhibitors of p53-MDM2. 2-piperidone 99-111 transformed mouse 3T3 cell double minute 2 Mus musculus 154-158 24858256-4 2014 In this study, a novel robust fragment-based QSAR model has been developed for piperidinone derived compounds experimentally known to inhibit p53-MDM2 interaction. 2-piperidone 79-91 transformation related protein 53, pseudogene Mus musculus 142-145 24858256-4 2014 In this study, a novel robust fragment-based QSAR model has been developed for piperidinone derived compounds experimentally known to inhibit p53-MDM2 interaction. 2-piperidone 79-91 transformed mouse 3T3 cell double minute 2 Mus musculus 146-150 25042256-0 2014 Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction. 2-piperidone 68-80 MDM2 proto-oncogene Homo sapiens 118-122 25042256-0 2014 Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction. 2-piperidone 68-80 tumor protein p53 Homo sapiens 123-126 25042256-1 2014 We recently reported on the discovery of AMG 232, a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 73-85 MDM2 proto-oncogene Homo sapiens 103-107 25042256-1 2014 We recently reported on the discovery of AMG 232, a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 73-85 tumor protein p53 Homo sapiens 108-111 24967612-1 2014 We recently reported the discovery of AMG 232 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 protein-protein interaction. 2-piperidone 74-86 MDM2 proto-oncogene Homo sapiens 104-108 24967612-1 2014 We recently reported the discovery of AMG 232 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 protein-protein interaction. 2-piperidone 74-86 tumor protein p53 Homo sapiens 109-112 24601644-1 2014 We previously reported the discovery of potent and selective morpholinone and piperidinone inhibitors of the MDM2-p53 interaction. 2-piperidone 78-90 tumor protein p53 Homo sapiens 114-117 24548297-1 2014 We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 79-91 MDM2 proto-oncogene Homo sapiens 109-113 24548297-1 2014 We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 79-91 tumor protein p53 Homo sapiens 114-117 17367123-0 2007 Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors. 2-piperidone 50-62 dipeptidyl peptidase 4 Homo sapiens 139-162 23811823-0 2013 Identification of 2-piperidone as a biomarker of CYP2E1 activity through metabolomic phenotyping. 2-piperidone 18-30 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 49-55 23811823-5 2013 Subsequently, 2-piperidone was identified as a urinary metabolite that inversely correlated to the CYP2E1 activity in the three mouse lines. 2-piperidone 14-26 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 99-105 23811823-6 2013 Backcrossing of WT and Cyp2e1-null mice, together with targeted analysis of 2-piperidone in mouse serum, confirmed the genotype dependency of 2-piperidone. 2-piperidone 142-154 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 23-29 23811823-7 2013 The accumulation of 2-piperidone in the Cyp2e1-null mice was mainly caused by the changes in the biosynthesis and degradation of 2-piperidone because compared with the WT mice, the conversion of cadaverine to 2-piperidone was higher, whereas the metabolism of 2-piperidone to 6-hydroxy-2-piperidone was lower in the Cyp2e1-null mice. 2-piperidone 20-32 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 40-46 23811823-7 2013 The accumulation of 2-piperidone in the Cyp2e1-null mice was mainly caused by the changes in the biosynthesis and degradation of 2-piperidone because compared with the WT mice, the conversion of cadaverine to 2-piperidone was higher, whereas the metabolism of 2-piperidone to 6-hydroxy-2-piperidone was lower in the Cyp2e1-null mice. 2-piperidone 20-32 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 316-322 23811823-7 2013 The accumulation of 2-piperidone in the Cyp2e1-null mice was mainly caused by the changes in the biosynthesis and degradation of 2-piperidone because compared with the WT mice, the conversion of cadaverine to 2-piperidone was higher, whereas the metabolism of 2-piperidone to 6-hydroxy-2-piperidone was lower in the Cyp2e1-null mice. 2-piperidone 129-141 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 40-46 23811823-7 2013 The accumulation of 2-piperidone in the Cyp2e1-null mice was mainly caused by the changes in the biosynthesis and degradation of 2-piperidone because compared with the WT mice, the conversion of cadaverine to 2-piperidone was higher, whereas the metabolism of 2-piperidone to 6-hydroxy-2-piperidone was lower in the Cyp2e1-null mice. 2-piperidone 129-141 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 40-46 23811823-7 2013 The accumulation of 2-piperidone in the Cyp2e1-null mice was mainly caused by the changes in the biosynthesis and degradation of 2-piperidone because compared with the WT mice, the conversion of cadaverine to 2-piperidone was higher, whereas the metabolism of 2-piperidone to 6-hydroxy-2-piperidone was lower in the Cyp2e1-null mice. 2-piperidone 129-141 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 40-46 23811823-8 2013 Overall, untargeted metabolomic analysis identified a correlation between 2-piperidone concentrations in urine and the expression and activity of CYP2E1, thus providing a noninvasive metabolite biomarker that can be potentially used in to monitor CYP2E1 activity. 2-piperidone 74-86 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 146-152 23811823-8 2013 Overall, untargeted metabolomic analysis identified a correlation between 2-piperidone concentrations in urine and the expression and activity of CYP2E1, thus providing a noninvasive metabolite biomarker that can be potentially used in to monitor CYP2E1 activity. 2-piperidone 74-86 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 247-253 22524527-2 2012 The affinity of these compounds for MDM2 was improved through conformational control of both the piperidinone ring and the appended N-alkyl substituent. 2-piperidone 97-109 MDM2 proto-oncogene Homo sapiens 36-40 24456472-1 2014 We recently reported the discovery of AM-8553 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 74-86 MDM2 proto-oncogene Homo sapiens 104-108 24456472-1 2014 We recently reported the discovery of AM-8553 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. 2-piperidone 74-86 tumor protein p53 Homo sapiens 109-112 22991965-2 2012 Here, we present kinetic, thermodynamic, and structural rationale for the remarkable potency of a new class of MDM2 inhibitors, the piperidinones. 2-piperidone 132-145 MDM2 proto-oncogene Homo sapiens 111-115 22991965-3 2012 While these compounds bind to the same site as previously reported for small molecule inhibitors, such as the Nutlins, data presented here demonstrate that the piperidinones also engage the N-terminal region (residues 10-16) of human MDM2, in particular, Val14 and Thr16. 2-piperidone 160-173 MDM2 proto-oncogene Homo sapiens 234-238 22991965-4 2012 This portion of MDM2 is unstructured in both the apo form of the protein and in MDM2 complexes with p53 or Nutlin, but adopts a novel beta-strand structure when complexed with the piperidinones. 2-piperidone 180-193 MDM2 proto-oncogene Homo sapiens 16-20 22991965-5 2012 The ordering of the N-terminus upon binding of the piperidinones extends the current model of MDM2-p53 interaction and provides a new route to rational design of superior inhibitors. 2-piperidone 51-64 MDM2 proto-oncogene Homo sapiens 94-98 22991965-5 2012 The ordering of the N-terminus upon binding of the piperidinones extends the current model of MDM2-p53 interaction and provides a new route to rational design of superior inhibitors. 2-piperidone 51-64 tumor protein p53 Homo sapiens 99-102 22530559-1 2012 Chiral 2-piperidinone compounds with various C-6 substituents were successfully synthesized via a Pd-catalyzed asymmetric 6-endo cyclization of dienamides, which were evidently activated by both N-p-toluenesulfonyl and C-3 ester substituents. 2-piperidone 7-21 complement C6 Homo sapiens 45-48 22530559-1 2012 Chiral 2-piperidinone compounds with various C-6 substituents were successfully synthesized via a Pd-catalyzed asymmetric 6-endo cyclization of dienamides, which were evidently activated by both N-p-toluenesulfonyl and C-3 ester substituents. 2-piperidone 7-21 complement C3 Homo sapiens 219-222 15104472-2 2004 The one-pot tandem oxidation-cyclization-oxidation of unsaturated alcohols 1a-e by PCC or PCC and trifluoromethanesulfonic acid affords piperidinones 2a-e in good yield. 2-piperidone 136-149 crystallin gamma D Homo sapiens 83-86 15863309-1 2005 Part 4: 2-Piperidones as selective EP4 receptor agonists. 2-piperidone 8-21 prostaglandin E receptor 4 Homo sapiens 35-38 15863309-4 2005 The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. 2-piperidone 4-17 prostaglandin E receptor 4 Homo sapiens 60-63 15104472-2 2004 The one-pot tandem oxidation-cyclization-oxidation of unsaturated alcohols 1a-e by PCC or PCC and trifluoromethanesulfonic acid affords piperidinones 2a-e in good yield. 2-piperidone 136-149 crystallin gamma D Homo sapiens 90-93 33548803-5 2021 This successfully led to the discovery of a piperidinone ring as a desirable motif at the indoline 5-position, which could minimize hERG liability as shown by 24b. 2-piperidone 44-56 ETS transcription factor ERG Homo sapiens 132-136 6436440-1 1984 1-Piperideine, 5-aminopentanoic acid, and its lactam, 2-piperidone, were identified as metabolites of cadaverine in 10,000 g mouse liver supernatants to which diamine oxidase had been added. 2-piperidone 54-66 amine oxidase, copper-containing 1 Mus musculus 159-174