PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 26418815-1 2015 Built upon the catalytic mechanism-based pan-SIRT1/2/3 inhibitory warhead L-2-amino-7-carboxamidoheptanoic acid (L-ACAH, a close structural analog of N(epsilon)-acetyl-lysine) that our laboratory discovered recently, in the current study, its carboxamide NH2-ethylated analog was found to be a ~2.4-6.6-fold stronger SIRT1/2/3 inhibitory warhead than L-ACAH. warhead 66-73 sirtuin 1 Homo sapiens 45-54 26418815-1 2015 Built upon the catalytic mechanism-based pan-SIRT1/2/3 inhibitory warhead L-2-amino-7-carboxamidoheptanoic acid (L-ACAH, a close structural analog of N(epsilon)-acetyl-lysine) that our laboratory discovered recently, in the current study, its carboxamide NH2-ethylated analog was found to be a ~2.4-6.6-fold stronger SIRT1/2/3 inhibitory warhead than L-ACAH. warhead 66-73 immunoglobulin kappa variable 3-15 Homo sapiens 74-77 16686537-6 2006 The resulting optimized P4-P3-P2 sequence was grafted onto a novel proteasome inhibitor warhead, 2-keto-1,3,4-oxadiazoles (KOD), to produce reversible, subnanomolar proteasome inhibitors that were 1000-fold selective versus cathepsin B (CatB), cathepsin S (CatS), and trypsin-like as well as PGPH-like proteasome activity. warhead 88-95 cathepsin B Homo sapiens 224-235 16686537-6 2006 The resulting optimized P4-P3-P2 sequence was grafted onto a novel proteasome inhibitor warhead, 2-keto-1,3,4-oxadiazoles (KOD), to produce reversible, subnanomolar proteasome inhibitors that were 1000-fold selective versus cathepsin B (CatB), cathepsin S (CatS), and trypsin-like as well as PGPH-like proteasome activity. warhead 88-95 cathepsin B Homo sapiens 237-241 16686537-6 2006 The resulting optimized P4-P3-P2 sequence was grafted onto a novel proteasome inhibitor warhead, 2-keto-1,3,4-oxadiazoles (KOD), to produce reversible, subnanomolar proteasome inhibitors that were 1000-fold selective versus cathepsin B (CatB), cathepsin S (CatS), and trypsin-like as well as PGPH-like proteasome activity. warhead 88-95 cathepsin S Homo sapiens 244-255 35395439-3 2022 Modification of warhead on pyrrolopyridone BET degraders significantly regulates BRD4 isoform (long and short) protein degradation, which induces differential cell cycle arrest and apoptosis on MV-4-11 cells. warhead 16-23 delta/notch like EGF repeat containing Homo sapiens 43-46 35395439-3 2022 Modification of warhead on pyrrolopyridone BET degraders significantly regulates BRD4 isoform (long and short) protein degradation, which induces differential cell cycle arrest and apoptosis on MV-4-11 cells. warhead 16-23 bromodomain containing 4 Homo sapiens 81-85