An overview of glutaminyl cyclase inhibitors for Alzheimer's disease
A diverse range of N-terminally truncated and modified forms of amyloid-β (Aβ) oligomers have been discovered in Alzheimer's disease brains, including the pyroglutamate-Aβ (AβpE3). AβpE3 species are shown to be more neurotoxic when compared with the full-length Aβ peptide. Findings visibly suggest that glutaminyl cyclase (QC) catalyzed the generation of cerebral AβpE3, and therapeutic effects are achieved by reducing its activity. In recent years, efforts to effectively develop QC inhibitors have been pursued worldwide. The inhibitory activity of current QC inhibitors is mainly triggered by zinc-binding groups that coordinate Zn2+ ion in the active site and other common features. Herein, we summarized the current state of discovery and evolution of QC inhibitors as a potential Alzheimer's disease-modifying strategy.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
|---|---|
| Enthalten in: |
Future medicinal chemistry - 11(2019), 24 vom: 21. Dez., Seite 3179-3194 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Coimbra, Judite Rm [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 10.07.2020 Date Revised 10.07.2020 published: Print Citation Status MEDLINE |
|---|
| doi: |
10.4155/fmc-2019-0163 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM30439968X |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM30439968X | ||
| 003 | DE-627 | ||
| 005 | 20231225114913.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/fmc-2019-0163 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1014.xml |
| 035 | |a (DE-627)NLM30439968X | ||
| 035 | |a (NLM)31838899 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Coimbra, Judite Rm |e verfasserin |4 aut | |
| 245 | 1 | 3 | |a An overview of glutaminyl cyclase inhibitors for Alzheimer's disease |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 10.07.2020 | ||
| 500 | |a Date Revised 10.07.2020 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a A diverse range of N-terminally truncated and modified forms of amyloid-β (Aβ) oligomers have been discovered in Alzheimer's disease brains, including the pyroglutamate-Aβ (AβpE3). AβpE3 species are shown to be more neurotoxic when compared with the full-length Aβ peptide. Findings visibly suggest that glutaminyl cyclase (QC) catalyzed the generation of cerebral AβpE3, and therapeutic effects are achieved by reducing its activity. In recent years, efforts to effectively develop QC inhibitors have been pursued worldwide. The inhibitory activity of current QC inhibitors is mainly triggered by zinc-binding groups that coordinate Zn2+ ion in the active site and other common features. Herein, we summarized the current state of discovery and evolution of QC inhibitors as a potential Alzheimer's disease-modifying strategy | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a Alzheimer's disease • drug discovery | |
| 650 | 4 | |a glutaminyl cyclase inhibitors | |
| 650 | 4 | |a pyroglutamate-amyloid-β (AβpE3) | |
| 650 | 4 | |a small molecules | |
| 650 | 7 | |a AbetapE3 peptide |2 NLM | |
| 650 | 7 | |a Amyloid beta-Peptides |2 NLM | |
| 650 | 7 | |a Enzyme Inhibitors |2 NLM | |
| 650 | 7 | |a Peptide Fragments |2 NLM | |
| 650 | 7 | |a Aminoacyltransferases |2 NLM | |
| 650 | 7 | |a EC 2.3.2.- |2 NLM | |
| 650 | 7 | |a glutaminyl-peptide cyclotransferase |2 NLM | |
| 650 | 7 | |a EC 2.3.2.5 |2 NLM | |
| 700 | 1 | |a Sobral, Pedro Jm |e verfasserin |4 aut | |
| 700 | 1 | |a Santos, Armanda E |e verfasserin |4 aut | |
| 700 | 1 | |a Moreira, Paula I |e verfasserin |4 aut | |
| 700 | 1 | |a Salvador, Jorge Ar |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Future medicinal chemistry |d 2009 |g 11(2019), 24 vom: 21. Dez., Seite 3179-3194 |w (DE-627)NLM194822109 |x 1756-8927 |7 nnns |
| 773 | 1 | 8 | |g volume:11 |g year:2019 |g number:24 |g day:21 |g month:12 |g pages:3179-3194 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/fmc-2019-0163 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 11 |j 2019 |e 24 |b 21 |c 12 |h 3179-3194 | ||