Experimental Approaches to Identify Selective Picomolar Inhibitors for Carbonic Anhydrase IX.
CA IX
Drug development
cancer
isothermal titration
calorimetry
organic chemistry
sulfonamide
thermal shift assay
Journal
Current medicinal chemistry
ISSN: 1875-533X
Titre abrégé: Curr Med Chem
Pays: United Arab Emirates
ID NLM: 9440157
Informations de publication
Date de publication:
2021
2021
Historique:
received:
14
04
2020
revised:
14
08
2020
accepted:
16
08
2020
pubmed:
4
11
2020
medline:
17
6
2021
entrez:
3
11
2020
Statut:
ppublish
Résumé
Carbonic anhydrases (CAs) regulate pH homeostasis via the reversible hydration of CO The current review presents the design, development, and identification of the selective nano- to picomolar CA IX inhibitors VD11-4-2, VR16-09, and VD12-09. Compounds were selected from our database, composed of over 400 benzensulfonamides, synthesized at our laboratory, and tested for their binding to 12 human CAs. Here we discuss the CA CO Novel CA IX inhibitors are promising derivatives for in vivo explorations. Furthermore, the simultaneous targeting of several proteins involved in proton flux upon tumor acidosis and the disruption of transport metabolons might improve cancer management.
Sections du résumé
BACKGROUND
BACKGROUND
Carbonic anhydrases (CAs) regulate pH homeostasis via the reversible hydration of CO
OBJECTIVE
OBJECTIVE
The current review presents the design, development, and identification of the selective nano- to picomolar CA IX inhibitors VD11-4-2, VR16-09, and VD12-09.
METHODS AND RESULTS
RESULTS
Compounds were selected from our database, composed of over 400 benzensulfonamides, synthesized at our laboratory, and tested for their binding to 12 human CAs. Here we discuss the CA CO
CONCLUSIONS
CONCLUSIONS
Novel CA IX inhibitors are promising derivatives for in vivo explorations. Furthermore, the simultaneous targeting of several proteins involved in proton flux upon tumor acidosis and the disruption of transport metabolons might improve cancer management.
Identifiants
pubmed: 33138744
pii: CMC-EPUB-111075
doi: 10.2174/0929867327666201102112841
doi:
Substances chimiques
Antigens, Neoplasm
0
Carbonic Anhydrase Inhibitors
0
Carbonic Anhydrase IX
EC 4.2.1.1
Carbonic Anhydrases
EC 4.2.1.1
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
3361-3384Informations de copyright
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