Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models.
Animals
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Barbiturates
/ chemical synthesis
Carbocyanines
/ chemistry
Cell Cycle Proteins
/ antagonists & inhibitors
Drug Design
Drug Screening Assays, Antitumor
Fluorescent Dyes
/ chemistry
G2 Phase Cell Cycle Checkpoints
/ drug effects
HeLa Cells
Humans
Male
Mice, Inbred BALB C
Mice, Inbred ICR
Molecular Structure
Neoplasms
/ diagnosis
Protein Binding
Protein Kinase Inhibitors
/ chemical synthesis
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins
/ antagonists & inhibitors
Structure-Activity Relationship
Xenograft Model Antitumor Assays
Polo-Like Kinase 1
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
10 12 2020
10 12 2020
Historique:
pubmed:
4
11
2020
medline:
4
2
2021
entrez:
3
11
2020
Statut:
ppublish
Résumé
Polo-like kinase-1 (Plk1) plays a key role in mitosis and has been identified as an attractive anticancer drug target. Plk1 consists of two drug-targeting sites, namely, N-terminal kinase domain (KD) and C-terminal polo-box domain (PBD). As KD-targeting inhibitors are associated with severe side effects, here we report on the pyrazole-based Plk1 PBD inhibitor, KBJK557, which showed a remarkable
Identifiants
pubmed: 33142063
doi: 10.1021/acs.jmedchem.0c01451
pmc: PMC8919061
mid: NIHMS1780917
doi:
Substances chimiques
Antineoplastic Agents
0
Barbiturates
0
Carbocyanines
0
Cell Cycle Proteins
0
Fluorescent Dyes
0
Protein Kinase Inhibitors
0
Proto-Oncogene Proteins
0
cyanine dye 5
0
Protein Serine-Threonine Kinases
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
14905-14920Subventions
Organisme : Intramural NIH HHS
ID : ZIA BC010681
Pays : United States
Références
J Med Chem. 2010 Apr 8;53(7):2719-40
pubmed: 20131845
Clin Cancer Res. 2010 Jan 15;16(2):384-9
pubmed: 20068088
Int J Nanomedicine. 2018 Jul 04;13:3921-3935
pubmed: 30013345
Mol Cancer Res. 2003 Mar;1(5):376-84
pubmed: 12651910
Proc Natl Acad Sci U S A. 1998 Aug 4;95(16):9301-6
pubmed: 9689075
Nat Rev Drug Discov. 2010 Aug;9(8):643-60
pubmed: 20671765
J Med Chem. 2015 Jan 8;58(1):294-304
pubmed: 25347203
Chem Biol. 2008 May;15(5):459-66
pubmed: 18482698
Cell Mol Life Sci. 2010 Jun;67(12):1957-70
pubmed: 20148280
Adv Drug Deliv Rev. 1999 Nov 10;40(1-2):103-127
pubmed: 10837783
Clin Cancer Res. 2009 May 1;15(9):3094-102
pubmed: 19383823
Cell. 2003 Oct 3;115(1):83-95
pubmed: 14532005
Am J Pathol. 2011 Oct;179(4):2091-9
pubmed: 21839059
Nat Biotechnol. 2011 Oct 30;29(11):1046-51
pubmed: 22037378
Pharmacol Rev. 2001 Jun;53(2):283-318
pubmed: 11356986
Cell. 2009 May 29;137(5):835-48
pubmed: 19490893
J Cell Mol Med. 2008 Jan-Feb;12(1):330-42
pubmed: 18366456
EMBO J. 2003 Nov 3;22(21):5757-68
pubmed: 14592974
Biopolymers. 2014 Nov;102(6):444-55
pubmed: 25283071
ChemMedChem. 2015 Jan;10(1):158-63
pubmed: 25196850
Oncogene. 2005 Apr 18;24(17):2844-59
pubmed: 15838519
Oncogene. 2005 Jan 10;24(2):248-59
pubmed: 15640840
J Biol Chem. 2009 Jan 23;284(4):2344-53
pubmed: 19033445
Oncogene. 2002 May 9;21(20):3162-71
pubmed: 12082631
J Chem Inf Model. 2015 Nov 23;55(11):2324-37
pubmed: 26479676
Nat Chem Biol. 2011 Jul 17;7(9):595-601
pubmed: 21765407
Curr Biol. 2007 Feb 20;17(4):304-15
pubmed: 17291761
J Pharm Sci. 2010 Mar;99(3):1107-22
pubmed: 19852037
Proc Natl Acad Sci U S A. 2005 Aug 16;102(33):11663-8
pubmed: 16085715
ACS Chem Biol. 2015 Nov 20;10(11):2570-9
pubmed: 26279064
Dev Cell. 2008 May;14(5):646-59
pubmed: 18477449
Curr Biol. 2007 Feb 20;17(4):316-22
pubmed: 17291758
Oncotarget. 2017 Jan 3;8(1):1234-1246
pubmed: 27902479
Nat Struct Mol Biol. 2009 Aug;16(8):876-82
pubmed: 19597481
Nat Rev Mol Cell Biol. 2009 Apr;10(4):265-75
pubmed: 19305416
Cell Rep. 2017 Jun 6;19(10):2060-2073
pubmed: 28591578
J Comput Chem. 2015 Jun 5;36(15):1132-56
pubmed: 25914306
Cancer Res. 2008 Jun 1;68(11):4077-85
pubmed: 18519666