Targeting CDK2 in cancer: challenges and opportunities for therapy
Highlights•CDK2 has key roles in cell cycle, DNA replication and DNA damage.•Multiple
biomarkers can indicate increased CDK2 activity.•Some cancers have particular …
biomarkers can indicate increased CDK2 activity.•Some cancers have particular …
Cyclin-dependent kinase 2 inhibitors in cancer therapy: an update
Cyclin-dependent kinase 2 (CDK2) drives the progression of cells into the S-and M-phases
of the cell cycle. CDK2 activity is largely dispensable for normal development, but it is …
of the cell cycle. CDK2 activity is largely dispensable for normal development, but it is …
[HTML][HTML] Targeting cell-cycle machinery in cancer
Abnormal activity of the core cell-cycle machinery is seen in essentially all tumor types and
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …
Cyclin E in normal physiology and disease states
E-type cyclins, collectively called cyclin E, represent key components of the core cell cycle
machinery. In mammalian cells, two E-type cyclins, E1 and E2, activate cyclin-dependent …
machinery. In mammalian cells, two E-type cyclins, E1 and E2, activate cyclin-dependent …
Development of isatin-thiazolo [3, 2-a] benzimidazole hybrids as novel CDK2 inhibitors with potent in vitro apoptotic anti-proliferative activity: Synthesis, biological and …
In the current medical era, human health is experiencing numerous challenges, particularly
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …
the human malignancies. Therefore, the therapeutic arsenal for these malignancies is to be …
[HTML][HTML] Cyclin-dependent kinase inhibitors and their therapeutic potential in colorectal cancer treatment
OM Thoma, MF Neurath, MJ Waldner - Frontiers in pharmacology, 2021 - frontiersin.org
Cyclin-dependent kinases (CDKs) are key players in cell cycle regulation. So far, more than
ten CDKs have been described. Their direct interaction with cyclins allow progression …
ten CDKs have been described. Their direct interaction with cyclins allow progression …
Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies
The serine/threonine protein kinases CDK2 and GSK-3β are key oncotargets in breast
cancer cell lines, therefore, in the present study three series of oxindole-benzofuran hybrids …
cancer cell lines, therefore, in the present study three series of oxindole-benzofuran hybrids …
Selective targeting of cyclin E1-amplified high-grade serous ovarian cancer by cyclin-dependent kinase 2 and AKT inhibition
G Au-Yeung, F Lang, WJ Azar, C Mitchell… - Clinical Cancer …, 2017 - AACR
Abstract Purpose: Cyclin E1 (CCNE1) amplification is associated with primary treatment
resistance and poor outcome in high-grade serous ovarian cancer (HGSC). Here, we …
resistance and poor outcome in high-grade serous ovarian cancer (HGSC). Here, we …
[HTML][HTML] Spatial competition constrains resistance to targeted cancer therapy
Adaptive therapy (AT) aims to control tumour burden by maintaining therapy-sensitive cells
to exploit their competition with resistant cells. This relies on the assumption that resistant …
to exploit their competition with resistant cells. This relies on the assumption that resistant …
Cyclin-dependent kinase (CDK) inhibitors: structure–activity relationships and insights into the CDK-2 selectivity of 6-substituted 2-arylaminopurines
Purines and related heterocycles substituted at C-2 with 4′-sulfamoylanilino and at C-6
with a variety of groups have been synthesized with the aim of achieving selectivity of …
with a variety of groups have been synthesized with the aim of achieving selectivity of …