Multiple myeloma: Combination therapy of BET proteolysis targeting chimeric molecule with CDK9 inhibitor

0 views | May 07 2021

Su-Lin Lim et al. found that the combination of a BET PROTAC (ARV 825) plus AZD 4573 (CDK9 inhibitor) was effective against MM cells. [Read the Full Post]

CDK9 inhibition improves diabetic nephropathy by reducing inflammation in the kidneys

2 views | Apr 26 2021

Xiaojing Yang et al. suggested that CDK9 might serve as a potential therapeutic target for DN. [Read the Full Post]

The molecular context of vulnerability for CDK9 suppression in triple wild-type melanoma

4 views | Apr 19 2021

Samantha M Guhan et al. found that transcriptional blockade through selective targeting of CDK9 was an effective method of suppressing therapeutically-orphaned BRAF/NRAS/NF1 wild-type melanomas. [Read the Full Post]

A high-throughput screen identifies that CDK7 activates glucose consumption in lung cancer cells

5 views | Mar 28 2021

Chiara Ghezzi et al. thought that CDK7 was a key regulator of glucose consumption in cells with an activated PI3K pathway. [Read the Full Post]

The role of drug efflux and uptake transporters ABCB1 (P-gp), ABCG2 (BCRP) and OATP1A/1B and of CYP3A4 in the pharmacokinetics of the CDK inhibitor milciclib

6 views | Mar 26 2021

Alejandra Martínez-Chávez found that the low impact of OATP1 and CYP3A could be clinically favorable for milciclib, reducing the risks of unintended drug-drug interactions or interindividual variation in CYP3A4 activity. [Read the Full Post]

Identification of hub genes and small molecule therapeutic drugs related to breast cancer with comprehensive bioinformatics analysis

16 views | Jan 28 2021

Mingqian Hao et al. identified six hub genes and 29 potential drug candidates for breast cancer. [Read the Full Post]

CKAP2L promotes non-small cell lung cancer progression through regulation of transcription elongation

16 views | Jan 28 2021

Tiziana Monteverde et al. found that the molecular mechanisms through which CKAP2L, a protein involved in CIN, promoted cancer progression and suggested that its inhibition represented a novel therapeutic strategy in NSCLC. [Read the Full Post]

Kinase activity-independent role of EphA2 in the regulation of M-phase progression

20 views | Jan 04 2021

Yuichiro Kaibori et al. suggested that EphA2 regulated M-phase progression in a manner independent of its kinase activity. [Read the Full Post]

Ginsenoside Rg1 reduces β‑amyloid levels by inhibiting CDΚ5‑induced PPARγ phosphorylation in a neuron model of Alzheimer's disease

25 views | Nov 12 2020

Qiankun Quan et al. suggested that ginsenoside Rg1 had neuroprotective properties and had potential for use in the treatment of AD. [Read the Full Post]

Identification of Quinazolinone Analogs Targeting CDK5 Kinase Activity and Glioblastoma Cell Proliferation

28 views | Nov 12 2020

Marion Peyressatre et al. found that the quinazolinone derivatives were the first small molecules reported to target CDK5 at a site other than the ATP pocket, thereby constituting attractive leads for glioblastoma therapeutics and providing therapeutic perspectives for neurodegenerative diseases. [Read the Full Post]