Evaluation of substituted pyrazole-based kinase inhibitors in one decade (2011–2020): Current status and future prospects

MI El-Gamal, SO Zaraei, MM Madkour, HS Anbar - Molecules, 2022 - mdpi.com
Pyrazole has been recognized as a pharmacologically important privileged scaffold whose
derivatives produce almost all types of pharmacological activities and have attracted much …

Inhibitors, protacs and molecular glues as diverse therapeutic modalities to target cyclin-dependent kinase

S Rana, JR Mallareddy, S Singh, L Boghean… - Cancers, 2021 - mdpi.com
Simple Summary Cyclin-dependent kinases (CDKs) are rich and viable therapeutic targets
for various cancers. The emergence of event-driven pharmacology as an alternative to …

Selective degradation of CDK6 by a palbociclib based PROTAC

S Rana, M Bendjennat, S Kour, HM King… - Bioorganic & medicinal …, 2019 - Elsevier
Abstract Development of selective kinase inhibitors that target the ATP binding site
continues to be a challenge largely due to similar binding pockets. Palbociclib is a cyclin …

Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax

HM King, S Rana, SP Kubica, JR Mallareddy… - Bioorganic & medicinal …, 2021 - Elsevier
Abstract Cyclin-dependent kinase 9 (CDK9) is a member of the cyclin-dependent kinase
(CDK) family which is involved in transcriptional regulation of several genes, including the …

A comprehensive insight on the recent development of cyclic dependent kinase inhibitors as anticancer agents

BN Marak, J Dowarah, L Khiangte, VP Singh - European Journal of …, 2020 - Elsevier
Cancer is one of the major leading causes of death worldwide despite many breakthroughs
in the development of novel anticancer drugs. The heterodimer CDK-Cyclin complex plays …

PROTACs in gastrointestinal cancers

Y Chen, Q Yang, J Xu, L Tang, Y Zhang, F Du… - Molecular Therapy …, 2022 - cell.com
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein
degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase …

Systemic administration of a brain permeable Cdk5 inhibitor alters neurobehavior

A Umfress, S Singh, KJ Ryan, A Chakraborti… - Frontiers in …, 2022 - frontiersin.org
Cyclin-dependent kinase 5 (Cdk5) is a crucial regulator of neuronal signal transduction.
Cdk5 activity is implicated in various neuropsychiatric and neurodegenerative conditions …

Advances in pyrazole based scaffold as cyclin-dependent kinase 2 inhibitors for the treatment of cancer

J Shaikh, K Patel, T Khan - Mini Reviews in Medicinal …, 2022 - ingentaconnect.com
The transformation of a normal cell into a tumor cell is one of the initial steps in cell cycle
deregulation. The cell cycle is regulated by cyclin-dependent kinases (CDKs) that belong to …

Identification of key transcription factors in endometrial cancer by systems bioinformatics analysis

Y Song, QT Chen, QQ He - Journal of cellular biochemistry, 2019 - Wiley Online Library
Endometrial cancer (EC) is one of the most common malignant diseases worldwide.
Although many studies have been performed on EC, a systems analysis between …

Antileishmanial aminopyrazoles: Studies into mechanisms and stability of experimental drug resistance

M Van den Kerkhof, D Mabille… - Antimicrobial Agents …, 2020 - Am Soc Microbiol
Current antileishmanial treatment is hampered by limitations, such as drug toxicity and the
risk of treatment failure, which may be related to parasitic drug resistance. Given the urgent …