2. Academic Validation
  3. Targeting cyclin-dependent kinase 2 (CDK2) interactions with cyclins and Speedy 1 (Spy1) for cancer and male contraception

Targeting cyclin-dependent kinase 2 (CDK2) interactions with cyclins and Speedy 1 (Spy1) for cancer and male contraception

  • Future Med Chem. 2025 Mar;17(5):607-627. doi: 10.1080/17568919.2025.2463868.
Jeanine Giarolla 1 2,  Kelsey A Holdaway 1,  Maryam Nazari 1,  Laila Aiad 3,  Bidisha Sarkar 3,  Gunda I Georg 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.
  • 2 Departamento de Farmacia, School of Pharmaceutical Sciences, University of São Paulo-USP, São Paulo, SP, Brazil.
  • 3 Department of Chemistry, University of Minnesota, Minneapolis, MN, USA.
  • 4 Medicinal Chemistry, University of Minnesota Twin Cities, Minneapolis, MN, USA.
PMID: 40034037 DOI: 10.1080/17568919.2025.2463868
Abstract

The review discusses progress in discovering cyclin-dependent kinase 2 (CDK2) inhibitors for Cancer treatment and their potential for male contraception. It summarizes first-, second-, and third-generation CDK inhibitors and selective CDK2 inhibitors currently in clinical trials for Cancer. Novel strategies to discover allosteric inhibitors, covalent inhibitors, and degraders are also discussed.

Keywords

CDK2 inhibitors; Oncological therapeutics; Spy1; clinical trials; covalent binders; degraders; male contraception; orthosteric and allosteric.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-155218
    99.38%, CDK2/CDK5 PROTAC Degrader