ldc067 and Neoplasms

ldc067 has been researched along with Neoplasms* in 2 studies

*Neoplasms: New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. [MeSH]

Reviews

1 review(s) available for ldc067 and Neoplasms

ArticleYear
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
    Journal of medicinal chemistry, 2022, 05-12, Volume: 65, Issue:9

    Inhibition of cyclin-dependent kinases (CDKs) has become an effective therapeutic strategy for treating various diseases, especially cancer. Over almost three decades, although great efforts have been made to discover CDK inhibitors, many of which have entered clinical trials, only four CDK inhibitors have been approved. In the process of CDK inhibitor development, many difficulties and misunderstandings have hampered their discovery and clinical applications, which mainly include inadequate understanding of the biological functions of CDKs, less attention paid to pan- and multi-CDK inhibitors, nonideal isoform selectivity of developed selective CDK inhibitors, overlooking the metabolic stability of early discovered CDK inhibitors, no effective resistance solutions, and a lack of available combination therapy and effective biomarkers for CDK therapies. After reviewing the mechanisms of CDKs and the research progress of CDK inhibitors, this perspective summarizes and discusses these difficulties or lessons, hoping to facilitate the successful discovery of more useful CDK inhibitors.

    Topics: Antineoplastic Agents; Cell Cycle; Cyclin-Dependent Kinase 4; Cyclin-Dependent Kinases; Drug Discovery; Humans; Neoplasms; Protein Kinase Inhibitors

2022

Other Studies

1 other study(ies) available for ldc067 and Neoplasms

ArticleYear
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
    Journal of medicinal chemistry, 2016, 10-13, Volume: 59, Issue:19

    Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly 2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has emerged as a druggable target for the development of cancer therapeutics. CDK9 plays a crucial role in transcription regulation; specifically, CDK9 mediated transcriptional regulation of short-lived antiapoptotic proteins is critical for the survival of transformed cells. Focused chemical libraries based on a plethora of scaffolds have resulted in mixed success with regard to the development of selective CDK9 inhibitors. Here we review the regulation of CDK9, its cellular functions, and common core structures used to target CDK9, along with their selectivity profile and efficacy in vitro and in vivo.

    Topics: Animals; Cyclin-Dependent Kinase 9; Drug Discovery; Flavonoids; Humans; Macrocyclic Compounds; Models, Molecular; Neoplasms; Protein Kinase Inhibitors; Purines; Pyrazoles; Pyrimidines; Triazines

2016