Tirozin Kinaz Enzim İnhibitörü Yeni Bileşikler ve Yapı-Aktivite İlişkilerinin Değerlendirilmesi


Gurkan-Alp A. S., Bozca F.

Fabad Journal of Pharmaceutical Sciences, cilt.44, sa.1, ss.65-78, 2019 (Scopus) identifier

  • Yayın Türü: Makale / Derleme
  • Cilt numarası: 44 Sayı: 1
  • Basım Tarihi: 2019
  • Dergi Adı: Fabad Journal of Pharmaceutical Sciences
  • Derginin Tarandığı İndeksler: Scopus
  • Sayfa Sayıları: ss.65-78
  • Anahtar Kelimeler: BCR-ABL gene, Cancer, Chronic myeloid leukemia, Imatinib, Philadelphia chromosome, Tyrosine kinase
  • Ankara Üniversitesi Adresli: Evet

Özet

© 2019 Society of Pharmaceutical Sciences of Ankara (FABAD). All rights reserved.Cancer is one of the most important health problems today and the number of cancer patients is rapidly increasing day by day. It has been proven in many studies that hereditary and environmental factors increase the risk of developing cancer. ABL gene, a part of the chromosome 9, and BCR gene, a part of the chromosome 22 combine to form the fusion oncogene BCR-ABL on chromosome 22 and the changed chromosome is called the Philadelphia chromosome. This genetic abnormality is a diagnostic feature of chronic myeloid leukemia. Chronic myeloid leukemia is a crucial example of the fact that specific molecular target therapy alters the natural course of malignant diseases, and has been helpful for the development of specific and targeted therapies for many malignant diseases where effective drug therapy is not available. The increase in the functions of protein kinases has revealed the role of these enzymes in cancer, and it has been thought that cancer could be treated when these functions are suppressed. As a result of the studies, the first tyrosine kinase inhibitor imatinib mesylate was developed and was approved by the FDA in 2001. Imantinib mesylate was developed as a targeted drug and has become the most promising compound in terms of clinical development. While developing other tyrosine kinase inhibitors, imatinib was used as a prototype and the chemical structure-activity relationships were studied.