Asian Pacific Journal of Health Sciences

Yazarlar: Sonu Kumar Gupta, Priyanka Singh, Villayat Ali, Malkhey Verma

Konular:-

DOI:10.21276/pjhs.2019.6.1.9

Anahtar Kelimeler:BCR,BL,Chronic Myeloid Leukemia,Maybridge Rule of 3 Fragment Library,PhiladelphiaChromosome,Tyrosine Kinase Inhibitor

Özet: Chronic Myeloid Leukemia (CML) is a well-known myeloproliferative disease characterized by the presence of the Philadelphia chromosome and its oncogenic product, BCR-ABL, a constitutively expressed tyrosine kinase that is present in the majority of the patients. The treatment of CML was transformed by the introduction of imatinib mesylate commercially known as Gleevec; a BCR-ABL tyrosine kinase inhibitor (TKI) which dramatically increased the survival rate and quality life of the patients. Despite having high efficacy majority of the patients have developed resistance to imatinib. To overcome this problem, new treatment options are required to treat CML patients. In this regard, the fragment-based drug discovery is a novel and generic methodology which uses the combination of targeted chemotherapeutic drugs with the suitable fragments from the screened library. These ligandefficient individual fragments examine the chemical space of the target transporter protein, covering a relatively large area due to their small sizes, may provide a way to future medicine to treat CML patients.

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