Dual-Target Kinase Drug Design: Current Strategies
Rabia Mehboob
ABSTRACT
Protein kinases are well-known to
arrange the activation signaling in
response to extracellular and intracellular
stimuli to control cell proliferation and
survival.
Due to mutation or abnormal protein
expressions cause cancer.
A series of small-molecule drugs have
been approved for the current cancer
therapy. However their complicated
mechanisms may lead to resistance,
therefore replaced by dual target drug.
Drug design:
1. Fused pharmacophore approach
2. Merged pharmacophore approach.
3. Docking-based drug design.
Acknowledgement: I would like to thank Dr. Mehr-un-Nisa for her expert advice, encouragement and extraordinary support throughout this difficult process.
Quratul Ain Habib
Gull e Zara
University of Lahore, 1-Km Defence Road, Lahore.
DRUG DESIGN &
INTRODUCTION CONCLUSION
EXPERIMENTS
1. About 50 kinase inhibitors have been Medicinal chemistry design strategies 1. Hitherto, more than 500 protein
approved by the US (FDA). Amoung of dual-target kinase drugs in cancer: kinases have been reported encoded by
them 45 kinase inhibitors are directed the human genome, and most of them
toward the current cancer treatment. 1. Repurposing of dual-target kinase are able to regarded as potential
drugs. drugable targets in cancer therapeutics.
2. Recently, treatment with single target 2. Pharmacophore-based combination of
drug has been widely reported to result single-target kinase drugs. 2. Accordingly, nearly 400 types of
in resistance to chemotherapy e.g on 3. Linked pharmacophore approach. known kinase inhibitors have also been
target and off target. 4. Skeleton modification of dual-target designed, which may be a relatively
kinase drugs. important branch of medicinal
֍ Combination Therapy: chemistry.
Erlotinib and Gefitinib inhibitors use to
target on (RTK) due to EGFR (Lung
Cancer)
֍ Dual Pathways:
Dasatinib (9 Targets) and Alectinib (2
Targets) and these are very cost
effective with desired effects.
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design