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Fig. 2 | Cell Communication and Signaling

Fig. 2

From: Motif mediated protein-protein interactions as drug targets

Fig. 2

Structural comparison between a drug within Lipinski’s rules (Lisinopril), a kinase inhibitor (Imatinib) and finally a protein-protein interaction inhibitor (ABT-263). Panel a (PDB: 1O86); Crystal structure of the drug Lisinopril in complex with angiotensin-converting enzyme. Lisinopril inhibits angiotensin-converting enzyme. This drug is used to treat hypertension and symptomatic congestive heart failure, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy. Angiotensin-converting enzyme is represented in cartoon representation colored in grey with the active site in red. The drug is shown in licorice representation. Panel b (PDB: 2HYY); Crystal structure of the Human Abl (Abelson murine leukemia viral oncogene homolog 1) kinase domain in complex with the inhibitory drug Imatinib (licorice representation). Imatinib, Gleevec (USA), or Glivec (Europe/Australia) is a kinase inhibitor used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumours (GISTs) among other malignancies. Abl kinase domain protein surface is colored in grey with the active site in red. Imatinib is represented in licorice representation. Panel c (PDB: 4LVT); High-resolution crystal structure of the drug ABT-263 (licorice representation) bound to Bcl-2 (grey surface with interface highlighted in red). ABT-263 or Navitoclax is an orally bioavailable small molecule inhibitor of Bcl-2 family proteins currently in clinical trials for the treatment of lymphomas and other types of cancer. Bcl-2 is shown as a grey surface, where the motif recognition interface is highlighted in red. ABT-263 is represented in licorice in the complex. A 2D representation of each drug is displayed in the lower section of the figure

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