Results: 5

1.
Figure 2

Figure 2. From: Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

Initial tripeptide binding model.

Marcos González-López, et al. Bioorg Med Chem Lett. 2011 July 15;21(14):4332-4336.
2.
Figure 4

Figure 4. From: Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

Apoptosis in TRAIL-resistant cells sensitized with compounds 9f, 9hor 9j.

Marcos González-López, et al. Bioorg Med Chem Lett. 2011 July 15;21(14):4332-4336.
3.
Figure 1

Figure 1. From: Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

Examples of monovalent tripeptide XIAP BIR3 inhibitors.

Marcos González-López, et al. Bioorg Med Chem Lett. 2011 July 15;21(14):4332-4336.
4.
Figure 3

Figure 3. From: Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

Model of compound 9t (magenta) bound to BIR2 (grey) with residues Lys 206 and Gln 197 depicted in yellow.

Marcos González-López, et al. Bioorg Med Chem Lett. 2011 July 15;21(14):4332-4336.
5.
Scheme 1

Scheme 1. From: Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

General synthetic route for the synthesis of small molecule XIAP inhibitors. Reagents and conditions: (a) EDC, HOBt, N-methylmorpholine, DMF (b) TFA, CH2Cl2 (c) H2, Pd/C, MeOH.

Marcos González-López, et al. Bioorg Med Chem Lett. 2011 July 15;21(14):4332-4336.

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