Juan R. Del Valle, PhD

Research in our laboratory is focused on the application of modern synthetic and medicinal chemistry techniques to challenges in cancer biology.  Approaches including peptide mimicry, natural product synthesis, and structure-based drug design are employed in pursuit of new anticancer drug candidates, with an emphasis on the discovery of inhibitors of protein-protein interactions implicated in oncogenesis.

• Kang CW, Sun Y, Del Valle JR. Substituted imidazo[1,2-a]pyridines as ?-strand peptidomimetics. Org Lett. 2012 Dec;14(24):6162-6165. Pubmedid: 23210770. Pmcid: PMC3528799.
• Ranatunga S, Tang CH, Hu CC, Del Valle JR. Total synthesis and structural revision of lucentamycin a. J Org Chem. 2012 Nov;77(21):9859-9864. Pubmedid: 23039096.
• Cha JW, Park JS, Sim T, Nam SJ, Kwon HC, Del Valle JR, Fenical W. Structure assignment of lucentamycin e and revision of the olefin geometries of the marine-derived lucentamycins. J Nat Prod. 2012 Sep;75(9):1648-1651. Pubmedid: 22953793.
• Kim YB, Balasis ME, Doi K, Berndt N, DuBoulay C, Hu CC, Guida W, Wang HG, Sebti SM, Del Valle JR. Synthesis and evaluation of substituted hexahydronaphthalenes as novel inhibitors of the Mcl-1/BimBH3 interaction. Bioorg Med Chem Lett. 2012 Sep;22(18):5961-5965. Pubmedid: 22901384. Pmcid: PMC3432503.
• Kriss CL, Pinilla-Ibarz JA, Mailloux AW, Powers JJ, Tang CH, Kang CW, Zanesi N, Epling-Burnette PK, Sotomayor EM, Croce CM, Del Valle JR, Hu CC. Overexpression of TCL1 activates the endoplasmic reticulum stress response: a novel mechanism of leukemic progression in mice. Blood. 2012 Aug;120(5):1027-1038. Pubmedid: 22692508.
• Ranatunga S, Del Valle JR. Synthesis of GSK3? mimetic inhibitors of Akt featuring a novel extended dipeptide surrogate. Bioorg Med Chem Lett. 2011 Dec;21(23):7166-7169. Pubmedid: 22001093.
• Ranatunga S, Kim JS, Pal U, Del Valle JR. An Ester Enolate-Claisen Rearrangement Route to Substituted 4-Alkylideneprolines. Studies toward a Definitive Structural Revision of Lucentamycin A. J Org Chem. 2011 Nov;76(21):8962-8976. Pubmedid: 21942643.
• Ranatunga S, Liyanage W, Del Valle JR. Synthesis and conformational analysis of bicyclic extended dipeptide surrogates. J Org Chem. 2010 Aug;75(15):5113-5125. Pubmedid: 20593836. Pmcid: PMC2914495.
• Pal U, Ranatunga S, Ariyarathna Y, Del Valle JR. Total synthesis of the putative structure of lucentamycin A. Org Lett. 2009 Nov;11(22):5298-5301. Pubmedid: 19863114.
• Hanessian S, Wang X, Ersmark K, Del Valle JR, Klegraf E. Total synthesis and structural revision of the presumed aeruginosins 205A and B. Org Lett. 2009 Sep;11(18):4232-4235. Pubmedid: 19691354.
• Ranatunga S, Del Valle JR. Synthesis of Boc-protected bicycloproline. Tetrahedron Lett. 2009 May;50(21):2464-2466. Pubmedid: 20090865.
• Liyanage W, Weerasinghe L, Strong RK, Del Valle JR. Synthesis of carbapyochelins via diastereoselective azidation of 5-(ethoxycarbonyl)methylproline derivatives. J Org Chem. 2008 Sep;73(18):7420-7423. Pubmedid: 18698823. Pmcid: PMC2802343.
• Ersmark K, Del Valle JR, Hanessian S. Chemistry and biology of the aeruginosin family of serine protease inhibitors. Angew Chem Int Ed Engl. 2008;47(7):1202-1223. Pubmedid: 18076006.
• Hanessian S, Ersmark K, Wang X, Del Valle JR, Blomberg N, Xue Y, Fjellström O. Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin. Bioorg Med Chem Lett. 2007 Jun;17(12):3480-3485. Pubmedid: 17428662.
• Hanessian S, Del Valle JR, Xue Y, Blomberg N. Total synthesis and structural confirmation of chlorodysinosin A. J Am Chem Soc. 2006 Aug;128(32):10491-10495. Pubmedid: 16895415.
• Zapf CW, Del Valle JR, Goodman M. Utilizing the intramolecular Fukuyama-Mitsunobu reaction for a flexible synthesis of novel heterocyclic scaffolds for peptidomimetic drug design. Bioorg Med Chem Lett. 2005 Sep;15(18):4033-4036. Pubmedid: 16002286.
• Hanessian S, Tremblay M, Marzi M, Del Valle JR. Synthetic studies in the intramolecular carbocyclization of N-acyloxyiminium ions. Stereoelectronic and steric implications of nucleophilic alkene, alkyne, and allene tethers. J Org Chem. 2005 Jun;70(13):5070-5085. Pubmedid: 15960507.
• Del Valle JR, Goodman M. An efficient RCM-based synthesis of orthogonally protected meso-DAP and FK565. J Org Chem. 2004 Dec;69(25):8946-8948. Pubmedid: 15575780.
• Del Valle JR, Goodman M. Asymmetric hydrogenations for the synthesis of Boc-protected 4-alkylprolinols and prolines. J Org Chem. 2003 May;68(10):3923-3931. Pubmedid: 12737573.
• Catalán J, Pérez P, del Valle JC, de Paz JL, Kasha M. The concerted mechanism of photo-induced biprotonic transfer in 7-azaindole dimers: structure, quantum-theoretical analysis, and simultaneity principles. Proc Natl Acad Sci U S A. 2002 Apr;99(9):5793-5798. Pubmedid: 11983883. Pmcid: PMC122855.