Rongshi Li, PhD

The Li laboratory has focused on the design and synthesis of biologically active compounds including protein kinase inhibitors, inhibitors for protein-protein interactions and potential therapeutic agents combating both cancers and bacterial resistance such as methicillin-resistant Staphylococcus aureus (MRSA). Several exciting research projects from our lab using fragment-based and structure-guided approach, natural product chemistry and high-throughput medicinal chemistry have been established.

• Patel RA, Liu Y, Wang B, Li R, Sebti SM. Identification of novel ROCK inhibitors with anti-migratory and anti-invasive activities. Oncogene. 2013 Feb. Pubmedid: 23396364.
• Ziarek JJ, Liu Y, Smith E, Zhang G, Peterson FC, Chen J, Yu Y, Chen Y, Volkman BF, Li R. Fragment-Based Optimization of Small Molecule CXCL12 Inhibitors for Antagonizing the CXCL12/CXCR4 Interaction. Curr Top Med Chem. 2012 Dec;12(24):2727-2740. Pubmedid: 23368099.
• Liu Y, Haste NM, Thienphrapa W, Nizet V, Hensler M, Li R. Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (I). Mar Drugs. 2012 Apr;10(4):953-962. Pubmedid: 22690153. Pmcid: PMC3366685.
• Doi K, Li R, Sung SS, Wu H, Liu Y, Manieri W, Krishnegowda G, Awwad A, Dewey A, Liu X, Amin S, Cheng C, Qin Y, Schonbrunn E, Daughdrill G, Loughran TP, Sebti S, Wang HG. Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation. J Biol Chem. 2012 Mar;287(13):10224-10235. Pubmedid: 22311987. Pmcid: PMC3323047.
• Li R, Martin MP, Liu Y, Wang B, Patel RA, Zhu JY, Sun N, Pireddu R, Lawrence NJ, Li J, Haura EB, Sung SS, Guida WC, Schonbrunn E, Sebti SM. Fragment-based and structure-guided discovery and optimization of rho kinase inhibitors. J Med Chem. 2012 Mar;55(5):2474-2478. Pubmedid: 22272748.
• Mo SL, Liu WF, Li CG, Luo HB, Li R, Zhou SF. Pharmacophore, QSAR, and Binding Mode Studies of Substrates ofHuman Cytochrome P450 2D6 (CYP2D6)using Molecular Docking and Virtual Mutations and an Application to Chinese Herbal Medicine Screening. Curr Pharm Biotechnol. 2011 Oct. Pubmedid: 22039821.
• He SM, Li R, Kanwar JR, Zhou SF. Structural and functional properties of human multidrug resistance protein 1 (MRP1/ABCC1). Curr Med Chem. 2011;18(3):439-481. Pubmedid: 21143116.
• Cheng C, Pan L, Chen Y, Song H, Qin Y, Li R. Total synthesis of (+/-)-marinopyrrole A and its library as potential antibiotic and anticancer agents. J Comb Chem. 2010 Jul;12(4):541-547. Pubmedid: 20429575.
• Li R, Pourpak A, Morris SW. Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. J Med Chem. 2009 Aug;52(16):4981-5004. Pubmedid: 19610618. Pmcid: PMC2888655.
• Li R, Morris SW. Development of anaplastic lymphoma kinase (ALK) small-molecule inhibitors for cancer therapy. Med Res Rev. 2008 May;28(3):372-412. Pubmedid: 17694547.
• Zhou H, Wu S, Zhai S, Liu A, Sun Y, Li R, Zhang Y, Ekins S, Swaan PW, Fang B, Zhang B, Yan B. Design, synthesis, cytoselective toxicity, structure-activity relationships, and pharmacophore of thiazolidinone derivatives targeting drug-resistant lung cancer cells. J Med Chem. 2008 Mar;51(5):1242-1251. Pubmedid: 18257542.
• Lu RJ, Tucker JA, Zinevitch T, Kirichenko O, Konoplev V, Kuznetsova S, Sviridov S, Pickens J, Tandel S, Brahmachary E, Yang Y, Wang J, Freel S, Fisher S, Sullivan A, Zhou J, Stanfield-Oakley S, Greenberg M, Bolognesi D, Bray B, Koszalka B, Jeffs P, Khasanov A, Ma YA, Jeffries C, Liu C, Proskurina T, Zhu T, Chucholowski A, Li R, Sexton C. Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group. J Med Chem. 2007 Dec;50(26):6535-6544. Pubmedid: 18052117.
• Webb T, Jiang L, Sviridov S, Venegas R, Vlaskina A, McGrath D, Tucker J, Wang J, Deschenes A, Li R. Application of a novel design paradigm to generate general nonpeptide combinatorial templates mimicking beta-turns: synthesis of ligands for melanocortin receptors. J Comb Chem. 2007 Jul;9(4):704-710. Pubmedid: 17429950.
• Li R, Xue L, Zhu T, Jiang Q, Cui X, Yan Z, McGee D, Wang J, Gantla VR, Pickens JC, McGrath D, Chucholowski A, Morris SW, Webb TR. Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase. J Med Chem. 2006 Feb;49(3):1006-1015. Pubmedid: 16451066.
• Zhu T, Yan Z, Chucholowski A, Webb TR, Li R. Polymer-supported synthesis of pyridone-focused libraries as inhibitors of anaplastic lymphoma kinase. J Comb Chem. 2006;8(3):401-409. Pubmedid: 16677010.
• Zhu T, Yan Z, Chucholowski A, Li R. Polymer-supported synthesis of bicyclic gamma-lactams. J Comb Chem. 2005 Jul;7(4):520-522. Pubmedid: 16004492.
• Xiao X, Li R, Hurst D, Zhuang H, Shi S, Czarnik A, Robichaud A, Wacker D, Robertson D. Solid-phase synthesis of alkyl aryl ethers via the Ullmann condensation. J Comb Chem. 2002 Sep;4(5):536-539. Pubmedid: 12217028.
• Irving M, Cournoyer J, Li R, Santos C, Yan B. Qualitative and quantitative analyses of resin-bound organic compounds. Comb Chem High Throughput Screen. 2001 Jun;4(4):353-362. Pubmedid: 11472224.
• Li R, Xiao XY, Czarnik A. Merrifield MicroTube Reactors for Solid Phase Synthesis. Tetrahedron Lett. 1998;39:8581-8584.
• Li R, Chen X, Gong B, Selzer P, Li Z, Davidson E, Kurzban G, Miller R, Nuzum E, McKerrow J, Fletterick R, Gillmor S, Craik C, Kuntz I, Cohen F, Kenyon G. Structure-based design of parasitic protease inhibitors. Bioorg Med Chem. 1996 Sep;4(9):1421-1427. Pubmedid: 8894100 .
• Li R, Muscate A, Kenyon GL. Synthesis, Characterization, and Inhibitory Activities of Nucleoside a,b-Imido Triphosphate Analogues on Human Immunodeficiency Virus-1 Reverse Transcriptase. Bioorg Chem. 1996;24:251-261.
• Li R, Kenyon G, Cohen F, Chen X, Gong B, Dominguez J, Davidson E, KurzbanG, Miller R, Nuzum E, et a. In vitro antimalarial activity of chalcones and their derivatives. J Med Chem. 1995 Dec;38(26):5031-5037. Pubmedid: 8544179 .
• Li R, Kenyon G. A spectrophotometric determination of alpha-dicarbonyl compounds and itsapplication to the enzymatic formation of alpha-ketobutyrate. Anal Biochem. 1995 Sep;230(1):37-40. Pubmedid: 8585627 .
• Li R, Farmer P, Wang J, Boyd R, Cameron T, Quilliam M, Walter J, HowlettSE. Molecular geometries of dibenzothiazepinone and dibenzoxazepinone calcium antagonists. Drug Des Discov. 1995 Apr;12(4):337-358. Pubmedid: 9040993 .
• Li R, Powers VM, Kozarich JW, Kenyon GL. Racemization of Vinylglycolate Catalyzed by Mandelate Racemase. J Org Chem. 1995;60:3347-3351.
• Li R, Farmer P, Quillam M, Howlett S. Dibenzothiazepinones as potential calcium channel antagonists. I. Drug Des Discov. 1993 10;10(4):331-342. Pubmedid: 8148472 .
• Li R, Farmer P, Xie M, Quilliam M, Pleasance S, Howlett S, Yeung P. Synthesis, characterization, and Ca2+ antagonistic activity of diltiazem metabolites. J Med Chem. 1992 Aug;35(17):3246-3253. Pubmedid: 1507210 .
• Neidhart D, Howell P, Petsko G, Powers V, Li R, Kenyon G, Gerlt J. Mechanism of the reaction catalyzed by mandelate racemase. 2. Crystal structureof mandelate racemase at 2.5-A resolution: identification of the active site andpossible catalytic residues. Biochemistry. 1991 Sep;30(38):9264-9273. Pubmedid: 1892834 .
• Xiao X, Li R, Zhuang H, Ewing B, Karunaratne K, Lillig J, Brown R, NicolaouKC. Solid-phase combinatorial synthesis using MicroKan reactors, Rf tagging, and directed sorting. Biotechnol Bioeng. 2000 Win;71(1):44-50. Pubmedid: 10629535.