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Our Science – Thomas Website

Craig J. Thomas, Ph.D.

Selected Publications

1)  Jiang JK, McCoy JG, Shen M, Leclair CA, Huang W, Negri A, Li J, Blue R, Harrington AW, Naini S, David G, Choi WS, Volpi E, Fernandez J, Babayeva M, Nedelman MA, Filizola M, Coller BS, Thomas CJ.
A novel class of ion displacement ligands as antagonists of the aIIbß3 receptor that limit conformational reorganization of the receptor.
Bioorg. Med. Chem. Lett. 2014.
[Journal]
2)  Thomas CJ, McKew JC.
Editorial: Playing Well with Others! Initiating and Sustaining Successful Collaborations between Industry, Academia and Government.
Curr Top Med Chem. 14: 291-3, 2014.
[Journal]
3)  Shukla S, Chufan EE, Singh S, Skoumbourdis AP, Kapoor K, Boxer MB, Duveau DY, Thomas CJ, Talele TT, Ambudkar SV.
Elucidation of the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna(®)) with the human ABC drug transporter P-glycoprotein.
Leukemia. 2014.
[Journal]
4)  Mathews Griner LA, Guha R, Shinn P, Young RM, Keller JM, Liu D, Goldlust IS, Yasgar A, McKnight C, Boxer MB, Duveau DY, Jiang JK, Michael S, Mierzwa T, Huang W, Walsh MJ, Mott BT, Patel P, Leister W, Maloney DJ, Leclair CA, Rai G, Jadhav A, Peyser BD, Austin CP, Martin SE, Simeonov A, Ferrer M, Staudt LM, Thomas CJ.
High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells.
Proc. Natl. Acad. Sci. U.S.A. 2014.
[Journal]
5)  Duveau DY, Yasgar A, Wang Y, Hu X, Kouznetsova J, Brimacombe KR, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ.
Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.
Bioorg. Med. Chem. Lett. 24: 630-5, 2014.
[Journal]
6)  Jain N, Miu B, Jiang JK, McKinstry KK, Prince A, Swain SL, Greiner DL, Thomas CJ, Sanderson MJ, Berg LJ, Kang J.
CD28 and ITK signals regulate autoreactive T cell trafficking.
Nat. Med. 2013.
[Journal]
7)  Lin DC, Xu L, Ding LW, Sharma A, Liu LZ, Yang H, Tan P, Vadgama J, Karlan BY, Lester J, Urban N, Schummer M, Doan N, Said JW, Sun H, Walsh M, Thomas CJ, Patel P, Yin D, Chan D, Koeffler HP.
Genomic and functional characterizations of phosphodiesterase subtype 4D in human cancers.
Proc. Natl. Acad. Sci. U.S.A. 110: 6109-14, 2013.
[Journal]
8)  Patel PR, Sun H, Li SQ, Shen M, Khan J, Thomas CJ, Davis MI.
Identification of potent Yes1 kinase inhibitors using a library screening approach.
Bioorg. Med. Chem. Lett. 23: 4398-403, 2013.
[Journal]
9)  Chen J, Feigenbaum L, Awasthi P, Butcher DO, Anver MR, Golubeva YG, Bamford R, Zhang X, St Claire MB, Thomas CJ, Discepolo V, Jabri B, Waldmann TA.
Insulin-dependent diabetes induced by pancreatic beta cell expression of IL-15 and IL-15Ra.
Proc. Natl. Acad. Sci. U.S.A. 110: 13534-9, 2013.
[Journal]
10)  Mathews LA, Keller JM, McKnight C, Michael S, Shinn P, Liu D, Staudt LM, Thomas CJ, Ferrer M.
Multiplexing High-Content Flow (HCF) and Quantitative High-Throughput Screening (qHTS) to Identify Compounds Capable of Decreasing Cell Viability, Activating Caspase 3/7, Expressing Annexin V, and Changing Mitochondrial Membrane Integrity.
Curr Protoc Chem Biol. 5: 195-212, 2013.
[Journal]
11)  Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ.
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
Bioorg. Med. Chem. Lett. 23: 682-6, 2013.
[Journal]
12)  Johnson BC, Pauly GT, Rai G, Patel D, Bauman JD, Baker HL, Das K, Schneider JP, Maloney DJ, Arnold E, Thomas CJ, Hughes SH.
A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants.
Retrovirology. 9: 99, 2012.
[Journal]
13)  Mott BT, Cheng KC, Guha R, Kommer VP, Williams DL, Vermeire JJ, Cappello M, Maloney DJ, Rai G, Jadhav A, Simeonov A, Inglese J, Posner GH, Thomas CJ.
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
Medchemcomm. 3: 1505-1511, 2012.
[Journal]
14)  Zhu J, Choi WS, McCoy JG, Negri A, Zhu J, Naini S, Li J, Shen M, Huang W, Bougie D, Rasmussen M, Aster R, Thomas CJ, Filizola M, Springer TA, Coller BS.
Structure-guided design of a high-affinity platelet integrin aIIbß3 receptor antagonist that disrupts Mg²? binding to the MIDAS.
Sci Transl Med. 4: 125ra32, 2012.
[Journal]
15)  Nayar R, Enos M, Prince A, Shin H, Hemmers S, Jiang JK, Klein U, Thomas CJ, Berg LJ.
TCR signaling via Tec kinase ITK and interferon regulatory factor 4 (IRF4) regulates CD8+ T-cell differentiation.
Proc. Natl. Acad. Sci. U.S.A. 109: E2794-802, 2012.
[Journal]
16)  Mathews LA, Keller JM, Goodwin BL, Guha R, Shinn P, Mull R, Thomas CJ, de Kluyver RL, Sayers TJ, Ferrer M.
A 1536-Well Quantitative High-Throughput Screen to Identify Compounds Targeting Cancer Stem Cells.
J. Biomol. Screen. 17: 1231-42, 2012.
[Journal]
17)  Law AJ, Wang Y, Sei Y, O'Donnell P, Piantadosi P, Papaleo F, Straub RE, Huang W, Thomas CJ, Vakkalanka R, Besterman AD, Lipska BK, Hyde TM, Harrison PJ, Kleinman JE, Weinberger DR.
Neuregulin 1-ErbB4-PI3K signaling in schizophrenia and phosphoinositide 3-kinase-p110δ inhibition as a potential therapeutic strategy.
Proc. Natl. Acad. Sci. U.S.A. 109: 12165-70, 2012.
[Journal]
18)  Anastasiou D, Yu Y, Israelsen WJ, Jiang J, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park H, Cantley LC, Thomas CJ, Heiden MG.
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Nat. Chem. Biol. 8: 839-47, 2012.
[Journal]
19)  Heidebrecht RW, Mulrooney C, Austin CP, Barker RH, Beaudoin JA, Cheng KC, Comer E, Dandapani S, Dick J, Duvall JR, Ekland EH, Fidock DA, Fitzgerald ME, Foley M, Guha R, Hinkson P, Kramer M, Lukens AK, Masi D, Marcaurelle LA, Su X, Thomas CJ, Weïwer M, Wiegand RC, Wirth D, Xia M, Yuan J, Zhao J, Palmer M, Munoz B, Schreiber S.
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.
ACS Med. Chem. Lett. 3: 112-117, 2012.
[Journal]
20)  Rahier NJ, Thomas CJ, Hecht SM.
Cragg GM, Kingston DG, Newman DJ, eds.
Captothecin and Its Analogs. In: Anticancer Agents from Natural Products, Second Edition.
Boca Raton: CRC Press; 2011. p. 5-25 [Book Chapter]
21)  Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Bioorg. Med. Chem. Lett. 21: 6322-7, 2011.
[Journal]
22)  Englund EE, Neumann S, Eliseeva E, McCoy JG, Titus S, Zheng W, Southall N, Shinn P, Leister W, Thomas CJ, Inglese J, Austin CP, Gershengorn MC, Huang W.
The synthesis and evaluation of dihydroquinazolin-4-ones and quinazolin-4-ones as thyroid stimulating hormone receptor agonists.
MedChemComm. 2: 1016-1020, 2011.
[Journal]
23)  Jiang JK, Shen M, Thomas CJ, Boxer MB.
Chiral kinase inhibitors.
Curr Top Med Chem. 11: 800-9, 2011.
[Journal]
24)  Chung S, Himmel DM, Jiang JK, Wojtak K, Bauman JD, Rausch JW, Wilson JA, Beutler JA, Thomas CJ, Arnold E, Le Grice SF.
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.
J. Med. Chem. 54: 4462-73, 2011.
[Journal]
25)  Ju W, Zhang M, Jiang JK, Thomas CJ, Oh U, Bryant BR, Chen J, Sato N, Tagaya Y, Morris JC, Janik JE, Jacobson S, Waldmann TA.
CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP.
Blood. 117: 1938-46, 2011.
[Journal]
26)  Guha R, Dexheimer TS, Kestranek AN, Jadhav A, Chervenak AM, Ford MG, Simeonov A, Roth GP, Thomas CJ.
Exploratory analysis of kinetic solubility measurements of a small molecule library.
Bioorg. Med. Chem. 19: 4127-34, 2011.
[Journal]
27)  Anastasiou D, Poulogiannis G, Asara JM, Boxer MB, Jiang JK, Shen M, Bellinger G, Sasaki AT, Locasale JW, Auld DS, Thomas CJ, Vander Heiden MG, Cantley LC.
Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses.
Science. 334: 1278-83, 2011.
[Journal]
28)  Ghoreschi K, Jesson MI, Li X, Lee JL, Ghosh S, Alsup JW, Warner JD, Tanaka M, Steward-Tharp SM, Gadina M, Thomas CJ, Minnerly JC, Storer CE, LaBranche TP, Radi ZA, Dowty ME, Head RD, Meyer DM, Kishore N, O'Shea JJ.
Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550).
J. Immunol. 186: 4234-43, 2011.
[Journal]
29)  Holm TM, Habashi JP, Doyle JJ, Bedja D, Chen Y, van Erp C, Lindsay ME, Kim D, Schoenhoff F, Cohn RD, Loeys BL, Thomas CJ, Patnaik S, Marugan JJ, Judge DP, Dietz HC.
Noncanonical TGF-beta signaling contributes to aortic aneurysm progression in Marfan syndrome mice.
Science. 332: 358-61, 2011.
[Journal]
30)  Yuan P, Tragon T, Xia M, Leclair CA, Skoumbourdis AP, Zheng W, Thomas CJ, Huang R, Austin CP, Chen G, Guitart X.
Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents.
Pharmacol. Biochem. Behav. 98: 349-55, 2011.
[Journal]
31)  Rosenthal AS, Tanega C, Shen M, Mott BT, Bougie JM, Nguyen DT, Misteli T, Auld DS, Maloney DJ, Thomas CJ.
Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).
Bioorg. Med. Chem. Lett. 21: 3152-8, 2011.
[Journal]
32)  Shukla S, Skoumbourdis AP, Walsh MJ, Hartz AM, Fung KL, Wu CP, Gottesman MM, Bauer B, Thomas CJ, Ambudkar SV.
Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters.
Mol. Pharm. 8: 1292-302, 2011.
[Journal]
33)  Boxer MB, Quinn AM, Shen M, Jadhav A, Leister W, Simeonov A, Auld DS, Thomas CJ.
A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety.
ChemMedChem. 5: 730-8, 2010.
[Journal]
34)  Neumann S, Huang W, Eliseeva E, Titus S, Thomas CJ, Gershengorn MC.
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
Endocrinology. 151: 3454-9, 2010.
[Journal]
35)  Auld DS, Thorne N, Boxer MB, Southall N, Shen M, Thomas CJ, Inglese J.
Understanding Enzymes as Reporters or Targets in Assays Using Quantitative High-throughput Screening (qHTS). In: Experimental Standard Conditions of Enzyme Characterizations.
Germany: Beilstein-Institut; 2010. p. 21-43 [Book Chapter]
36)  Feng J, Petersen CD, Coy DH, Jiang JK, Thomas CJ, Pollak MR, Wank SA.
Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion.
Proc. Natl. Acad. Sci. U.S.A. 107: 17791-6, 2010.
[Journal]
37)  Davis RE, Ngo VN, Lenz G, Tolar P, Young RM, Romesser PB, Kohlhammer H, Lamy L, Zhao H, Yang Y, Xu W, Shaffer AL, Wright G, Xiao W, Powell J, Jiang JK, Thomas CJ, Rosenwald A, Ott G, Muller-Hermelink HK, Gascoyne RD, Connors JM, Johnson NA, Rimsza LM, Campo E, Jaffe ES, Wilson WH, Delabie J, Smeland EB, Fisher RI, Braziel RM, Tubbs RR, Cook JR, Weisenburger DD, Chan WC, Pierce SK, Staudt LM.
Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma.
Nature. 463: 88-92, 2010.
[Journal]
38)  Dolle RE, Bourdonnec BL, Worm K, Morales GA, Thomas CJ, Zhang W.
Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.
J Comb Chem. 12: 765-806, 2010.
[Journal]
39)  Rui L, Emre NC, Kruhlak MJ, Chung HJ, Steidl C, Slack G, Wright GW, Lenz G, Ngo VN, Shaffer AL, Xu W, Zhao H, Yang Y, Lamy L, Davis RE, Xiao W, Powell J, Maloney D, Thomas CJ, Möller P, Rosenwald A, Ott G, Muller-Hermelink HK, Savage K, Connors JM, Rimsza LM, Campo E, Jaffe ES, Delabie J, Smeland EB, Weisenburger DD, Chan WC, Gascoyne RD, Levens D, Staudt LM.
Cooperative epigenetic modulation by cancer amplicon genes.
Cancer Cell. 18: 590-605, 2010.
[Journal]
40)  Boxer MB, Jiang JK, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ.
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
J. Med. Chem. 53: 1048-55, 2010.
[Journal]
41)  Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ.
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Bioorg. Med. Chem. Lett. 20: 3387-93, 2010.
[Journal]
42)  Mott BT, Ferreira RS, Simeonov A, Jadhav A, Ang KK, Leister W, Shen M, Silveira JT, Doyle PS, Arkin MR, McKerrow JH, Inglese J, Austin CP, Thomas CJ, Shoichet BK, Maloney DJ.
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
J. Med. Chem. 53: 52-60, 2010.
[Journal]
43)  Auld DS, Lovell S, Thorne N, Lea WA, Maloney DJ, Shen M, Rai G, Battaile KP, Thomas CJ, Simeonov A, Hanzlik RP, Inglese J.
Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124.
Proc. Natl. Acad. Sci. U.S.A. 107: 4878-83, 2010.
[Journal]
44)  Jadhav A, Ferreira RS, Klumpp C, Mott BT, Austin CP, Inglese J, Thomas CJ, Maloney DJ, Shoichet BK, Simeonov A.
Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
J. Med. Chem. 53: 37-51, 2010.
[Journal]
45)  Leclair CA, Boxer MB, Thomas CJ, Maloney DJ.
Total synthesis of LL-Z1640-2 utilizing a late-stage intramolecular Nozaki-Hiyama-Kishi reaction.
Tetrahedron Lett. 51: 6852-6855, 2010.
[Journal]
46)  Auld DS, Zhang YQ, Southall NT, Rai G, Landsman M, MacLure J, Langevin D, Thomas CJ, Austin CP, Inglese J.
A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.
J. Med. Chem. 52: 1450-8, 2009.
[Journal]
47)  Tanega C, Shen M, Mott BT, Thomas CJ, MacArthur R, Inglese J, Auld DS.
Comparison of bioluminescent kinase assays using substrate depletion and product formation.
Assay Drug Dev Technol. 7: 606-14, 2009.
[Journal]
48)  Dolle RE, Le Bourdonnec B, Goodman AJ, Morales GA, Thomas CJ, Zhang W.
Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008.
J Comb Chem. 11: 739-90, 2009.
[Journal]
49)  Mott BT, Tanega C, Shen M, Maloney DJ, Shinn P, Leister W, Marugan JJ, Inglese J, Austin CP, Misteli T, Auld DS, Thomas CJ.
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
Bioorg. Med. Chem. Lett. 19: 6700-5, 2009.
[Journal]
50)  Skoumbourdis AP, Leclair CA, Stefan E, Turjanski AG, Maguire W, Titus SA, Huang R, Auld DS, Inglese J, Austin CP, Michnick SW, Xia M, Thomas CJ.
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
Bioorg. Med. Chem. Lett. 19: 3686-92, 2009.
[Journal]
51)  Fernandes AF, Bian Q, Jiang JK, Thomas CJ, Taylor A, Pereira P, Shang F.
Proteasome inactivation promotes p38 mitogen-activated protein kinase-dependent phosphatidylinositol 3-kinase activation and increases interleukin-8 production in retinal pigment epithelial cells.
Mol. Biol. Cell. 20: 3690-9, 2009.
[Journal]
52)  Zhu PJ, Hobson JP, Southall N, Qiu C, Thomas CJ, Lu J, Inglese J, Zheng W, Leppla SH, Bugge TH, Austin CP, Liu S.
Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.
Bioorg. Med. Chem. 17: 5139-45, 2009.
[Journal]
53)  Neumann S, Huang W, Titus S, Krause G, Kleinau G, Alberobello AT, Zheng W, Southall NT, Inglese J, Austin CP, Celi FS, Gavrilova O, Thomas CJ, Raaka BM, Gershengorn MC.
Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.
Proc. Natl. Acad. Sci. U.S.A. 106: 12471-6, 2009.
[Journal]
54)  Rai G, Sayed AA, Lea WA, Luecke HF, Chakrapani H, Prast-Nielsen S, Jadhav A, Leister W, Shen M, Inglese J, Austin CP, Keefer L, Arnér ES, Simeonov A, Maloney DJ, Williams DL, Thomas CJ.
Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.
J. Med. Chem. 52: 6474-83, 2009.
[Journal]
55)  Rai G, Thomas CJ, Leister W, Maloney DJ.
Synthesis of Oxadiazole-2-oxide Analogues as Potential Antischistosomal Agents.
Tetrahedron Lett. 50: 1710-1713, 2009.
[Journal]
56)  Thomas CJ, Auld DS, Huang R, Huang W, Jadhav A, Johnson RL, Leister W, Maloney DJ, Marugan JJ, Michael S, Simeonov A, Southall N, Xia M, Zheng W, Inglese J, Austin CP.
The pilot phase of the NIH Chemical Genomics Center.
Curr Top Med Chem. 9: 1181-93, 2009.
[Journal]
57)  Neumann S, Kleinau G, Costanzi S, Moore S, Jiang JK, Raaka BM, Thomas CJ, Krause G, Gershengorn MC.
A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism.
Endocrinology. 149: 5945-50, 2008.
[Journal]
58)  Engel S, Skoumbourdis AP, Childress J, Neumann S, Deschamps JR, Thomas CJ, Colson AO, Costanzi S, Gershengorn MC.
A virtual screen for diverse ligands: discovery of selective G protein-coupled receptor antagonists.
J. Am. Chem. Soc. 130: 5115-23, 2008.
[Journal]
59)  Marinello J, Marchand C, Mott BT, Bain A, Thomas CJ, Pommier Y.
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants.
Biochemistry. 47: 9345-54, 2008.
[Journal]
60)  Babaoglu K, Simeonov A, Irwin JJ, Nelson ME, Feng B, Thomas CJ, Cancian L, Costi MP, Maltby DA, Jadhav A, Inglese J, Austin CP, Shoichet BK.
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
J. Med. Chem. 51: 2502-11, 2008.
[Journal]
61)  Dolle RE, Le Bourdonnec B, Goodman AJ, Morales GA, Thomas CJ, Zhang W.
Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2007.
J Comb Chem. 10: 753-802, 2008.
[Journal]
62)  Jiang JK, Ghoreschi K, Deflorian F, Chen Z, Perreira M, Pesu M, Smith J, Nguyen DT, Liu EH, Leister W, Costanzi S, O'Shea JJ, Thomas CJ.
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).
J. Med. Chem. 51: 8012-8, 2008.
[Journal]
63)  Simeonov A, Jadhav A, Thomas CJ, Wang Y, Huang R, Southall NT, Shinn P, Smith J, Austin CP, Auld DS, Inglese J.
Fluorescence spectroscopic profiling of compound libraries.
J. Med. Chem. 51: 2363-71, 2008.
[Journal]
64)  Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Bioorg. Med. Chem. Lett. 18: 1297-303, 2008.
[Journal]
65)  Xie Y, Deng S, Thomas CJ, Liu Y, Zhang YQ, Rinderspacher A, Huang W, Gong G, Wyler M, Cayanis E, Aulner N, Többen U, Chung C, Pampou S, Southall N, Vidović D, Schürer S, Branden L, Davis RE, Staudt LM, Inglese J, Austin CP, Landry DW, Smith DH, Auld DS.
Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.
Bioorg. Med. Chem. Lett. 18: 329-35, 2008.
[Journal]
66)  Sayed AA, Simeonov A, Thomas CJ, Inglese J, Austin CP, Williams DL.
Identification of oxadiazoles as new drug leads for the control of schistosomiasis.
Nat. Med. 14: 407-12, 2008.
[Journal]
67)  Bhanu NV, Lee YT, Oneal PA, Gantt NM, Aerbajinai W, Noel P, Thomas CJ, Miller JL.
Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives.
Biochim. Biophys. Acta. 1782: 504-10, 2008.
[Journal]
68)  Simeonov A, Jadhav A, Sayed AA, Wang Y, Nelson ME, Thomas CJ, Inglese J, Williams DL, Austin CP.
Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade.
PLoS Negl Trop Dis. 2: e127, 2008.
[Journal]
69)  Titus S, Neumann S, Zheng W, Southall N, Michael S, Klumpp C, Yasgar A, Shinn P, Thomas CJ, Inglese J, Gershengorn MC, Austin CP.
Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor.
J Biomol Screen. 13: 120-7, 2008.
[Journal]
70)  Readinger JA, Schiralli GM, Jiang JK, Thomas CJ, August A, Henderson AJ, Schwartzberg PL.
Selective targeting of ITK blocks multiple steps of HIV replication.
Proc. Natl. Acad. Sci. U.S.A. 105: 6684-9, 2008.
[Journal]
71)  Tikhonova IG, Sum CS, Neumann S, Thomas CJ, Raaka BM, Costanzi S, Gershengorn MC.
Bidirectional, iterative approach to the structural delineation of the functional.
J. Med. Chem. 50: 2981-9, 2007.
[Journal]
72)  Kim EJ, Amorelli B, Abdo M, Thomas CJ, Love DC, Knapp S, Hanover JA.
Distinctive inhibition of O-GlcNAcase isoforms by an alpha-GlcNAc thiolsulfonate.
J. Am. Chem. Soc. 129: 14854-5, 2007.
[Journal]
73)  Huang W, Zheng W, Urban DJ, Inglese J, Sidransky E, Austin CP, Thomas CJ.
N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Bioorg. Med. Chem. Lett. 17: 5783-9, 2007.
[Journal]
74)  Skoumbourdis AP, Moore S, Landsman M, Thomas CJ.
Synthesis of Substituted 2-phenylhistamines via a Microwave Promoted Suzuki Coupling.
Tetrahedron Lett. 48: 9140-9143, 2007.
[Journal]
75)  Jäschke H, Neumann S, Moore S, Thomas CJ, Colson AO, Costanzi S, Kleinau G, Jiang JK, Paschke R, Raaka BM, Krause G, Gershengorn MC.
A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).
J. Biol. Chem. 281: 9841-4, 2006.
[Journal]
76)  Hu J, Jiang J, Costanzi S, Thomas CJ, Yang W, Feyen JH, Jacobson KA, Spiegel AM.
A missense mutation in the seven-transmembrane domain of the human Ca2+ receptor converts a negative allosteric modulator into a positive allosteric modulator.
J. Biol. Chem. 281: 21558-65, 2006.
[Journal]
77)  Kim EJ, Perreira M, Thomas CJ, Hanover JA.
An O-GlcNAcase-specific inhibitor and substrate engineered by the extension of the N-acetyl moiety.
J. Am. Chem. Soc. 128: 4234-5, 2006.
[Journal]
78)  Moore S, Jaeschke H, Kleinau G, Neumann S, Costanzi S, Jiang JK, Childress J, Raaka BM, Colson A, Paschke R, Krause G, Thomas CJ, Gershengorn MC.
Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.
J. Med. Chem. 49: 3888-96, 2006.
[Journal]
79)  Arimondo PB, Thomas CJ, Oussedik K, Baldeyrou B, Mahieu C, Halby L, Guianvarc'h D, Lansiaux A, Hecht SM, Bailly C, Giovannangeli C.
Exploring the cellular activity of camptothecin-triple-helix-forming oligonucleotide conjugates.
Mol. Cell. Biol. 26: 324-33, 2006.
[Journal]
80)  Thomas CJ.
Fluorinated natural products with clinical significance.
Curr Top Med Chem. 6: 1529-43, 2006.
[Journal]
81)  Perreira M, Kim EJ, Thomas CJ, Hanover JA.
Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry.
Bioorg. Med. Chem. 14: 837-46, 2006.
[Journal]
82)  De Soto JA, Wang X, Tominaga Y, Wang RH, Cao L, Qiao W, Li C, Xu X, Skoumbourdis AP, Prindiville SA, Thomas CJ, Deng CX.
The inhibition and treatment of breast cancer with poly (ADP-ribose) polymerase (PARP-1) inhibitors.
Int. J. Biol. Sci. 2: 179-85, 2006.
[Journal]
83)  Perreira M, Jiang J, Klutz AM, Gao Z, Shainberg A, Lu C, Thomas CJ, Jacobson KA.
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
J. Med. Chem. 48: 4910-8, 2005.
[Journal]
84)  Rahier NJ, Thomas CJ, Hecht SM.
Cragg GM, Kingston DG, Newman DJ, eds.
Captothecin and Its Analogs. In: In: Anticancer Agents from Natural Products.
Boca Raton: CRC Press; 2005. p. 5-21 [Book Chapter]
85)  Hu J, McLarnon SJ, Mora S, Jiang J, Thomas CJ, Jacobson KA, Spiegel AM.
A region in the seven-transmembrane domain of the human Ca2+ receptor critical for response to Ca2+.
J. Biol. Chem. 280: 5113-20, 2005.
[Journal]
86)  Jiang JK, Thomas CJ, Neumann S, Lu X, Rice KC, Gershengorn MC.
1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors.
Bioorg. Med. Chem. Lett. 15: 733-6, 2005.
[Journal]
87)  Arimondo PB, Laco GS, Thomas CJ, Halby L, Pez D, Schmitt P, Boutorine A, Garestier T, Pommier Y, Hecht SM, Sun JS, Bailly C.
Activation of camptothecin derivatives by conjugation to triple helix-forming oligonucleotides.
Biochemistry. 44: 4171-80, 2005.
[Journal]
88)  Besada P, Mamedova L, Thomas CJ, Costanzi S, Jacobson KA.
Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality.
Org. Biomol. Chem. 3: 2016-25, 2005.
[Journal]
89)  Thomas CJ, Rahier NJ, Hecht SM.
Camptothecin: current perspectives.
Bioorg. Med. Chem. 12: 1585-604, 2004.
[Journal]
90)  Rishel MJ, Thomas CJ, Tao ZF, Vialas C, Leitheiser CJ, Hecht SM.
Conformationally constrained analogues of bleomycin A5.
J. Am. Chem. Soc. 125: 10194-205, 2003.
[Journal]
91)  Leitheiser CJ, Smith KL, Rishel MJ, Hashimoto S, Konishi K, Thomas CJ, Li C, McCormick MM, Hecht SM.
Solid-phase synthesis of bleomycin group antibiotics. Construction of a 108-member deglycobleomycin library.
J. Am. Chem. Soc. 125: 8218-27, 2003.
[Journal]
92)  Wolak MA, Thomas CJ, Gillespie NB, Birge RR, Lees WJ.
Tuning the optical properties of fluorinated indolylfulgimides.
J. Org. Chem. 68: 319-26, 2003.
[Journal]
93)  Thomas CJ, McCormick MM, Vialas C, Tao ZF, Leitheiser CJ, Rishel MJ, Wu X, Hecht SM.
Alteration of the selectivity of DNA cleavage by a deglycobleomycin analogue containing a trithiazole moiety.
J. Am. Chem. Soc. 124: 3875-84, 2002.
[Journal]
94)  Thomas CJ, Chizhov AO, Leitheiser CJ, Rishel MJ, Konishi K, Tao ZF, Hecht SM.
Solid-phase synthesis of bleomycin A(5) and three monosaccharide analogues: exploring the role of the carbohydrate moiety in RNA cleavage.
J. Am. Chem. Soc. 124: 12926-7, 2002.
[Journal]
95)  Wolak MA, Finn RC, Rarig RS, Thomas CJ, Hammond RP, Birge RR, Zubieta J, Lees WJ.
Structural properties of a series of photochromic fluorinated indolylfulgides.
Acta Crystallogr C. 58: o389-93, 2002.
[Journal]
96)  Wolak MA, Gillespie NB, Thomas CJ, Birge RR, Lees WJ.
Optical and thermal properties of photochromic fluorinated adamantylidene indolyfulgides.
J. Photochem. Photobiol. A: Chem. 147: 39-44, 2002.
[Journal]
97)  Thomas CJ, Wolak MA, Birge RR, Lees WJ.
Improved synthesis of indolyl fulgides.
J. Org. Chem. 66: 1914-8, 2001.
[Journal]
98)  Wolak MA, Sullivan JM, Thomas CJ, Finn RC, Birge RR, Lees WJ.
Thermolysis of a fluorinated indolylfulgide features a novel 1,5-indolyl shift.
J. Org. Chem. 66: 4739-41, 2001.
[Journal]
99)  Wolak MA, Gillespie NB, Thomas CJ, Birge RR, Lees WJ.
Optical properties of photochromic fluorinated indolyfulgides.
J. Photochem. Photobiol. A: Chem. 144: 83-91, 2001.
[Journal]
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