Kulak O, Yamaguchi K, and Lum L. High-throughput strategies using multiplexed pathway read-outs to identify therapeutic small molecule leads. Chemical Biology--Methods and Protocols (in press).
Fan C-W, Chen B, Franco I, Lu J, Shi H, Wei S, Wang C, Wu X, Tang W, Roth MG, Williams NS, Hirsch E, Chen C, and Lum L. The Hedgehog pathway effector Smoothened exhibits signaling competency in the absence of ciliary accumulation Chemistry and Biology. Published on-line Dec. 4 2014.
Zhong R, Kim J, Kim H, Kim M, Lum L, Levine B, Xiao G, White M, and Xie Y. Computational detection and suppression of sequence-specific off-target phenotypes from whole genome RNAi screens. Nucleic Acids Res. 2014 Sep 1;42(13):8214-22.
Singel SM, Cornelius C, Zaganjor E, Batten K, Sarode VR, Buckley DL, Peng Y, John GB, Li HC, Sadeghi N, Wright WE, Lum L, Corson TW, Shay JW. KIF14 Promotes AKT phosphorylation and contributes to chemoresistance in triple-negative breast cancer. Neoplasia 2014. Mar; 16(3):247-256.
Das A, Tanigawa S, Karner CM, Xin M, Lum L, Chen C, Olson EN, Perantoni AO, and Carroll TJ. Stromal-epithelial crosstalk regulates kidney progenitor cell differentiation. Nat. Cell Biol 2013 Sep;15(9):1035-44.
Kulak O and Lum L. A multiplexed luciferase-based screening platform for interrogating cancer-associated signal transduction in cultured cells. J Vis Exp 2013 Jul 3;(77).
Fan C-h, Tuladhar R, and Lum L. Signaling: Making a leaner hedgehog. Nat. Chem Biol 2013 Apr;9(4):217-8.
Singel SM, Cornelius C, Batten K, Fasciani G, Wright WE, Lum L, Shay JW. A targeted RNAi screen of the breast cancer genome identifies KIF14 and TLN1 as genes that modulate docetaxel chemosensitivity in triple-negative breast cancer. Clin Cancer Res. 2013 Apr 15;19(8):2061-70.
Wang X, Moon J, Dodge ME, Pan X, Zhang L, Hanson J, Tuladhar R, Ma Z, Shi H, Williams NS, Amatruda J, Carroll TJ, Lum L, Chen C. The Development of Highly Potent Inhibitors for Porcupine. J Med Chem 2013 Mar 28;56(6):2700-4.
Takebe N, Lum L, and Ivy, SP. Wnt Signaling in Cancer Pathogenesis and Therapeutics. Signaling Pathways in Cancer Pathogenesis and Therapy 2012, 1-94, DOI: 10.1007/978-1-4614-1216-8_6.
Wu X and Lum L. Hedgehog signaling proteins. McGraw-Hill Yearbook of Science and Technology 2013. Dec 10, 2012. ISBN-10: 0071801405, ISBN-13: 978-0071801409.
Lum L and Clevers H. Cell biology. The unusual case of Porcupine. Science 2012 Aug 24;337(6097):922-3.
Moro E, Ozhan-Kizil G, Mongera A, Beis D, Wierzbicki C, Young RM, Bournele D, Domenichini A, Valdivia LE, Lum L, Chen C, Amatruda JF, Tiso N, Weidinger G, Argenton F. In vivo Wnt signaling tracing through a transgenic biosensor fish reveals novel activity domains. Dev Biol 2012 Jun 15;366(2):327-40.
Dodge ME, Moon J, Tuladhar R, Lu J, Jacob LS, Zhang LS, Shi H, Wang X, Moro E, Mongera A, Argenton F, Karner CM, Carroll TJ, Chen C, Amatruda JF, Lum L. Diverse chemical scaffolds support direct inhibition of the membrane bound O-acyltransferase Porcupine. J Biol Chem 2012 Jun 29;287(27):23246-54.
Gao S, Wang Q, Wang G, Lomenick B, Liu J, Fan C-W, Deng L-W, Huang J, Lum L, and Chen C. The Chemistry and Biology of Nakiterpiosin. Synlett 2012 23(16): 2298-2310.
Zhang X, Farrell A, Daniel C, Arnold H, Scanlan C, Laraway B, Janghorban M, Lum L, Chen D, Troxell M, and Sears RC. Mechanistic insight into Myc stabilization in breast cancer involving aberrant Axin1 expression. PNAS 2012 Feb 21;109(8):2790-5.
Jacob S, Wu X, Dodge M, Kulak O, Chen B, Fan C-W, Tang W, Wang B, Amatruda JF, and Lum L. Genome-wide RNAi screen reveals disease-associated genes that are common to Hedgehog and Wnt signaling. Sci Signaling, 25 January 2011 Vol. 4, Issue 157, p. ra4.
Dodge M and Lum L. Drugging the cancer stem cell compartment: lessons learned from the Hh and Wnt signal transduction pathways. Annu Rev Pharmacol Toxicol. 2011 Feb 10;51:289-310.
Karner CM, Das A, Ma Z, Self M, Chen C, Lum L, Oliver G, and Carroll TJ. Canonical Wnt9b signaling balances progenitor cell expansion and differentiation during kidney development. Development 2011 Apr;138(7):1247-57.
Ren Y, Lee MY, Schliffke S, Paavola J, Amos PJ, Ge X, Ye M, Zhu S, Senyei G, Lum L, Ehrlich B, and Qyang Y. Small molecule Wnt inhibitors enhance the efficiency of BMP-4-directed cardiac differentiation of human pluripotent stem cells. J Mol Cell Cardiol 2011 Sep;51(3):280-7.
Gao S, Wang Q, Huang L, Lum L, and Chen C. Chemical and Biological Studies of Nakiterpiosin and Nakiterpiosinone. J Am Chem Soc 2010 Jan 13;132(1):371-83.
Karner, M., Dodge M.E., Ma Z, Lu J, Chen C, Lum L, and Carroll T.J. The PARP tankyrase is necessary for canonical Wnt signaling during development of the kidney. Dev Dyn 2010 Jun14; 239(7):2014-2023.
Chen B, Dodge M, Tang W, Lu J, Ma Z, Fan C-W, Wei S, Hao W, Kilgore J, Williams N, Roth M, Amatruda J, Chen C, and Lum L. Small molecule-mediated disruption of Wnt-dependent signal transduction in tissue regeneration and cancer. Nature Chem Biol 2009 Feb; 5(2):100-7.
Lu J, Ma Z, Hsieh JC, Fan CW, Chen W, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small molecule inhibitors of Wnt response. Bioorg Med Chem Lett 2009 Jul 15;19(14):3825-7.
Tang W, Dodge M, Gundapaneni D, Michnoff C, Roth M, and Lum L. A genome-wide RNAi screen for Wnt/β-catenin pathway components identifies unexpected roles for TCF transcription factors in cancer. PNAS 2008 Jul 15;105(28):9697-702.
Jacob L, and Lum L. Deconvoluting the Hedgehog signal transduction pathway in development and disease. Review. Science 2007 Oct 5; 318(5847): 66-8.
Jacob L, and Lum L. The Hedgehog signaling pathway. Sci STKE 2007 Oct 9; 2007(407): cm6.
Jacob L. and Lum L. The Hedgehog signaling pathway in Drosophila. Sci STKE 2007 Oct 9; 2007(407): cm7.
Echeverri CJ, Beachy PA, Baum B, Boutros M, Buchholz F, Chanda SK, Downward J, Ellenberg J, Fraser AG, Hacohen N, Hahn WC, Jackson AL, Kiger A, Linsley PS, Lum L, Ma Y, Mathey-Prevot B, Root DE, Sabatini DM, Taipale J, Perrimon N, Bernards R. Minimizing the risk of reporting false positives in large-scale RNAi screens. Nat Methods 2006 Oct 3; (10):777-9.
Yao S, Lum L, and Beachy PA. The ihog cell-surface proteins bind Hedgehog and mediate pathway activation. Cell 2006 Apr; 125(2):343-57.
Dorner S, Lum L, Kim M, Paro R, Beachy PA, Green R. A genomewide screen for components of the RNAi pathway in Drosophila cultured cells. PNAS 2006 Aug 8;103(32):11880-5.
Ma Y, Creanga A, Lum L, and Beachy PA. Prevalence of off-target effects in Drosophila RNAi screens. Nature 2006 Sept 21;443(7109):359-63.
Lum L, and P.A.Beachy. The Hedgehog Response Network: Sensors, Switches, and Routers. Science 2004 304, 1755-1759.
Zhang C, Williams EH, Guo Y, Lum L, and Beachy, PA. Extensive phosphorylation of Smoothened in Hedgehog pathway activation. PNAS 2004 Dec; 101: 17897-17899.
Weskamp G, Schlondorff J, Lum L, Becherer D, Kim T-W, Saftig P, Hartmann D, Murphy G, and Blobel CP. Evidence for a critical role of the TNF convertase (TACE) in ectodomain shedding of the p75 neurotrophin receptor (p75NTR). J Biol Chem 2004 Feb 6; 279 (6): 4241-9.
Lum L, Yao S, Mozer B, Rovescalli A, Von Kessler D, Nirenberg M, Beachy PA. Identification of Hedgehog pathway components by RNAi in Drosophila cultured cells. Science 2003 Mar 28; 299 (5615): 2039-45.
Lum L*, Zhang C*, Oh S, Mann R, Von Kessler DP, Taipale J, Weis-Garcia F, Gong R, Wang B, Beachy PA. Hedgehog signal transduction via Smoothened association with a cytoplasmic complex scaffolded by the atypical kinesin, Costal-2. Mol Cell 2003 Nov (12), 1261-1274.
Schlondorff J, Lum L, Blobel CP. Biochemical and pharmacological criteria define two shedding activities for TRANCE/OPGL that are distinct from the tumor necrosis factor alpha convertase. J Biol Chem 2001 May 4; 276(18): 14665-74.
Horiuchi K, Weskamp G, Lum L, Hammes HP, Cai H, Brodie TA, Ludwig T, Chiusaroli R, Baron R, Preissner KT, Manova K, Blobel CP. Potential role for ADAM15 in pathological neovascularization in mice. Mol Cell Biol 2003 Aug; 23(16): 5614-24.
Lum L*, Wong BR*, Josien R, Becherer JD, Erdjument-Bromage H, Schlondorff J, Tempst P, Choi Y, Blobel CP. Evidence for a role of a tumor necrosis factor-alpha (TNF-alpha)-converting enzyme-like protease in shedding of TRANCE, a TNF family member involved in osteoclastogenesis and dendritic cell survival. J Biol Chem 1999 May 7; 274(19): 13613-8.
Inoue D, Reid M, Lum L, Kratzschmar J, Weskamp G, Myung YM, Baron R, Blobel CP. Cloning and initial characterization of mouse meltrin beta and analysis of the expression of four metalloprotease-disintegrins in bone cells. J Biol Chem 1998 Feb 13; 273 (7): 4180-7.
Lum L, Reid MS, Blobel CP. Intracellular maturation of the mouse metalloprotease disintegrin MDC15. J Biol Chem 1998 Oct 2; 273 (40): 26236-47.
Lum L, Blobel CP. Evidence for distinct serine protease activities with a potential role in processing the sperm protein fertilin. Dev Biol 1997 Nov 1; 191(1):131-45.
Kratzschmar J, Lum L, Blobel CP. Metargidin, a membrane-anchored metalloprotease-disintegrin protein with an RGD integrin binding sequence. J Biol Chem 1996 Mar 1; 271(9): 4593-6.
Zhou BB, Waldrop GL, Lum L, Schachman HK. A 70-amino acid zinc-binding polypeptide fragment from the regulatory chain of aspartate transcarbamoylase causes marked changes in the kinetic mechanism of the catalytic trimer. Protein Sci 1994 Jun; 3(6): 967-74.
Lum L, Roth M, Chen B, Chen C, Dodge M, and Tang W. Wnt protein signaling inhibitors. WO/2009/155001. Filed May 27,2009. Published Jun 9, 2011. Issued May 21, 2013 (8,445,491). Describe the IWR and IWP classes of Wnt pathway inhibitors.
Lum L, Roth M, Chen B, Chen C, Dodge M, and Tang W. Wnt protein signaling inhibitors. Filed May 11, 2012. Describes diverse chemical scaffolds supporting Porcupine inhibition.
Lum L, and Chen C. Highly Potent Inhibitors of Porcupine. Filed May 14, 2012. Describes next-generation Porcupine inhibitors with picomolar potency.
Lum L and Kulak O. A Multiplexed Luciferase-Based Reporter Assay System Using Small Molecule Inhibitors of Firefly and Renilla Luciferase Enzymes. Filed Oct. 20, 2010. Published April 26, 2012. Issued Oct. 29, 2013 (12/908,754). Describes reagents that enable multiplexing of luciferase-based cellular read-outs.