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Wen-Cherng Lee

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Chemicals & Drugs

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Kendra Garrison; Tobias Hahn; Wen-Cherng Lee; Leona E Ling; Andrew D Weinberg; Emmanuel T Akporiaye
The small molecule TGF-β signaling inhibitor SM16 synergizes with agonistic OX40 antibody to suppress established mammary tumors and reduce spontaneous metastasis.
Leona E Ling; Wen-Cherng Lee
Tgf-beta type I receptor (Alk5) kinase inhibitors in oncology.
Daniel A Erlanson; Joseph W Arndt; Mark T Cancilla; Kathy Cao; Robert A Elling; Nicki English; Jessica Friedman; Stig K Hansen; Cathy Hession; Ingrid Joseph; Gnanasambandam Kumaravel; Wen-Cherng Lee; Ken E Lind; Robert S McDowell; Konrad Miatkowski; Christine Nguyen; Thinh B Nguyen; Sophia Park; Nuzhat Pathan; David M Penny; Michael J Romanowski; Daniel Scott; Laura Silvian; Robert L Simmons; Bradley T Tangonan; Wenjin Yang; Lihong Sun
Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.

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All Publications

2012: Kendra Garrison; Tobias Hahn; Wen-Cherng Lee; Leona E Ling; Andrew D Weinberg; Emmanuel T Akporiaye
The small molecule TGF-β signaling inhibitor SM16 synergizes with agonistic OX40 antibody to suppress established mammary tumors and reduce spontaneous metastasis.
Cancer immunology, immunotherapy : CII 2012;61(4):511-21.
2011: Leona E Ling; Wen-Cherng Lee
Tgf-beta type I receptor (Alk5) kinase inhibitors in oncology.
Current pharmaceutical biotechnology 2011;12(12):2190-202.
2011: Daniel A Erlanson; Joseph W Arndt; Mark T Cancilla; Kathy Cao; Robert A Elling; Nicki English; Jessica Friedman; Stig K Hansen; Cathy Hession; Ingrid Joseph; Gnanasambandam Kumaravel; Wen-Cherng Lee; Ken E Lind; Robert S McDowell; Konrad Miatkowski; Christine Nguyen; Thinh B Nguyen; Sophia Park; Nuzhat Pathan; David M Penny; Michael J Romanowski; Daniel Scott; Laura Silvian; Robert L Simmons; Bradley T Tangonan; Wenjin Yang; Lihong Sun
Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
Bioorganic & medicinal chemistry letters 2011;21(10):3078-83.
2010: Bin Ma; Kevin M Guckian; Edward Yin-Shiang Lin; Wen-Cherng Lee; Daniel Scott; Gnanasambandam Kumaravel; Timothy L Macdonald; Kevin R Lynch; Cheryl Black; Sowmya Chollate; Kyungmin Hahm; Gregg Hetu; Ping Jin; Yi Luo; Ellen Rohde; Anthony Rossomando; Robert Scannevin; Joy Wang; Chunhua Yang
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Bioorganic & medicinal chemistry letters 2010;20(7):2264-9.
2010: Marco A Biamonte; Ryan Van de Water; Joseph W Arndt; Robert H Scannevin; Daniel Perret; Wen-Cherng Lee
Heat shock protein 90: inhibitors in clinical trials.
Journal of medicinal chemistry 2010;53(1):3-17.
2010: Kevin Guckian; Mary Beth Carter; Edward Yin-Shiang Lin; Michael Choi; Lihong Sun; P Ann Boriack-Sjodin; Claudio Chuaqui; Benjamin Lane; Kam Cheung; Leona Ling; Wen-Cherng Lee
Pyrazolone based TGFbetaR1 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(1):326-9.
2009: Dominique Bonafoux; Wen-Cherng Lee
Strategies for TGF-beta modulation: a review of recent patents.
Expert opinion on therapeutic patents 2009;19(12):1759-69.
2009: Matthew P Rausch; Tobias Hahn; Lalitha Ramanathapuram; Deborah Bradley-Dunlop; Daruka Mahadevan; Melania Mercado-Pimentel; Raymond Runyan; David G Besselsen; Xiamei Zhang; H-Kam Cheung; Wen-Cherng Lee; Leona E Ling; Emmanuel T Akporiaye
An orally active small molecule TGF-beta receptor I antagonist inhibits the growth of metastatic murine breast cancer.
Anticancer research 2009;29(6):2099-109.
2009: Dominique Bonafoux; Claudio Chuaqui; P Ann Boriack-Sjodin; Chris Fitch; Gretchen Hankins; Serene Josiah; Cheryl Black; Gregg Hetu; Leona Ling; Wen-Cherng Lee
2-Aminoimidazoles inhibitors of TGF-beta receptor 1.
Bioorganic & medicinal chemistry letters 2009;19(3):912-6.
2008: Mitchell S. Anscher; Bradley Thrasher; Larisa Zgonjanin; Zahid Rabbani; Michael J Corbley; Kai Fu; Lihong Sun; Wen-Cherng Lee; Leona E Ling; Zeljko Vujaskovic
Small molecular inhibitor of transforming growth factor-beta protects against development of radiation-induced lung injury.
International journal of radiation oncology, biology, physics 2008;71(3):829-37.
2008: Kai Fu; Michael J Corbley; Lihong Sun; Jessica E Friedman; Feng Shan; James L Papadatos; Donald Costa; Frank Lutterodt; Harry Sweigard; Scott Bowes; Michael Choi; P Ann Boriack-Sjodin; Robert M Arduini; Dongyu Sun; Miki N Newman; Xiamei Zhang; Jonathan N Mead; Claudio E Chuaqui; H-Kam Cheung; Xiamei Zhang; Mark Cornebise; Mary Beth Carter; Serene Josiah; Juswinder Singh; Wen-Cherng Lee; Alan Gill; Leona E Ling
SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model.
Arteriosclerosis, thrombosis, and vascular biology 2008;28(4):665-71.
2007: Peter C Simons; Susan M Young; Veronica Gibaja; Wen-Cherng Lee; Serene Josiah; Bruce S Edwards; Larry A Sklar
Duplexed, bead-based competitive assay for inhibitors of protein kinases.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 2007;71(7):451-9.
2007: Eiji Suzuki; Samuel Kim; H-Kam Cheung; Michael J Corbley; Xiamei Zhang; Lihong Sun; Feng Shan; Juswinder Singh; Wen-Cherng Lee; Steven M Albelda; Leona E Ling
A novel small-molecule inhibitor of transforming growth factor beta type I receptor kinase (SM16) inhibits murine mesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection.
Cancer research 2007;67(5):2351-9.
2006: Wataru Ishida; Yasuji Mori; Gabriella Lakos; Lihong Sun; Feng Shan; Scott Bowes; Serene Josiah; Wen-Cherng Lee; Juswinder Singh; Leona E Ling; john varga
Intracellular TGF-beta receptor blockade abrogates Smad-dependent fibroblast activation in vitro and in vivo.
The Journal of investigative dermatology 2006;126(8):1733-44.
2006: Dongyu Sun; Claudio Chuaqui; Zhan Deng; Scott Bowes; Donovan Chin; Juswinder Singh; Patrick Cullen; Gretchen Hankins; Wen-Cherng Lee; Jason Donnelly; Jessica Friedman; Serene Josiah
A kinase-focused compound collection: compilation and screening strategy.
Chemical biology & drug design 2006;67(6):385-94.
2005: R Blake Pepinsky; Wen-Cherng Lee; Mark Cornebise; Alan Gill; K Wortham; Ling Ling Chen; Diane R Leone; Keith Giza; Brian M Dolinski; Stuart J Perper; Cheryl Nickerson-Nutter; Doreen J Lepage; Abhijit Chakraborty; Eric T Whalley; Russell C Petter; Steven P Adams; Roy R Lobb; Daniel M Scott
Design, synthesis, and analysis of a polyethelene glycol-modified (PEGylated) small molecule inhibitor of integrin {alpha}4{beta}1 with improved pharmaceutical properties.
The Journal of pharmacology and experimental therapeutics 2005;312(2):742-50.
2004: Juswinder Singh; Leona E Ling; J Scott Sawyer; Wen-Cherng Lee; Faming Zhang; Jonathan M Yingling
Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5).
Current opinion in drug discovery & development 2004;7(4):437-45.
2004: Juswinder Singh; Steve Adams; Mary Beth Carter; Hernan Cuervo; Wen-Cherng Lee; Roy R Lobb; R Blake Pepinsky; Russell C Petter; Daniel Scott
Rational design of potent and selective VLA-4 inhibitors and their utility in the treatment of asthma.
Current topics in medicinal chemistry 2004;4(14):1497-507.
2003: Juswinder Singh; Claudio Chuaqui; P Ann Boriack-Sjodin; Wen-Cherng Lee; Timothy Pontz; Michael J Corbley; H-Kam Cheung; Robert M Arduini; Jonathan N Mead; Miki N Newman; James L Papadatos; Scott Bowes; Serene Josiah; Leona E Ling
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI).
Bioorganic & medicinal chemistry letters 2003;13(24):4355-9.
2003: Linda A Egger; Jin Cao; Christine McCallum; Usha Kidambi; Gail Van Riper; Ermengilda McCauley; Richard A Mumford; Thomas J Lanza; Linus S Lin; Stephen E de Laszlo; David N Young; Ginger Yang; Dennis C Dean; Conrad E Raab; Michael A Wallace; Allen Jones; William K Hagmann; John A Schmidt; R Blake Pepinsky; Daniel M Scott; Wen-Cherng Lee; Mark Cornebise; Patricia A Detmers
A small molecule alpha4beta1/alpha4beta7 antagonist differentiates between the low-affinity states of alpha4beta1 and alpha4beta7: characterization of divalent cation dependence.
The Journal of pharmacology and experimental therapeutics 2003;306(3):903-13.
2003: Paul J Hergenrother; Anne Hodgson; Andrew S Judd; Wen-Cherng Lee; Stephen F Martin
An abiotic strategy for the enantioselective synthesis of erythromycin B.
Angewandte Chemie (International ed. in English) 2003;42(28):3278-81.
2003: Diane R Leone; Keith Giza; Alan Gill; Brian M Dolinski; W Yang; Stuart J Perper; Daniel M Scott; Wen-Cherng Lee; Mark Cornebise; K Wortham; Cheryl Nickerson-Nutter; Ling Ling Chen; Doreen J Lepage; J C Spell; Eric T Whalley; Russell C Petter; Steven P Adams; Roy R Lobb; R Blake Pepinsky
An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis.
The Journal of pharmacology and experimental therapeutics 2003;305(3):1150-62.
2002: Juswinder Singh; Herman van Vlijmen; Yusheng Liao; Wen-Cherng Lee; Mark Cornebise; Mary Harris; I-hsiang Shu; Alan Gill; Julio H Cuervo; William W Abraham; Steven P Adams
Identification of potent and novel alpha4beta1 antagonists using in silico screening.
Journal of medicinal chemistry 2002;45(14):2988-93.
2001: Ling Ling Chen; Adrian Whitty; D Scott; Wen-Cherng Lee; Mark Cornebise; Steven P Adams; Russell C Petter; Roy R Lobb; R Blake Pepinsky
Evidence that ligand and metal ion binding to integrin alpha 4beta 1 are regulated through a coupled equilibrium.
The Journal of biological chemistry 2001;276(39):36520-9.
1999: K c Lin; H S Ateeq; S H Hsiung; L T Chong; C N Zimmerman; A Castro; Wen-Cherng Lee; C E Hammond; S Kalkunte; Ling Ling Chen; R Blake Pepinsky; Diane R Leone; Andrew G Sprague; William W Abraham; Alan Gill; Roy R Lobb; Steven P Adams
Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.
Journal of medicinal chemistry 1999;42(5):920-34.