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1.

Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11ß-HSD1.

Burns, David M; He, Chunhong; Li, Yun-Long; Zhuo, Jincong; Qian, Ding-Quan; Chen, Lihua; Jalluri, Ravi; Diamond, Sharon; Covington, Maryanne B; Li, Yanlong; Wynn, Richard; Scherle, Peggy; Yeleswaram, Swamy; Hollis, Gregory; Friedman, Steve; Metcalf, Brian; Yao, Wenqing.

Bioorg Med Chem Lett ; 73: 128884, 2022 10 01.

Article in English | MEDLINE | ID: mdl-35835377

2.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11ß-HSD1 using a scaffold-hopping approach.

Zhang, Colin; Xu, Meizhong; He, Chunhong; Zhuo, Jincong; Burns, David M; Qian, Ding-Quan; Lin, Qiyan; Li, Yun-Long; Chen, Lihua; Shi, Eric; Agrios, Costas; Weng, Linkai; Sharief, Vaqar; Jalluri, Ravi; Li, Yanlong; Scherle, Peggy; Diamond, Sharon; Hunter, Deborah; Covington, Maryanne; Marando, Cindy; Wynn, Richard; Katiyar, Kamna; Contel, Nancy; Vaddi, Kris; Yeleswaram, Swamy; Hollis, Gregory; Huber, Reid; Friedman, Steve; Metcalf, Brian; Yao, Wenqing.

Bioorg Med Chem Lett ; 69: 128782, 2022 08 01.

Article in English | MEDLINE | ID: mdl-35537608

3.

The Janus kinase 2 inhibitor fedratinib inhibits thiamine uptake: a putative mechanism for the onset of Wernicke's encephalopathy.

Zhang, Qiang; Zhang, Yan; Diamond, Sharon; Boer, Jason; Harris, Jennifer J; Li, Yu; Rupar, Mark; Behshad, Elham; Gardiner, Christine; Collier, Paul; Liu, Phillip; Burn, Timothy; Wynn, Richard; Hollis, Gregory; Yeleswaram, Swamy.

Drug Metab Dispos ; 42(10): 1656-62, 2014 Oct.

Article in English | MEDLINE | ID: mdl-25063672

4.

A frameshift variant in the melanophilin gene is associated with loss of pigment from shed skin in ball pythons ( Python regius ).

Lederer, Izabella; Shahid, Basmah; Dao, Uyen; Brogdon, Alex; Byrtus, Hannah; Delva, Marcelin; Deva, Orson; Hatfield, Paige; Hertz, Mikayla; Justice, Jenna; Mavor, Sarah; Pilbeam, Erin; Rice, Zoe; Simpson, Abbey; Temar, Hallie; Wynn, Richard; Xhangolli, Joana; Graves, Chiron; Seidel, Hannah.

MicroPubl Biol ; 20232023.

Article in English | MEDLINE | ID: mdl-37637270

5.

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

Liu, Xiangdong; Shin, Niu; Koblish, Holly K; Yang, Gengjie; Wang, Qian; Wang, Kathy; Leffet, Lynn; Hansbury, Michael J; Thomas, Beth; Rupar, Mark; Waeltz, Paul; Bowman, Kevin J; Polam, Padmaja; Sparks, Richard B; Yue, Eddy W; Li, Yanlong; Wynn, Richard; Fridman, Jordan S; Burn, Timothy C; Combs, Andrew P; Newton, Robert C; Scherle, Peggy A.

Blood ; 115(17): 3520-30, 2010 Apr 29.

Article in English | MEDLINE | ID: mdl-20197554

6.

Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor.

Koblish, Holly K; Wu, Liangxing; Wang, Liang-Chuan S; Liu, Phillip C C; Wynn, Richard; Rios-Doria, Jonathan; Spitz, Susan; Liu, Hao; Volgina, Alla; Zolotarjova, Nina; Kapilashrami, Kanishk; Behshad, Elham; Covington, Maryanne; Yang, Yan-Ou; Li, Jingwei; Diamond, Sharon; Soloviev, Maxim; O'Hayer, Kevin; Rubin, Stephen; Kanellopoulou, Chrysi; Yang, Gengjie; Rupar, Mark; DiMatteo, Darlise; Lin, Luping; Stevens, Christina; Zhang, Yue; Thekkat, Pramod; Geschwindt, Ryan; Marando, Cindy; Yeleswaram, Swamy; Jackson, Jeff; Scherle, Peggy; Huber, Reid; Yao, Wenqing; Hollis, Gregory.

Cancer Discov ; 12(6): 1482-1499, 2022 06 02.

Article in English | MEDLINE | ID: mdl-35254416

7.

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Wu, Liangxing; Zhang, Colin; He, Chunhong; Qian, Dingquan; Lu, Liang; Sun, Yaping; Xu, Meizhong; Zhuo, Jincong; Liu, Phillip C C; Klabe, Ronald; Wynn, Richard; Covington, Maryanne; Gallagher, Karen; Leffet, Lynn; Bowman, Kevin; Diamond, Sharon; Koblish, Holly; Zhang, Yue; Soloviev, Maxim; Hollis, Gregory; Burn, Timothy C; Scherle, Peggy; Yeleswaram, Swamy; Huber, Reid; Yao, Wenqing.

J Med Chem ; 64(15): 10666-10679, 2021 08 12.

Article in English | MEDLINE | ID: mdl-34269576

8.

Identification of pAKT as a pharmacodynamic marker for MER kinase in human melanoma G361 cells.

Chen, Yaoyu; Favata, Margaret; Pusey, Michelle; Li, Jun; Lo, Yvonne; Ye, Min; Wynn, Richard; Wang, Xiaozhao; Yao, Wenqing; Chen, Yingnan.

Biomark Res ; 8: 4, 2020.

Article in English | MEDLINE | ID: mdl-32042425

9.

A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity.

Rios-Doria, Jonathan; Favata, Margaret; Lasky, Kerri; Feldman, Patricia; Lo, Yvonne; Yang, Gengjie; Stevens, Christina; Wen, Xiaoming; Sehra, Sarita; Katiyar, Kamna; Liu, Ke; Wynn, Richard; Harris, Jennifer J; Ye, Min; Spitz, Susan; Wang, Xiaozhao; He, Chunhong; Li, Yun-Long; Yao, Wenqing; Covington, Maryanne; Scherle, Peggy; Koblish, Holly.

Front Oncol ; 10: 598477, 2020.

Article in English | MEDLINE | ID: mdl-33425754

10.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models.

Liu, Phillip C C; Koblish, Holly; Wu, Liangxing; Bowman, Kevin; Diamond, Sharon; DiMatteo, Darlise; Zhang, Yue; Hansbury, Michael; Rupar, Mark; Wen, Xiaoming; Collier, Paul; Feldman, Patricia; Klabe, Ronald; Burke, Krista A; Soloviev, Maxim; Gardiner, Christine; He, Xin; Volgina, Alla; Covington, Maryanne; Ruggeri, Bruce; Wynn, Richard; Burn, Timothy C; Scherle, Peggy; Yeleswaram, Swamy; Yao, Wenqing; Huber, Reid; Hollis, Gregory.

PLoS One ; 15(4): e0231877, 2020.

Article in English | MEDLINE | ID: mdl-32315352

11.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Burns, David M; Li, Yun-Long; Shi, Eric; He, Chunhong; Xu, Meizhong; Zhuo, Jincong; Zhang, Colin; Qian, Ding-Quan; Li, Yanlong; Wynn, Richard; Covington, Maryanne B; Katiyar, Kamna; Marando, Cindy A; Fridman, Jordan S; Scherle, Peggy; Friedman, Steve; Metcalf, Brian; Yao, Wenqing.

Bioorg Med Chem Lett ; 19(13): 3525-30, 2009 Jul 01.

Article in English | MEDLINE | ID: mdl-19457660

12.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Stubbs, Matthew C; Burn, Timothy C; Sparks, Richard; Maduskuie, Thomas; Diamond, Sharon; Rupar, Mark; Wen, Xiaoming; Volgina, Alla; Zolotarjova, Nina; Waeltz, Paul; Favata, Margaret; Jalluri, Ravi; Liu, Huiqing; Liu, Xuesong Mike; Li, Jun; Collins, Robert; Falahatpisheh, Nikoo; Polam, Padmaja; DiMatteo, Darlise; Feldman, Patricia; Dostalik, Valerie; Thekkat, Pramod; Gardiner, Christine; He, Xin; Li, Yanlong; Covington, Maryanne; Wynn, Richard; Ruggeri, Bruce; Yeleswaram, Swamy; Xue, Chu-Biao; Yao, Wenqing; Combs, Andrew P; Huber, Reid; Hollis, Gregory; Scherle, Peggy; Liu, Phillip C C.

Clin Cancer Res ; 25(1): 300-311, 2019 01 01.

Article in English | MEDLINE | ID: mdl-30206163

13.

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.

Douty, Brent; Wayland, Brian; Ala, Paul J; Bower, Michael J; Pruitt, James; Bostrom, Lori; Wei, Min; Klabe, Ronald; Gonneville, Lucie; Wynn, Richard; Burn, Timothy C; Liu, Phillip C C; Combs, Andrew P; Yue, Eddy W.

Bioorg Med Chem Lett ; 18(1): 66-71, 2008 Jan 01.

Article in English | MEDLINE | ID: mdl-18037290

14.

Azithromycin associated with a small increased risk of cardiovascular death: a review.

Wynn, Richard L.

Gen Dent ; 61(2): 8-9, 2013.

Article in English | MEDLINE | ID: mdl-23454312

15.

Diet drugs Belviq and Qsymia receive FDA approval: what dentists need to know.

Wynn, Richard L.

Gen Dent ; 61(1): 11-3, 2013.

Article in English | MEDLINE | ID: mdl-23302354

16.

Vitamin D deficiency and nonspecific musculoskeletal pain.

Wynn, Richard L.

Gen Dent ; 61(3): 10-3, 2013.

Article in English | MEDLINE | ID: mdl-23649566

17.

Binding Assays for Bromodomain Proteins: Their Utility in Drug Discovery in Oncology and Inflammatory Disease.

Zolotarjova, Nina I; Wynn, Richard.

Curr Protoc Pharmacol ; 80(1): 3.16.1-3.16.14, 2018 03.

Article in English | MEDLINE | ID: mdl-30040205

18.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.

Koblish, Holly; Li, Yun-Long; Shin, Niu; Hall, Leslie; Wang, Qian; Wang, Kathy; Covington, Maryanne; Marando, Cindy; Bowman, Kevin; Boer, Jason; Burke, Krista; Wynn, Richard; Margulis, Alex; Reuther, Gary W; Lambert, Que T; Dostalik Roman, Valerie; Zhang, Ke; Feng, Hao; Xue, Chu-Biao; Diamond, Sharon; Hollis, Greg; Yeleswaram, Swamy; Yao, Wenqing; Huber, Reid; Vaddi, Kris; Scherle, Peggy.

PLoS One ; 13(6): e0199108, 2018.

Article in English | MEDLINE | ID: mdl-29927999

19.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Yao, Wenqing; Zhuo, Jincong; Burns, David M; Xu, Meizhong; Zhang, Colin; Li, Yun-Long; Qian, Ding-Quan; He, Chunhong; Weng, Lingkai; Shi, Eric; Lin, Qiyan; Agrios, Costas; Burn, Timothy C; Caulder, Eian; Covington, Maryanne B; Fridman, Jordan S; Friedman, Steven; Katiyar, Kamna; Hollis, Gregory; Li, Yanlong; Liu, Changnian; Liu, Xiangdong; Marando, Cindy A; Newton, Robert; Pan, Max; Scherle, Peggy; Taylor, Nancy; Vaddi, Kris; Wasserman, Zelda R; Wynn, Richard; Yeleswaram, Swamy; Jalluri, Ravi; Bower, Michael; Zhou, Bing-Bing; Metcalf, Brian.

J Med Chem ; 50(4): 603-6, 2007 Feb 22.

Article in English | MEDLINE | ID: mdl-17256836

20.

High-throughput determination of mode of inhibition in lead identification and optimization.

Wei, Min; Wynn, Richard; Hollis, Gregory; Liao, Boshan; Margulis, Alexander; Reid, Brian G; Klabe, Ronald; Liu, Phillip C C; Becker-Pasha, Mary; Rupar, Mark; Burn, Timothy C; McCall, Dale E; Li, Yanlong.

J Biomol Screen ; 12(2): 220-8, 2007 Mar.

Article in English | MEDLINE | ID: mdl-17351185

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Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11ß-HSD1.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11ß-HSD1 using a scaffold-hopping approach.

The Janus kinase 2 inhibitor fedratinib inhibits thiamine uptake: a putative mechanism for the onset of Wernicke's encephalopathy.

A frameshift variant in the melanophilin gene is associated with loss of pigment from shed skin in ball pythons ( Python regius ).

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor.

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Identification of pAKT as a pharmacodynamic marker for MER kinase in human melanoma G361 cells.

A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.

Azithromycin associated with a small increased risk of cardiovascular death: a review.

Diet drugs Belviq and Qsymia receive FDA approval: what dentists need to know.

Vitamin D deficiency and nonspecific musculoskeletal pain.

Binding Assays for Bromodomain Proteins: Their Utility in Drug Discovery in Oncology and Inflammatory Disease.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

High-throughput determination of mode of inhibition in lead identification and optimization.