Search Results - "Skotnicki, Jerauld"

Biosynthesis of the immunosuppressants FK506, FK520, and rapamycin involves a previously undescribed family of enzymes acting on chorismate by Andexer, Jennifer N, Kendrew, Steven G, Nur-e-Alam, Mohammad, Lazos, Orestis, Foster, Teresa A, Zimmermann, Anna-Sophie, Warneck, Tony D, Suthar, Dipen, Coates, Nigel J, Koehn, Frank E, Skotnicki, Jerauld S, Carter, Guy T, Gregory, Matthew A, Martin, Christine J, Moss, Steven J, Leadlay, Peter F, Wilkinson, Barrie

“…The macrocyclic polyketides FK506, FK520, and rapamycin are potent immunosuppressants that prevent T-cell proliferation through initial binding to the…”
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Synthesis of rapamycin glycoconjugates via a CuAAC-based approach by Moni, Lisa, Marra, Alberto, Skotnicki, Jerauld S., Koehn, Frank E., Abou-Gharbia, Magid, Dondoni, Alessandro

“…The conversion of the C40 secondary hydroxyl group of rapamycin into the azido group was followed by copper catalyzed cycloaddition of the resulting…”
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Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated Mammalian Target of Rapamycin Pathway by CRABTREE, Judy S, JELINSKY, Scott A, DAVE, Bhuvanesh, BROADDUS, Russell R, BROWN, Eugene L, WENLING KAO, SKOTNICKI, Jerauld S, ABOU-GHARBIA, Magid, WINNEKER, Richard C, WALKER, Cheryl L, HARRIS, Heather A, CHOE, Sung E, COTREAU, Monette M, KIMBERLAND, Michelle L, WILSON, Ewa, SARAF, Kathryn A, WEI LIU, MCCAMPBELL, Adrienne S

“…Uterine leiomyomata, or fibroids, are benign tumors of the uterine myometrium that significantly affect up to 30% of reproductive-age women. Despite being the…”
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Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities by Ruan, Benfang, Pong, Kevin, Jow, Flora, Bowlby, Mark, Crozier, Robert A, Liu, Danni, Liang, Shi, Chen, Yi, Mercado, Mary Lynn, Feng, Xidong, Bennett, Frann, von Schack, David, McDonald, Leonard, Zaleska, Margaret M, Wood, Andrew, Reinhart, Peter H, Magolda, Ronald L, Skotnicki, Jerauld, Pangalos, Menelas N, Koehn, Frank E, Carter, Guy T, Abou-Gharbia, Magid, Graziani, Edmund I

“…Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target…”
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Recombinant strains for the enhanced production of bioengineered rapalogs by Kendrew, Steven G., Petkovic, Hrvoje, Gaisser, Sabine, Ready, Sarah J., Gregory, Matthew A., Coates, Nigel J., Nur-e-Alam, Mohammad, Warneck, Tony, Suthar, Dipen, Foster, Teresa A., McDonald, Leonard, Schlingman, Gerhard, Koehn, Frank E., Skotnicki, Jerauld S., Carter, Guy T., Moss, Steven J., Zhang, Ming-Qiang, Martin, Christine J., Sheridan, Rose M., Wilkinson, Barrie

“…The rapK gene required for biosynthesis of the DHCHC starter acid that initiates rapamycin biosynthesis was deleted from strain BIOT-3410, a derivative of…”
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Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis by Hu, Yonghan, Xiang, Jason S., DiGrandi, Martin J., Du, Xuemei, Ipek, Manus, Laakso, Leif M., Li, Jianchang, Li, Wei, Rush, Thomas S., Schmid, Jean, Skotnicki, Jerauld S., Tam, Steve, Thomason, Jennifer R., Wang, Qin, Levin, Jeremy I.

“…Modification of α-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and…”
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Synthesis and SAR of highly selective MMP-13 inhibitors by Li, Jianchang, Rush, Thomas S., Li, Wei, DeVincentis, Dianne, Du, Xuemei, Hu, Yonghan, Thomason, Jennifer R., Xiang, Jason S., Skotnicki, Jerauld S., Tam, Steve, Cunningham, Kristina M., Chockalingam, Priya S., Morris, Elisabeth A., Levin, Jeremy I.

“…The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1,…”
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PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors by Yu, Ker, Lucas, Judy, Zhu, Tianmin, Zask, Arie, Gaydos, Christine, Toral-Barza, Lourdes, Gu, Jianxin, Li, Fangbiao, Chaudhary, Inder, Cai, Ping, Lotvin, Jason, Petersen, Roseann, Ruppen, Mark, Fawzi, Mahdi, Ayral-Kaloustian, Semiramis, Skotnicki, Jerauld, Mansour, Tarek, Frost, Philip, Gibbons, James

“…Deregulated phosphatidylinositol 3-kinase (PI3K) signaling pathway is widely implicated in tumor growth and resistance to chemotherapy. While a strong…”
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3,4-Disubstituted benzofuran P1′ MMP-13 inhibitors: Optimization of selectivity and reduction of protein binding by Li, Wei, Hu, Yonghan, Li, Jianchang, Thomason, Jennifer R., DeVincentis, Dianne, Du, Xuemei, Wu, Junjun, Hotchandani, Rajeev, Rush, Thomas S., Skotnicki, Jerauld S., Tam, Steve, Chockalingam, Priya S., Morris, Elisabeth A., Levin, Jeremy I.

“…Potent and selective 3,4-disubstituted benzofuran P1′ MMP-13 inhibitors have been prepared with a substituent at the C4 position of the benzofuran P1′ moiety…”
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Synthesis and Structure−Activity Relationship of N-Substituted 4-Arylsulfonylpiperidine-4-hydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis by Aranapakam, Venkatesan, Davis, Jamie M, Grosu, George T, Baker, Ellingboe, John, Zask, Arie, Levin, Jeremy I, Sandanayaka, Vincent P, Du, Mila, Skotnicki, Jerauld S, DiJoseph, John F, Sung, Amy, Sharr, Michele A, Killar, Loran M, Walter, Thomas, Jin, Guixian, Cowling, Rebecca, Tillett, Jeff, Zhao, Weiguang, McDevitt, Joseph, Xu, Zhang Bao

“…The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue…”
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Synthesis and Structure−Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis by Aranapakam, Venkatesan, Grosu, George T, Davis, Jamie M, Hu, Baihua, Ellingboe, John, Baker, Jannie L, Skotnicki, Jerauld S, Zask, Arie, DiJoseph, John F, Sung, Amy, Sharr, Michele A, Killar, Loran M, Walter, Thomas, Jin, Guixian, Cowling, Rebecca

“…The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue…”
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Synthesis and Structure−Activity Relationships of 4-alkynyloxy Phenyl Sulfanyl, Sulfinyl, and Sulfonyl Alkyl Hydroxamates as Tumor Necrosis Factor-α Converting Enzyme and Matrix Metalloproteinase Inhibitors by Venkatesan, Aranapakam M, Davis, Jamie M, Grosu, George T, Baker, Jannie, Zask, Arie, Levin, Jeremy I, Ellingboe, John, Skotnicki, Jerauld S, DiJoseph, John F, Sung, Amy, Jin, Guixian, Xu, Weixin, McCarthy, Diane Joseph, Barone, Dauphine

“…A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized. Their structure−activity…”
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2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis by ZHONG LI, FRANCISCO, Gerardo D, SKOTNICKI, Jerauld S, MANSOUR, Tarek S, HU, William, LABTHAVIKUL, Pornpen, PETERSEN, Peter J, SEVERIN, Anatoly, SINGH, Guy, YOUJUN YANG, RASMUSSEN, Beth A, LIN, Yang-I

“…Twenty-five 2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives were synthesized for evaluation as new inhibitors of bacterial cell wall…”
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NMR Solution Structure of the Catalytic Fragment of Human Fibroblast Collagenase Complexed with a Sulfonamide Derivative of a Hydroxamic Acid Compound by Moy, Franklin J, Chanda, Pranab K, Chen, James M, Cosmi, Scott, Edris, Wade, Skotnicki, Jerauld S, Wilhelm, Jim, Powers, Robert

“…The solution structure of the catalytic fragment of human fibroblast collagenase (MMP-1) complexed with a sulfonamide derivative of a hydroxamic acid compound…”
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Benzodiazepine inhibitors of the MMPs and TACE by NELSON, Frances C, DELOS SANTOS, Efren, GUIXIAN JIN, ROTH, Catherine E, ALBRIGHT, J. Donald, LEVIN, Jeremy I, CHEN, James M, SKOTNICKI, Jerauld S, DIJOSEPH, John F, SHARR, Michele A, SUNG, Amy, KILLAR, Loran M, COWLING, Rebecca

“…A series of benzodiazepine inhibitors of the MMPs and TACE has been developed. These compounds display an interesting selectivity profile and should be useful…”
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Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases by LEVIN, Jeremy I, YANSONG GU, COSMI, Scott, HSIAO, Chu-Lai, EDRIS, Wade, WILHELM, James, KILLAR, Loran M, SKOTNICKI, Jerauld S, NELSON, Frances C, ZASK, Arie, DIJOSEPH, John F, SHARR, Michele A, SUNG, Amy, GUIXIAN JIN, COWLING, Rebecca, CHANDA, Pranab

“…Heteroaryl and cycloalkyl sulfonamide-hydroxamic acid MMP inhibitors were investigated. Of these, the pyridyl analogue 2 is the most potent and selective…”
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The synthesis and biological activity of a novel series of diazepine MMP inhibitors by Levin, Jeremy I., DiJoseph, John F., Killar, Loran M., Sung, Amy, Walter, Thomas, Sharr, Michele A., Roth, Catherine E., Skotnicki, Jerauld S., Albright, J.Donald

“…A novel series of diazepine-based hydroxamic acid inhibitors of MMP-1, MMP-9, and MMP-13 were prepared and evaluated both in vitro and in vivo. A novel series…”
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Design strategies for the identification of MMP-13 and Tace inhibitors by Skotnicki, Jerauld S, DiGrandi, Martin J, Levin, Jeremy I

“…Inhibitors of matrix metalloprotease (MMP)-13 and tumor necrosis factor-alpha converting enzyme (TACE) have been highly sought as potential therapeutic agents…”
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Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: A class of potent aggrecanase-1 inhibitors by Hopper, Darrin W., Vera, Matthew D., How, David, Sabatini, Joshua, Xiang, Jason S., Ipek, Manus, Thomason, Jennifer, Hu, Yonghan, Feyfant, Eric, Wang, Qin, Georgiadis, Katy E., Reifenberg, Erica, Sheldon, Richard T., Keohan, Cristin C., Majumdar, Manas K., Morris, Elisabeth A., Skotnicki, Jerauld, Sum, Phaik-Eng

“…A subset of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides were identified as potent Agg-1, MMP-2 and MMP-13 inhibitors through the synthesis of a series of…”
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Pegylated Wortmannin and 17-Hydroxywortmannin Conjugates as Phosphoinositide 3-Kinase Inhibitors Active in Human Tumor Xenograft Models by Zhu, Tianmin, Gu, Jianxin, Yu, Ker, Lucas, Judy, Cai, Ping, Tsao, Russ, Gong, Yumin, Li, Fangbiao, Chaudhary, Inder, Desai, Parimal, Ruppen, Mark, Fawzi, Mahdi, Gibbons, James, Ayral-Kaloustian, Semiramis, Skotnicki, Jerauld, Mansour, Tarek, Zask, Arie

“…Phosphoinositide 3-kinase (PI3K) is an important target for cancer chemotherapy due to the deregulation of its signaling pathway in a wide spectrum of human…”
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