Search Results - "SKOTNICKI, Jerauld S"

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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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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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 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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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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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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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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A convenient synthesis of 1-benzhydryl-N-arylsulfonyl-3-oxo-1,2-diazetidine-2-carboxamides by Skotnicki, J S

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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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Synthesis and biological evaluation of a 4-fluoromethyl monobactam analog by Skotnicki, J S, Commons, T J, Rees, R W, Speth, J L

“…The synthesis and in vitro antibacterial activity of (+/-)(cis)-3-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-…”
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Prostaglandins and congeners. 22. Synthesis of 11-substituted derivatives of 11-deoxyprostaglandins E1 and E2. Potential bronchodilators by Floyd, M. Brawner, Schaub, Robert E, Siuta, Gerald J, Skotnicki, Jerauld S, Grudzinskas, Charles V, Weiss, Martin J, Dessy, Franz, VanHumbeeck, L

“…The interesting bronchodilator activity of l-11-deoxy-11 alpha-[(2-hydroxyethyl)thio]prostaglandin E2 methyl ester (3a) is described. The preparation of 3a and…”
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Prostaglandins and congeners. 14. Synthesis and bronchodilator activity of dl-16,16-trimethyleneprostaglandins by Skotnicki, Jerauld S, Schaub, Robert E, Weiss, Martin J, Dessy, F

“…The interesting bronchodilator activity of novel dl-16,16-trimethyleneprostaglandin congeners and their preparation via the conjugate addition of the…”
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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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