Search Results - "Liclican, Albert"

Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition by Liclican, Albert, Serafini, Loredana, Xing, Weimei, Czerwieniec, Gregg, Steiner, Bart, Wang, Ting, Brendza, Katherine M., Lutz, Justin D., Keegan, Kathleen S., Ray, Adrian S., Schultz, Brian E., Sakowicz, Roman, Feng, Joy Y.

“…Bruton's tyrosine kinase (BTK) is a key component of the B-cell receptor (BCR) pathway and a clinically validated target for small molecule inhibitors such as…”
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Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells by Li, Ruidong, Liclican, Albert, Xu, Yili, Pitts, Jared, Niu, Congrong, Zhang, Jingyu, Kim, Cynthia, Zhao, Xiaofeng, Soohoo, Daniel, Babusis, Darius, Yue, Qin, Ma, Bin, Murray, Bernard P, Subramanian, Raju, Xie, Xuping, Zou, Jing, Bilello, John P, Li, Li, Schultz, Brian E, Sakowicz, Roman, Smith, Bill J, Shi, Pei-Yong, Murakami, Eisuke, Feng, Joy Y

“…Remdesivir (RDV; GS-5734, Veklury), the first FDA-approved antiviral to treat COVID-19, is a single-diastereomer monophosphoramidate prodrug of an adenosine…”
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Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A by Steadman, Victoria A, Pettit, Simon B, Poullennec, Karine G, Lazarides, Linos, Keats, Andrew J, Dean, David K, Stanway, Steven J, Austin, Carol A, Sanvoisin, Jonathan A, Watt, Gregory M, Fliri, Hans G, Liclican, Albert C, Jin, Debi, Wong, Melanie H, Leavitt, Stephanie A, Lee, Yu-Jen, Tian, Yang, Frey, Christian R, Appleby, Todd C, Schmitz, Uli, Jansa, Petr, Mackman, Richard L, Schultz, Brian E

“…Cyclophilin inhibition has been a target for the treatment of hepatitis C and other diseases, but the generation of potent, drug-like molecules through…”
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RNase H Active Site Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase: Design, Biochemical Activity, and Structural Information by Kirschberg, Thorsten A, Balakrishnan, Mini, Squires, Neil H, Barnes, Tiffany, Brendza, Katherine M, Chen, Xiaowu, Eisenberg, Eugene J, Jin, Weili, Kutty, Nilima, Leavitt, Stephanie, Liclican, Albert, Liu, Qi, Liu, Xiaohong, Mak, John, Perry, Jason K, Wang, Michael, Watkins, William J, Lansdon, Eric B

“…Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H…”
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Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase—Structure–activity relationships and crystallographic analysis by Kirschberg, Thorsten A., Balakrishnan, Mini, Huang, Wei, Hluhanich, Rebecca, Kutty, Nilima, Liclican, Albert C., McColl, Damian J., Squires, Neil H., Lansdon, Eric B.

“…A series of 3,4,5-trisubstituted 1,2,4-4 H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure…”
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A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model by Yant, Stephen R., Mulato, Andrew, Hansen, Derek, Tse, Winston C., Niedziela-Majka, Anita, Zhang, Jennifer R., Stepan, George J., Jin, Debi, Wong, Melanie H., Perreira, Jill M., Singer, Eric, Papalia, Giuseppe A., Hu, Eric Y., Zheng, Jim, Lu, Bing, Schroeder, Scott D., Chou, Kevin, Ahmadyar, Shekeba, Liclican, Albert, Yu, Helen, Novikov, Nikolai, Paoli, Eric, Gonik, Daniel, Ram, Renee R., Hung, Magdeleine, McDougall, William M., Brass, Abraham L., Sundquist, Wesley I., Cihlar, Tomas, Link, John O.

“…People living with HIV (PLWH) have expressed concern about the life-long burden and stigma associated with taking pills daily and can experience medication…”
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Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ by Somoza, John R., Koditek, David, Villaseñor, Armando G., Novikov, Nikolai, Wong, Melanie H., Liclican, Albert, Xing, Weimei, Lagpacan, Leanna, Wang, Ruth, Schultz, Brian E., Papalia, Giuseppe A., Samuel, Dharmaraj, Lad, Latesh, McGrath, Mary E.

“…Idelalisib (also known as GS-1101, CAL-101, IC489666, and Zydelig) is a PI3Kδ inhibitor that has recently been approved for the treatment of several…”
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Biochemical characterization and structure determination of a potent, selective antibody inhibitor of human MMP9 by Appleby, Todd C., Greenstein, Andrew E., Hung, Magdeleine, Liclican, Albert, Velasquez, Maile, Villaseñor, Armando G., Wang, Ruth, Wong, Melanie H., Liu, Xiaohong, Papalia, Giuseppe A., Schultz, Brian E., Sakowicz, Roman, Smith, Victoria, Kwon, Hyock Joo

“…Matrix metalloproteinase 9 (MMP9) is a member of a large family of proteases that are secreted as inactive zymogens. It is a key regulator of the extracellular…”
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Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability by Mulato, Andrew, Lansdon, Eric, Aoyama, Ron, Voigt, Johannes, Lee, Michael, Liclican, Albert, Lee, Gary, Singer, Eric, Stafford, Brian, Gong, Ruoyu, Murray, Bernard, Chan, Julie, Lee, Johnny, Xu, Yili, Ahmadyar, Shekeba, Gonzalez, Ana, Cho, Aesop, Stepan, George J, Schmitz, Uli, Schultz, Brian, Marchand, Bruno, Brumshtein, Boris, Wang, Ruth, Yu, Helen, Cihlar, Tomas, Xu, Lianhong, Yant, Stephen R

“…Protease inhibitors (PIs) remain an important component of antiretroviral therapy for the treatment of HIV-1 infection due to their high genetic barrier to…”
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Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle by Mackman, Richard L, Steadman, Victoria A, Dean, David K, Jansa, Petr, Poullennec, Karine G, Appleby, Todd, Austin, Carol, Blakemore, Caroline A, Cai, Ruby, Cannizzaro, Carina, Chin, Gregory, Chiva, Jean-Yves C, Dunbar, Neil A, Fliri, Hans, Highton, Adrian J, Hui, Hon, Ji, Mingzhe, Jin, Haolun, Karki, Kapil, Keats, Andrew J, Lazarides, Linos, Lee, Yu-Jen, Liclican, Albert, Mish, Michael, Murray, Bernard, Pettit, Simon B, Pyun, Peter, Sangi, Michael, Santos, Rex, Sanvoisin, Jonathan, Schmitz, Uli, Schrier, Adam, Siegel, Dustin, Sperandio, David, Stepan, George, Tian, Yang, Watt, Gregory M, Yang, Hai, Schultz, Brian E

“…Cyclophilins are a family of peptidyl-prolyl isomerases that are implicated in a wide range of diseases including hepatitis C. Our aim was to discover through…”
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Biochemical Characterization of GS-4059 As a Potent and Selective Covalent Irreversible Inhibitor of Bruton's Tyrosine Kinase by Liclican, Albert, Xing, Weimei, Serafini, Loredana, Wang, Ting, Brendza, Kathy, Lutz, Justin, Ray, Adrian S., Schultz, Brian, Sakowicz, Roman, Feng, Joy Y.

“…Introduction:Bruton's tyrosine kinase (BTK) plays a crucial role in B-cell development, differentiation, and signaling in the B-cell receptor (BCR) signaling…”
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Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors by Mavunkel, Babu J., Perumattam, John J., Tan, Xuefei, Luedtke, Gregory R., Lu, Qing, Lim, Don, Kizer, Darin, Dugar, Sundeep, Chakravarty, Sarvajit, Xu, Yong-jin, Jung, Joon, Liclican, Albert, Levy, Daniel E., Tabora, Jocelyn

“…A new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine substituted heterocycles is described. Optimal features include a piperidine and an…”
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Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles by Tan, Xuefei, Tester, Richland W., Luedtke, Gregory R., Chakravarty, Sarvajit, Mavunkel, Babu J., Perumattam, John J., Lu, Qing, Nashashibi, Imad, Jung, Joon, Hu, Jie, Liclican, Albert, Almirez, Ramona, Tabora, Jocelyn, Tran, Vinh, Laney, Maureen, Levy, Daniel E., Dugar, Sundeep

“…SAR studies of the p38α MAP kinase inhibitor SCIO-469 focused on maintaining activity while improving pharmacokinetic properties. Advantages were noted for…”
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Amide-based inhibitors of p38α MAP kinase. Part 2: Design, synthesis and SAR of potent N-pyrimidyl amides by Tester, Richland, Tan, Xuefei, Luedtke, Gregory R., Nashashibi, Imad, Schinzel, Kurt, Liang, Weiling, Jung, Joon, Dugar, Sundeep, Liclican, Albert, Tabora, Jocelyn, Levy, Daniel E., Do, Steven

“…Identification and optimization of a new class of N-pyrimidyl amide based p38α MAP kinase inhibitors is described. The lead structure was derived from a…”
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Amide-based inhibitors of p38a MAP kinase. Part 2: Design, synthesis and SAR of potent N-pyrimidyl amides by Tester, Richland, Tan, Xuefei, Luedtke, Gregory R, Nashashibi, Imad, Schinzel, Kurt, Liang, Weiling, Jung, Joon, Dugar, Sundeep, Liclican, Albert, Tabora, Jocelyn, Levy, Daniel E, Do, Steven

“…Optimization of a tri-substituted N-pyridyl amide led to the discovery of a new class of potent N-pyrimidyl amide based p38a MAP kinase inhibitors. Initial SAR…”
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Design and synthesis of piperazine-indole p38a MAP kinase inhibitors with improved pharmacokinetic profiles by Tan, Xuefei, Tester, Richland W, Luedtke, Gregory R, Chakravarty, Sarvajit, Mavunkel, Babu J, Perumattam, John J, Lu, Qing, Nashashibi, Imad, Jung, Joon, Hu, Jie, Liclican, Albert, Almirez, Ramona, Tabora, Jocelyn, Tran, Vinh, Laney, Maureen, Levy, Daniel E, Dugar, Sundeep

“…Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38a MAP kinase inhibitors are described. Biological evaluation of these compounds focused…”
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Piperidine-based heterocyclic oxalyl amides as potent p38a MAP kinase inhibitors by Mavunkel, Babu J, Perumattam, John J, Tan, Xuefei, Luedtke, Gregory R, Lu, Qing, Lim, Don, Kizer, Darin, Dugar, Sundeep, Chakravarty, Sarvajit, Xu, Yong-Jin, Jung, Joon, Liclican, Albert, Levy, Daniel E, Tabora, Jocelyn

“…The design and synthesis of a new class of p38a MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these…”
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Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region by Levy, Daniel E., Wang, Dan-Xiong, Lu, Qing, Chen, Zheng, Perumattam, John, Xu, Yong-jin, Liclican, Albert, Higaki, Jeffrey, Dong, Hanmin, Laney, Maureen, Mavunkel, Babu, Dugar, Sundeep

“…Aryl-substituted maleimides were prepared and studied for their activity against CaMKIIδ. Inhibitory activities ranged from 34 nM to >20 μM. Key predicted…”
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Pyrimidine-based inhibitors of CaMKIIδ by Mavunkel, Babu, Xu, Yong-jin, Goyal, Bindu, Lim, Don, Lu, Qing, Chen, Zheng, Wang, Dan-Xiong, Higaki, Jeffrey, Chakraborty, Indrani, Liclican, Albert, Sideris, Steve, Laney, Maureen, Delling, Ulrike, Catalano, Rosanne, Higgins, Linda S., Wang, Hui, Wang, Jing, Feng, Ying, Dugar, Sundeep, Levy, Daniel E.

“…Pyrimidine-based inhibitors of CaMKIIδ were identified. Through computational studies, a probable binding mode was identified leading to the design of ATP…”
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Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 2: SAR of the amine tether by Levy, Daniel E., Wang, Dan-Xiong, Lu, Qing, Chen, Zheng, Perumattam, John, Xu, Yong-jin, Higaki, Jeffrey, Dong, Hanmin, Liclican, Albert, Laney, Maureen, Mavunkel, Babu, Dugar, Sundeep

“…Aryl-substituted maleimides were prepared and studied for their activity against CaMKIIδ. Inhibitory activities ranged from 34 nM to >20 μM. Key predicted…”
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