Search Results - "PARIKH, Mihir D"

Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes by Hett, Erik C, Xu, Hua, Geoghegan, Kieran F, Gopalsamy, Ariamala, Kyne, Robert E, Menard, Carol A, Narayanan, Arjun, Parikh, Mihir D, Liu, Shenping, Roberts, Lee, Robinson, Ralph P, Tones, Michael A, Jones, Lyn H

“…This work describes the first rational targeting of tyrosine residues in a protein binding site by small-molecule covalent probes. Specific tyrosine residues…”
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Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors by Han, Seungil, Czerwinski, Robert M, Caspers, Nicole L, Limburg, David C, Ding, WeiDong, Wang, Hong, Ohren, Jeffrey F, Rajamohan, Francis, McLellan, Thomas J, Unwalla, Ray, Choi, Chulho, Parikh, Mihir D, Seth, Nilufer, Edmonds, Jason, Phillips, Chris, Shakya, Subarna, Li, Xin, Spaulding, Vikki, Hughes, Samantha, Cook, Andrew, Robinson, Colin, Mathias, John P, Navratilova, Iva, Medley, Quintus G, Anderson, David R, Kurumbail, Ravi G, Aulabaugh, Ann

“…ITK (interleukin-2-inducible T-cell kinase) is a critical component of signal transduction in T-cells and has a well-validated role in their proliferation,…”
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A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS by Xu, Hua, Hett, Erik C, Gopalsamy, Ariamala, Parikh, Mihir D, Geoghegan, Kieran F, Kyne, Jr, Robert E, Menard, Carol A, Narayanan, Arjun, Robinson, Ralph P, Johnson, Douglas S, Tones, Michael A, Jones, Lyn H

“…Despite its diverse applications, such as identification of the protein binding partners of small molecules and investigation of intracellular drug-target…”
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases by Vazquez, Michael L, Kaila, Neelu, Strohbach, Joseph W, Trzupek, John D, Brown, Matthew F, Flanagan, Mark E, Mitton-Fry, Mark J, Johnson, Timothy A, TenBrink, Ruth E, Arnold, Eric P, Basak, Arindrajit, Heasley, Steven E, Kwon, Soojin, Langille, Jonathan, Parikh, Mihir D, Griffin, Sarah H, Casavant, Jeffrey M, Duclos, Brian A, Fenwick, Ashley E, Harris, Thomas M, Han, Seungil, Caspers, Nicole, Dowty, Martin E, Yang, Xin, Banker, Mary Ellen, Hegen, Martin, Symanowicz, Peter T, Li, Li, Wang, Lu, Lin, Tsung H, Jussif, Jason, Clark, James D, Telliez, Jean-Baptiste, Robinson, Ralph P, Unwalla, Ray

“…Janus kinases (JAKs) are intracellular tyrosine kinases that mediate the signaling of numerous cytokines and growth factors involved in the regulation of…”
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Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase by Taylor, Alexandria P, Swewczyk, Magdalena, Kennedy, Steven, Trush, Viacheslav V, Wu, Hong, Zeng, Hong, Dong, Aiping, Ferreira de Freitas, Renato, Tatlock, John, Kumpf, Robert A, Wythes, Martin, Casimiro-Garcia, Agustin, Denny, Rajiah Aldrin, Parikh, Mihir D, Li, Fengling, Barsyte-Lovejoy, Dalia, Schapira, Matthieu, Vedadi, Masoud, Brown, Peter J, Arrowsmith, Cheryl H, Owen, Dafydd R

“…The first chemical probe to primarily occupy the co-factor binding site of a Su­(var)­3−9, enhancer of a zeste, trithorax (SET) domain containing protein…”
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Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis by Fadeyi, Olugbeminiyi, Parikh, Mihir D., Chen, Ming Z., Kyne Jr, Robert E., Taylor, Alexandria P., O'Doherty, Inish, Kaiser, Stephen E., Barbas, Sabrina, Niessen, Sherry, Shi, Manli, Weinrich, Scott L., Kath, John C., Jones, Lyn H., Robinson, Ralph P.

“…Sulfonyl fluoride (SF)‐based activity probes have become important tools in chemical biology. Herein, exploiting the relative chemical stability of SF to carry…”
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Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA) by Gopalsamy, Ariamala, Narayanan, Arjun, Liu, Shenping, Parikh, Mihir D, Kyne, Robert E, Fadeyi, Olugbeminiyi, Tones, Michael A, Cherry, Jonathan J, Nabhan, Joseph F, LaRosa, Gregory, Petersen, Donna N, Menard, Carol, Foley, Timothy L, Noell, Stephen, Ren, Yong, Loria, Paula M, Maglich-Goodwin, Jodi, Rong, Haojing, Jones, Lyn H

“…The C-5 substituted 2,4-diaminoquinazoline RG3039 (compound 1), a member of a chemical series that was identified and optimized using an SMN2 promoter screen,…”
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Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning by Schnute, Mark E, Benoit, Stephen E, Buchler, Ingrid P, Caspers, Nicole, Grapperhaus, Margaret L, Han, Seungil, Hotchandani, Rajeev, Huang, Nelson, Hughes, Robert O, Juba, Brian M, Kim, Kyung-Hee, Liu, Erica, McCarthy, Erin, Messing, Dean, Miyashiro, Joy S, Mohan, Shashi, O’Connell, Thomas N, Ohren, Jeffrey F, Parikh, Mihir D, Schmidt, Michelle, Selness, Shaun R, Springer, John R, Thanabal, Venkataraman, Trujillo, John I, Walker, Daniel P, Wan, Zhao-Kui, Withka, Jane M, Wittwer, Arthur J, Wood, Nancy L, Xing, Li, Zapf, Christoph W, Douhan, John

“…Potent covalent inhibitors of Bruton’s tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based…”
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Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency by Anderson, David R., Meyers, Marvin J., Kurumbail, Ravi G., Caspers, Nicole, Poda, Gennadiy I., Long, Scott A., Pierce, Betsy S., Mahoney, Matthew W., Mourey, Robert J., Parikh, Mihir D.

“…Improvements in cell potency and selectivity of a new class of MK2 inhibitors are discussed. Optimization of kinase selectivity for a set of benzothiophene MK2…”
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Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode by Meyers, Marvin J., Pelc, Matthew, Kamtekar, Satwik, Day, Jacqueline, Poda, Gennadiy I., Hall, Molly K., Michener, Marshall L., Reitz, Beverly A., Mathis, Karl J., Pierce, Betsy S., Parikh, Mihir D., Mischke, Deborah A., Long, Scott A., Parlow, John J., Anderson, David R., Thorarensen, Atli

“…The work described herein demonstrates the utility of structure-based drug design (SBDD) in shifting the binding mode of an HTS hit from a DFG-in to a DFG-out…”
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Biochemical, cellular, and anti-inflammatory properties of a potent, selective, orally bioavailable benzamide inhibitor of Rho kinase activity by Rajagopalan, Lakshman E, Davies, Michael S, Kahn, Larry E, Kornmeier, Christine M, Shimada, Hideaki, Steiner, Toni A, Zweifel, Ben S, Wendling, Jay M, Payne, Maria A, Loeffler, Richard F, Case, Brenda L, Norton, Monica B, Parikh, Mihir D, Nemirovskiy, Olga V, Mourey, Robert J, Masferrer, Jaime L, Misko, Thomas P, Kolodziej, Stephen A

“…Rho kinase, is the most widely studied downstream effector of the small Rho GTPase RhoA. Two Rho kinase isoforms have been described and are frequently…”
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Discovery of + (2 -{4 -[2 -(5,6,7,8 -tetrahydro -1,8 -naphthyridin -2-yl )ethoxy ]phenyl} -cyclopropyl )acetic acid as potent and selective αvβ3 inhibitor : Design, synthesis, and optimization by NAGARAJAN, Srinivasan R, LU, Hwang-Fun, KEENE, Jeffery L, DUFFIN, Tiffany, ENGLEMAN, V. Wayne, FINN, Mary B, FREEMAN, Sandra K, KLOVER, Jon A, NICKOLS, G. Alan, NICKOLS, Maureen A, SHANNON, Kristen E, STEININGER, Christina A, GASIECKI, Alan F, WESTLIN, William F, WESTLIN, Marisa M, WILLIAMS, Melanie L, KHANNA, Ish K, PARIKH, Mihir D, DESAI, Bipinchandra N, ROGERS, Thomas E, CLARE, Michael, CHEN, Barbara B, RUSSELL, Mark A

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Demonstration of a Multikilogram-Scale Birch Reduction and Evaluation of Alternative Synthetic Routes to a Ketalized Cyclohexene Derivative by Goetz, Adam E., Arcari, Joel, Bagley, Scott W., Hicklin, Robert, Jin, Liangxue, Jin, Zuxi, Li, Xinnan, Liu, Zhiqing, McWilliams, J. Christopher, Parikh, Mihir D., Potter, Tyler, Smith, William J., Sun, Lijie, Trujillo, John, Wang, Pan, Zhao, Xin

“…We report the successful manufacture of several >50 kg batches of a key intermediate via a Birch reduction that utilized liquified ammonia as well as lithium…”
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PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease by Gopalsamy, Ariamala, Aulabaugh, Ann E, Barakat, Amey, Beaumont, Kevin C, Cabral, Shawn, Canterbury, Daniel P, Casimiro-Garcia, Agustin, Chang, Jeanne S, Chen, Ming Z, Choi, Chulho, Dow, Robert L, Fadeyi, Olugbeminiyi O, Feng, Xidong, France, Scott P, Howard, Roger M, Janz, Jay M, Jasti, Jayasankar, Jasuja, Reema, Jones, Lyn H, King-Ahmad, Amanda, Knee, Kelly M, Kohrt, Jeffrey T, Limberakis, Chris, Liras, Spiros, Martinez, Carlos A, McClure, Kim F, Narayanan, Arjun, Narula, Jatin, Novak, Jonathan J, O'Connell, Thomas N, Parikh, Mihir D, Piotrowski, David W, Plotnikova, Olga, Robinson, Ralph P, Sahasrabudhe, Parag V, Sharma, Raman, Thuma, Benjamin A, Vasa, Dipy, Wei, Liuqing, Wenzel, A Zane, Withka, Jane M, Xiao, Jun, Yayla, Hatice G

“…Sickle cell disease (SCD) is a genetic disorder caused by a single point mutation (β6 Glu → Val) on the β-chain of adult hemoglobin (HbA) that results in…”
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Porphyrins with exocyclic rings. Part 19: Efficient syntheses of phenanthrolinoporphyrins by Lash, Timothy D., Lin, Yanning, Novak, Bennett H., Parikh, Mihir D.

“…5-Nitro-1,10-phenanthrolines react with isocyanoacetate esters in the presence of DBU in THF to give excellent yields of the corresponding…”
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Claudin-18 deficiency is associated with airway epithelial barrier dysfunction and asthma by Sweerus, Kelly, MD, Lachowicz-Scroggins, Marrah, PhD, Gordon, Erin, MD, LaFemina, Michael, MD, Huang, Xiaozhu, MD, Parikh, Mihir, MD, Kanegai, Cindy, MD, Fahy, John V., MD, Frank, James A., MD

“…Background Epithelial barrier dysfunction and increased permeability may contribute to antigen sensitization and disease progression in asthma. Claudin-18.1 is…”
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Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization by Nagarajan, Srinivasan R, Lu, Hwang-Fun, Gasiecki, Alan F, Khanna, Ish K, Parikh, Mihir D, Desai, Bipinchandra N, Rogers, Thomas E, Clare, Michael, Chen, Barbara B, Russell, Mark A, Keene, Jeffery L, Duffin, Tiffany, Engleman, V Wayne, Finn, Mary B, Freeman, Sandra K, Klover, Jon A, Nickols, G Alan, Nickols, Maureen A, Shannon, Kristen E, Steininger, Christina A, Westlin, William F, Westlin, Marisa M, Williams, Melanie L

“…The integrin alpha(v)beta(3) is expressed in a number of cell types and is thought to play a major role in several pathological conditions. Various small…”
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Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective α vβ 3 inhibitor: Design, synthesis, and optimization by Nagarajan, Srinivasan R., Lu, Hwang-Fun, Gasiecki, Alan F., Khanna, Ish K., Parikh, Mihir D., Desai, Bipinchandra N., Rogers, Thomas E., Clare, Michael, Chen, Barbara B., Russell, Mark A., Keene, Jeffery L., Duffin, Tiffany, Engleman, V. Wayne, Finn, Mary B., Freeman, Sandra K., Klover, Jon A., Nickols, G. Alan, Nickols, Maureen A., Shannon, Kristen E., Steininger, Christina A., Westlin, William F., Westlin, Marisa M., Williams, Melanie L.

“…The tripeptide RGD a common binding motif in several ligands that bind to α vβ 3, has been depeptidized and optimized in our efforts toward discovering a small…”
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