Search Results - "Kalin, Jay"

Development and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors by Kalin, Jay H, Bergman, Joel A

“…This Perspective provides an in depth look at the numerous disease states in which histone deacetylase 6 (HDAC6) has been implicated. The physiological…”
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Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A by Butler, Kyle V, Kalin, Jay, Brochier, Camille, Vistoli, Guilio, Langley, Brett, Kozikowski, Alan P

“…Structure-based drug design combined with homology modeling techniques were used to develop potent inhibitors of HDAC6 that display superior selectivity for…”
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Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors by Kalin, Jay H., Wu, Muzhou, Gomez, Andrea V., Song, Yun, Das, Jayanta, Hayward, Dawn, Adejola, Nkosi, Wu, Mingxuan, Panova, Izabela, Chung, Hye Jin, Kim, Edward, Roberts, Holly J., Roberts, Justin M., Prusevich, Polina, Jeliazkov, Jeliazko R., Roy Burman, Shourya S., Fairall, Louise, Milano, Charles, Eroglu, Abdulkerim, Proby, Charlotte M., Dinkova-Kostova, Albena T., Hancock, Wayne W., Gray, Jeffrey J., Bradner, James E., Valente, Sergio, Mai, Antonello, Anders, Nicole M., Rudek, Michelle A., Hu, Yong, Ryu, Byungwoo, Schwabe, John W. R., Mattevi, Andrea, Alani, Rhoda M., Cole, Philip A.

“…Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 inhibitor (tranylcypromine analog). Enzymologic…”
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Re-programing Chromatin with a Bifunctional LSD1/HDAC Inhibitor Induces Therapeutic Differentiation in DIPG by Anastas, Jamie N., Zee, Barry M., Kalin, Jay H., Kim, Mirhee, Guo, Robyn, Alexandrescu, Sanda, Blanco, Mario Andres, Giera, Stefanie, Gillespie, Shawn M., Das, Jayanta, Wu, Muzhou, Nocco, Sarah, Bonal, Dennis M., Nguyen, Quang-De, Suva, Mario L., Bernstein, Bradley E., Alani, Rhoda, Golub, Todd R., Cole, Philip A., Filbin, Mariella G., Shi, Yang

“…H3K27M mutations resulting in epigenetic dysfunction are frequently observed in diffuse intrinsic pontine glioma (DIPGs), an incurable pediatric cancer. We…”
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Development and characterization of rabbit monoclonal antibodies that recognize human spermine oxidase and application to immunohistochemistry of human cancer tissues by Tepper, Armand W J W, Chu, Gerald, Klaren, Vincent N A, Kalin, Jay H, Molina-Ortiz, Patricia, Impagliazzo, Antonietta

“…The enzyme spermine oxidase (SMOX) is involved in polyamine catabolism and converts spermine to spermidine. The enzymatic reaction generates reactive hydrogen…”
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Inhibiting the coregulator CoREST impairs Foxp3+ Treg function and promotes antitumor immunity by Xiong, Yan, Wang, Liqing, Di Giorgio, Eros, Akimova, Tatiana, Beier, Ulf H, Han, Rongxiang, Trevisanut, Matteo, Kalin, Jay H, Cole, Philip A, Hancock, Wayne W

“…Foxp3+ Tregs are key to immune homeostasis, but the contributions of various large, multiprotein complexes that regulate gene expression remain unexplored. We…”
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Site-Specific Protein Labeling with N‑Hydroxysuccinimide-Esters and the Analysis of Ubiquitin Ligase Mechanisms by Dempsey, Daniel R, Jiang, Hanjie, Kalin, Jay H, Chen, Zan, Cole, Philip A

“…N-Hydroxysuccinimide (NHS)-esters are widely used to label proteins nonselectively on free amino groups. Such broad labeling can be disadvantageous because it…”
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Inhibition of the CoREST Repressor Complex Promotes Wound Re-Epithelialization through the Regulation of Keratinocyte Migration by Kida, Maki, Fatima, Iqra, Rozhkova, Elena, Otero-Viñas, Marta, Wu, Muzhou, Kalin, Jay H, Cole, Philip A, Falanga, Vincent, Alani, Rhoda M, Sharov, Andrey A

“…Wound healing is a complex process involving phases of hemostasis, inflammation, proliferation, and remodeling. The regenerative process in the skin requires…”
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The CoREST repressor complex mediates phenotype switching and therapy resistance in melanoma by Wu, Muzhou, Hanly, Ailish, Gibson, Frederick, Fisher, Robert, Rogers, Samantha, Park, Kihyun, Zuger, Angelina, Kuang, Kevin, Kalin, Jay H, Nocco, Sarah, Cole, Matthew, Xiao, Amy, Agus, Filisia, Labadorf, Adam, Beck, Samuel, Collard, Marianne, Cole, Philip A, Alani, Rhoda M

“…Virtually all patients with BRAF-mutant melanoma develop resistance to MAPK inhibitors largely through nonmutational events. Although the epigenetic landscape…”
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RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells by Budke, Brian, Logan, Hillary L, Kalin, Jay H, Zelivianskaia, Anna S, Cameron McGuire, William, Miller, Luke L, Stark, Jeremy M, Kozikowski, Alan P, Bishop, Douglas K, Connell, Philip P

“…Homologous recombination serves multiple roles in DNA repair that are essential for maintaining genomic stability. We here describe RI-1, a small molecule that…”
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Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in PIK3CA -Mutant Colorectal Cancer by Miller, Samuel A, Policastro, Robert A, Savant, Sudha S, Sriramkumar, Shruthi, Ding, Ning, Lu, Xiaoyu, Mohammad, Helai P, Cao, Sha, Kalin, Jay H, Cole, Philip A, Zentner, Gabriel E, O'Hagan, Heather M

“…Activation of the epithelial-to-mesenchymal transition (EMT) program is a critical mechanism for initiating cancer progression and migration. Colorectal…”
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Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex by Wu, Mingxuan, Hayward, Dawn, Kalin, Jay H, Song, Yun, Schwabe, John Wr, Cole, Philip A

“…The core CoREST complex (LHC) contains histone deacetylase HDAC1 and histone demethylase LSD1 held together by the scaffold protein CoREST. Here, we analyze…”
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An Optimized RAD51 Inhibitor That Disrupts Homologous Recombination without Requiring Michael Acceptor Reactivity by Budke, Brian, Kalin, Jay H, Pawlowski, Michal, Zelivianskaia, Anna S, Wu, Megan, Kozikowski, Alan P, Connell, Philip P

“…Homologous recombination (HR) is an essential process in cells that provides repair of DNA double-strand breaks and lesions that block DNA replication. RAD51…”
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Investigation into the use of histone deacetylase inhibitor MS-275 as a topical agent for the prevention and treatment of cutaneous squamous cell carcinoma in an SKH-1 hairless mouse model by Kalin, Jay H, Eroglu, Abdulkerim, Liu, Hua, Holtzclaw, W David, Leigh, Irene, Proby, Charlotte M, Fahey, Jed W, Cole, Philip A, Dinkova-Kostova, Albena T

“…Cutaneous squamous cell carcinomas are a common form of highly mutated keratinocyte skin cancers that are of particular concern in immunocompromised patients…”
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HDAC2 targeting stabilizes the CoREST complex in renal tubular cells and protects against renal ischemia/reperfusion injury by Aufhauser, David D., Hernandez, Paul, Concors, Seth J., O’Brien, Ciaran, Wang, Zhonglin, Murken, Douglas R., Samanta, Arabinda, Beier, Ulf H., Krumeich, Lauren, Bhatti, Tricia R., Wang, Yanfeng, Ge, Guanghui, Wang, Liqing, Cheraghlou, Shayan, Wagner, Florence F., Holson, Edward B., Kalin, Jay H., Cole, Philip A., Hancock, Wayne W., Levine, Matthew H.

“…Histone/protein deacetylases (HDAC) 1 and 2 are typically viewed as structurally and functionally similar enzymes present within various co-regulatory…”
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A novel role for histone deacetylase 6 in the regulation of the tolerogenic STAT3/IL-10 pathway in APCs by Cheng, Fengdong, Lienlaf, Maritza, Wang, Hong-Wei, Perez-Villarroel, Patricio, Lee, Calvin, Woan, Karrune, Rock-Klotz, Jennifer, Sahakian, Eva, Woods, David, Pinilla-Ibarz, Javier, Kalin, Jay, Tao, Jianguo, Hancock, Wayne, Kozikowski, Alan, Seto, Edward, Villagra, Alejandro, Sotomayor, Eduardo M

“…APCs are critical in T cell activation and in the induction of T cell tolerance. Epigenetic modifications of specific genes in the APC play a key role in this…”
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Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot–Marie–Tooth Disease by Shen, Sida, Benoy, Veronick, Bergman, Joel A, Kalin, Jay H, Frojuello, Mariana, Vistoli, Giulio, Haeck, Wanda, Van Den Bosch, Ludo, Kozikowski, Alan P

“…Charcot–Marie–Tooth (CMT) disease is a disorder of the peripheral nervous system where progressive degeneration of motor and sensory nerves leads to motor…”
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Second-Generation Histone Deacetylase 6 Inhibitors Enhance the Immunosuppressive Effects of Foxp3+ T-Regulatory Cells by Kalin, Jay H, Butler, Kyle V, Akimova, Tatiana, Hancock, Wayne W, Kozikowski, Alan P

“…Second-generation Tubastatin A analogues were synthesized and evaluated for their ability to inhibit selectively histone deacetylase 6 (HDAC6). Substitutions…”
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Exploration of the labeling of [11C]tubastatin A at the hydroxamic acid site with [11C]carbon monoxide by Lu, Shuiyu, Zhang, Yi, Kalin, Jay H., Cai, Lisheng, Kozikowski, Alan P., Pike, Victor W.

“…We aimed to label tubastatin A (1) with carbon‐11 (t1/2 = 20.4 min) in the hydroxamic acid site to provide a potential radiotracer for imaging histone…”
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A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1 by Prusevich, Polina, Kalin, Jay H, Ming, Shonoi A, Basso, Manuela, Givens, Jeffrey, Li, Xin, Hu, Jianfei, Taylor, Martin S, Cieniewicz, Anne M, Hsiao, Po-Yuan, Huang, Rong, Roberson, Heather, Adejola, Nkosi, Avery, Lindsay B, Casero, Robert A, Taverna, Sean D, Qian, Jiang, Tackett, Alan J, Ratan, Rajiv R, McDonald, Oliver G, Feinberg, Andrew P, Cole, Philip A

“…Lysine-specific demethylase 1 (LSD1) is an epigenetic enzyme that oxidatively cleaves methyl groups from monomethyl and dimethyl Lys4 of histone H3 (H3K4Me1,…”
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