Drug discovery for epigenetics targets

Authors: Holdgate, Geoffrey A., Bardelle, Catherine, Lanne, Alice, Read, Jon, O'Donovan, Daniel H., Smith, James M., Selmi, Nidhal, Sheppard, Robert

Source: In Drug Discovery Today April 2022 27(4):1088-1098

Hypervelocity impact testing of materials for additive construction: Applications on Earth, the Moon, and Mars

Authors: Ordonez, Erick, Edmunson, Jennifer, Fiske, Michael, Christiansen, Eric, Miller, Joshua, Davis, Bruce (Alan), Read, Jon, Johnston, Mallory, Fikes, John

Source: In Procedia Engineering 2017 204:390-396

Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology

Authors: Soutter, Holly H., Centrella, Paolo, Clark, Matthew A., Cuozzo, John W., Dumelin, Christoph E., Guie, Marie-Aude, Habeshian, Sevan, Keefe, Anthony D., Kennedy, Kaitlyn M., Sigel, Eric A., Troast, Dawn M., Zhang, Ying, Ferguson, Andrew D., Davies, Gareth, Stead, Eleanor R., Breed, Jason, Madhavapeddi, Prashanti, Read, Jon A.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2016 Dec 01. 113(49), E7880-E7889.

Access URL: https://www.jstor.org/stable/26472788

AMP-activated protein kinase activation suppresses leptin expression independently of adipogenesis in primary murine adipocytes.

Authors: Bustraan, Sophia, Bennett, Jane, Whilding, Chad, Pennycook, Betheney R., Smith, David, Barr, Alexis R., Read, Jon, Carling, David, Pollard, Alice

Source: Biochemical Journal; Mar2024, Vol. 481 Issue 5, p345-362, 18p

Subject Terms: ADIPOGENESIS, GENE expression, AMP-activated protein kinases, FAT cells, LEPTIN, SMALL molecules, PROTEIN kinases

Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Authors: Grimster, Neil P., Gingipalli, Lakshmaiah, Balazs, Amber, Barlaam, Bernard, Boiko, Scott, Boyd, Scott, Dry, Hannah, Goldberg, Frederick W., Ikeda, Tim, Johnson, Tony, Kawatkar, Sameer, Kemmitt, Paul, Lamont, Scott, Lorthioir, Olivier, Mfuh, Adelphe, Patel, Joe, Pike, Andy, Read, Jon, Romero, Romulo, Sarkar, Ujjal, Sha, Li, Simpson, Iain, Song, Kun, Su, Qibin, Wang, Haixia, Watson, David, Wu, Allan, Zehnder, Troy E., Zheng, XiaoLan, Li, Shaolu, Dong, Zhiqiang, Yang, Dejian, Song, Yanwei, Wang, Peng, Liu, Xuemei, Dowling, James E., Edmondson, Scott D.

Source: In Bioorganic & Medicinal Chemistry Letters 15 July 2023 91

Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein–Ligand Interactions and High Selectivity.

Authors: Collie, Gavin W., Clark, Matthew A., Keefe, Anthony D., Madin, Andrew, Read, Jon A., Rivers, Emma L., Zhang, Ying

Source: Journal of Medicinal Chemistry; 1/25/2024, Vol. 67 Issue 2, p864-884, 21p

Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase

Authors: O' Donovan, Daniel H., Gregson, Clare, Packer, Martin J., Greenwood, Ryan, Pike, Kurt G., Kawatkar, Sameer, Bloecher, Andrew, Robinson, James, Read, Jon, Code, Erin, Hsu, Jessie Hao-Ru, Shen, Minhui, Woods, Haley, Barton, Peter, Fillery, Shaun, Williamson, Beth, Rawlins, Philip B., Bagal, Sharan K.

Source: In Bioorganic & Medicinal Chemistry Letters 1 May 2021 39

Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors

Authors: Barlaam, Bernard, Boiko, Scott, Boyd, Scott, Dry, Hannah, Gingipalli, Lakshmaiah, Ikeda, Timothy, Johnson, Tony, Kawatkar, Sameer, Lorthioir, Olivier, Pike, Andy, Pollard, Hannah, Read, Jon, Su, Qibin, Wang, Haiyun, Wang, Huimin, Wang, Lianghe, Wang, Peng, Edmondson, Scott D.

Source: In Bioorganic & Medicinal Chemistry Letters 15 November 2020 30(22)

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Authors: Grimster, Neil P., Gingipalli, Lakshmaiah, Barlaam, Bernard, Su, Qibin, Zheng, XiaoLan, Watson, David, Wang, Haixia, Simpson, Iain, Pike, Andy, Balazs, Amber, Boiko, Scott, Ikeda, Timothy P., Impastato, Anna C., Jones, Natalie H., Kawatkar, Sameer, Kemmitt, Paul, Lamont, Scott, Patel, Joe, Read, Jon, Sarkar, Ujjal, Sha, Li, Tomlinson, Ronald C., Wang, Haiyun, Wilson, David M., Zehnder, Troy E., Wang, Lianghe, Wang, Peng, Goldberg, Frederick W., Shao, Wenlin, Fawell, Stephen, Dry, Hannah, Dowling, James E., Edmondson, Scott D.

Source: In Bioorganic & Medicinal Chemistry Letters 1 October 2020 30(19)

Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase

Authors: Kawatkar, Sameer P., Barlaam, Bernard, Kemmitt, Paul, Simpson, Iain, Watson, David, Wang, Peng, Lamont, Scott, Su, Qibin, Boiko, Scott, Ikeda, Timothy, Patel, Joe, Pike, Andy, Pollard, Hannah, Read, Jon, Sarkar, Ujjal, Wang, Haiyun, Wen, Quanshan, Yan, Zhiyuan, Dowling, James E., Dry, Hannah, Edmondson, Scott D.

Source: In Bioorganic & Medicinal Chemistry Letters 15 September 2020 30(18)

CHEMICAL COMPOUNDS 251

PYRIMIDINE DERIVATIVES

Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase

Authors: Read, Jon, Collie, Iain T., Nguyen-McCarty, Michelle, Lucaj, Christopher, Robinson, James, Conway, Leslie, Mukherjee, Jayanta, McCall, Eileen, Donohoe, Gerard, Flavell, Elizabeth, Peciak, Karolina, Warwicker, Juli, Dix, Carly, Van den Hoven, Bernard G., Madin, Andrew, Brown, Dean G., Moss, Stephen, Haggarty, Stephen J., Brandon, Nicholas J., Bürli, Roland W.

Source: In Bioorganic & Medicinal Chemistry Letters 1 August 2019 29(15):1962-1967

Mapping the binding site for gossypol-like inhibitors of Plasmodium falciparum lactate dehydrogenase

Authors: Conners, Rebecca, Schambach, Felix, Read, Jon, Cameron, Angus, Sessions, Richard B., Vivas, Livia, Easton, Anna, Croft, Simon L., Brady, R. Leo ^*

Source: In Molecular & Biochemical Parasitology 2005 142(2):137-148

Identification and Activity of a Series of Azole-based Compounds with Lactate Dehydrogenase-directed Anti-malarial Activity

Authors: Cameron, Angus ^‡, Read, Jon ^‡, Tranter, Rebecca ^‡, Winter, Victoria J. ^{‡, §}, Sessions, Richard B. ^‡, Brady, R. Leo ^{‡, ¶}, Vivas, Livia ^∥, Easton, Anna ^∥, Kendrick, Howard ^∥, Croft, Simon L. ^∥, Barros, David ^**, Lavandera, Jose Luis ^**, Martin, José Julio ^**, Risco, Felix ^**, García-Ochoa, Silvestre ^**, Gamo, Fracisco Javier ^**, Sanz, Laura ^**, Leon, Luisa ^**, Ruiz, Jose R. ^**, Gabarró, Raquel ^**, Mallo, Araceli ^**, de las Heras, Federico Gómez ^**

Source: In Journal of Biological Chemistry 23 July 2004 279(30):31429-31439

Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.

Authors: Bagal, Sharan K., Gregson, Clare, O' Donovan, Daniel H., Pike, Kurt G., Bloecher, Andrew, Barton, Peter, Borodovsky, Alexandra, Code, Erin, Fillery, Shaun M., Hsu, Jessie Hao-Ru, Kawatkar, Sameer P., Li, Chengzhi, Longmire, David, Nai, Youfeng, Nash, Samuel C., Pike, Andrew, Robinson, James, Read, Jon A., Rawlins, Phillip B., Shen, Minhui

Source: Journal of Medicinal Chemistry; 12/9/2021, Vol. 64 Issue 23, p17146-17183, 38p

The crystal structure of human phosphoglucose isomerase at 1.6 Å resolution: implications for catalytic mechanism, cytokine activity and haemolytic anaemia

Authors: Read, Jon, Pearce, Jake, Li, Xiaochun, Muirhead, Hilary, Chirgwin, John, Davies, Christopher ^*

Source: In Journal of Molecular Biology 1 June 2001 309(2):447-463

Effector Sites in the Three-Dimensional Structure of Mammalian Sperm β-Acrosin

Authors: Tranter, Rebecca ^*, Read, Jon A. ^*, Jones, Roy ^†, Brady, R.Leo ^{*, *}

Source: In Structure 2000 8(11):1179-1188

Identification of azabenzimidazoles as potent JAK1 selective inhibitors

Authors: Vasbinder, Melissa M., Alimzhanov, Marat, Augustin, Martin, Bebernitz, Geraldine, Bell, Kirsten, Chuaqui, Claudio, Deegan, Tracy, Ferguson, Andrew D., Goodwin, Kelly, Huszar, Dennis, Kawatkar, Aarti, Kawatkar, Sameer, Read, Jon, Shi, Jie, Steinbacher, Stefan, Steuber, Holger, Su, Qibin, Toader, Dorin, Wang, Haixia, Woessner, Richard, Wu, Allan, Ye, Minwei, Zinda, Michael

Source: In Bioorganic & Medicinal Chemistry Letters 1 January 2016 26(1):60-67

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