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Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1.
Park JJ, Thi EP, Carpio VH, Bi Y, Cole AG, Dorsey BD, Fan K, Harasym T, Iott CL, Kadhim S, Kim JH, Lee ACH, Nguyen D, Paratala BS, Qiu R, White A, Lakshminarasimhan D, Leo C, Suto RK, Rijnbrand R, Tang S, Sofia MJ, Moore CB. Park JJ, et al. Among authors: white a. Nat Commun. 2021 Feb 22;12(1):1222. doi: 10.1038/s41467-021-21410-1. Nat Commun. 2021. PMID: 33619272 Free PMC article.
RVX-297- a novel BD2 selective inhibitor of BET bromodomains.
Kharenko OA, Gesner EM, Patel RG, Norek K, White A, Fontano E, Suto RK, Young PR, McLure KG, Hansen HC. Kharenko OA, et al. Among authors: white a. Biochem Biophys Res Commun. 2016 Aug 12;477(1):62-67. doi: 10.1016/j.bbrc.2016.06.021. Epub 2016 Jun 6. Biochem Biophys Res Commun. 2016. PMID: 27282480
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.
Duffy BC, Liu S, Martin GS, Wang R, Hsia MM, Zhao H, Guo C, Ellis M, Quinn JF, Kharenko OA, Norek K, Gesner EM, Young PR, McLure KG, Wagner GS, Lakshminarasimhan D, White A, Suto RK, Hansen HC, Kitchen DB. Duffy BC, et al. Among authors: white a. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2818-23. doi: 10.1016/j.bmcl.2015.04.107. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 26022843
Antibody-mediated inhibition of GDF15-GFRAL activity reverses cancer cachexia in mice.
Suriben R, Chen M, Higbee J, Oeffinger J, Ventura R, Li B, Mondal K, Gao Z, Ayupova D, Taskar P, Li D, Starck SR, Chen HH, McEntee M, Katewa SD, Phung V, Wang M, Kekatpure A, Lakshminarasimhan D, White A, Olland A, Haldankar R, Solloway MJ, Hsu JY, Wang Y, Tang J, Lindhout DA, Allan BB. Suriben R, et al. Among authors: white a. Nat Med. 2020 Aug;26(8):1264-1270. doi: 10.1038/s41591-020-0945-x. Epub 2020 Jul 13. Nat Med. 2020. PMID: 32661391
Non-homeostatic body weight regulation through a brainstem-restricted receptor for GDF15.
Hsu JY, Crawley S, Chen M, Ayupova DA, Lindhout DA, Higbee J, Kutach A, Joo W, Gao Z, Fu D, To C, Mondal K, Li B, Kekatpure A, Wang M, Laird T, Horner G, Chan J, McEntee M, Lopez M, Lakshminarasimhan D, White A, Wang SP, Yao J, Yie J, Matern H, Solloway M, Haldankar R, Parsons T, Tang J, Shen WD, Alice Chen Y, Tian H, Allan BB. Hsu JY, et al. Among authors: white a. Nature. 2017 Oct 12;550(7675):255-259. doi: 10.1038/nature24042. Epub 2017 Sep 27. Nature. 2017. PMID: 28953886
RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR. McLure KG, et al. Among authors: white a. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PLoS One. 2013. PMID: 24391744 Free PMC article.
Erratum: Non-homeostatic body weight regulation through a brainstem-restricted receptor for GDF15.
Hsu JY, Crawley S, Chen M, Ayupova DA, Lindhout DA, Higbee J, Kutach A, Joo W, Gao Z, Fu D, To C, Mondal K, Li B, Kekatpure A, Wang M, Laird T, Horner G, Chan J, McEntee M, Lopez M, Lakshminarasimhan D, White A, Wang SP, Yao J, Yie J, Matern H, Solloway M, Haldankar R, Parsons T, Tang J, Shen WD, Alice Chen Y, Tian H, Allan BB. Hsu JY, et al. Among authors: white a. Nature. 2017 Nov 16;551(7680):398. doi: 10.1038/nature24481. Epub 2017 Nov 8. Nature. 2017. PMID: 29144449
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Moriarty KJ, Takahashi H, Pullen SS, Khine HH, Sallati RH, Raymond EL, Woska JR Jr, Jeanfavre DD, Roth GP, Winters MP, Qiao L, Ryan D, DesJarlais R, Robinson D, Wilson M, Bobko M, Cook BN, Lo HY, Nemoto PA, Kashem MA, Wolak JP, White A, Magolda RL, Tomczuk B. Moriarty KJ, et al. Among authors: white a. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5545-9. doi: 10.1016/j.bmcl.2008.09.015. Epub 2008 Sep 7. Bioorg Med Chem Lett. 2008. PMID: 18819799
6,830 results