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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1963 1
1965 2
1967 1
1968 1
1970 1
1971 9
1972 3
1973 2
1974 2
1975 2
1976 2
1977 9
1978 4
1979 8
1980 5
1981 7
1982 7
1983 8
1984 15
1985 13
1986 20
1987 18
1988 16
1989 22
1990 27
1991 28
1992 34
1993 32
1994 40
1995 60
1996 67
1997 59
1998 63
1999 81
2000 72
2001 65
2002 95
2003 110
2004 120
2005 150
2006 137
2007 130
2008 187
2009 172
2010 215
2011 237
2012 246
2013 288
2014 267
2015 292
2016 299
2017 298
2018 304
2019 328
2020 348
2021 368
2022 395
2023 396
2024 154

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5,760 results

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Page 1
Induced protein degradation: an emerging drug discovery paradigm.
Lai AC, Crews CM. Lai AC, et al. Nat Rev Drug Discov. 2017 Feb;16(2):101-114. doi: 10.1038/nrd.2016.211. Epub 2016 Nov 25. Nat Rev Drug Discov. 2017. PMID: 27885283 Free PMC article. Review.
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that directly affects protein function, and this approach typically precludes targeting proteins that lack such amenable sites. ...Induced protein degradation is an alternative approach …
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that directly affects protein function, and th …
The HDAC10 instructs macrophage M2 program via deacetylation of STAT3 and promotes allergic airway inflammation.
Zhong Y, Huang T, Huang J, Quan J, Su G, Xiong Z, Lv Y, Li S, Lai X, Xiang Y, Wang Q, Luo L, Gao X, Shao Y, Tang J, Lai T. Zhong Y, et al. Theranostics. 2023 Jun 19;13(11):3568-3581. doi: 10.7150/thno.82535. eCollection 2023. Theranostics. 2023. PMID: 37441601 Free PMC article.
Hdac10 deficiency significantly attenuated STAT3 expression and decreased M2 macrophage polarization following allergen exposure. Mechanistically, HDAC10 directly binds STAT3 for deacetylation in macrophages, by which it promotes STAT3 expression and activates the macropha …
Hdac10 deficiency significantly attenuated STAT3 expression and decreased M2 macrophage polarization following allergen exposure. Mechanisti …
Computational design of ligand-binding proteins.
Yang W, Lai L. Yang W, et al. Curr Opin Struct Biol. 2017 Aug;45:67-73. doi: 10.1016/j.sbi.2016.11.021. Epub 2016 Dec 9. Curr Opin Struct Biol. 2017. PMID: 27951448 Review.
Custom-designed ligand-binding proteins with novel functions hold the potential for numerous applications. ...Though much has been learned in these successful design cases, advances in our understanding of protein dynamics and functions related to ligand binding and …
Custom-designed ligand-binding proteins with novel functions hold the potential for numerous applications. ...Though much has been le …
Tumor cell-released kynurenine biases MEP differentiation into megakaryocytes in individuals with cancer by activating AhR-RUNX1.
Zhou L, Wu D, Zhou Y, Wang D, Fu H, Huang Q, Qin G, Chen J, Lv J, Lai S, Zhang H, Tang K, Ma J, Fiskesund R, Zhang Y, Zhang X, Huang B. Zhou L, et al. Nat Immunol. 2023 Dec;24(12):2042-2052. doi: 10.1038/s41590-023-01662-3. Epub 2023 Nov 2. Nat Immunol. 2023. PMID: 37919525 Free PMC article.
During tumor growth, large amounts of Kyn from tumor cells are released into the periphery, where they are taken up by MEPs via the transporter SLC7A8. In the cytosol, Kyn binds to and activates AhR, leading to its translocation into the nucleus where AhR transactivates RU …
During tumor growth, large amounts of Kyn from tumor cells are released into the periphery, where they are taken up by MEPs via the transpor …
Building Transcription Factor Binding Site Models to Understand Gene Regulation in Plants.
Lai X, Stigliani A, Vachon G, Carles C, Smaczniak C, Zubieta C, Kaufmann K, Parcy F. Lai X, et al. Mol Plant. 2019 Jun 3;12(6):743-763. doi: 10.1016/j.molp.2018.10.010. Epub 2018 Nov 15. Mol Plant. 2019. PMID: 30447332 Free article. Review.
Transcription factors (TFs) are key cellular components that control gene expression. They recognize specific DNA sequences, the TF binding sites (TFBSs), and thus are targeted to specific regions of the genome where they can recruit transcriptional co-factors and/or chrom …
Transcription factors (TFs) are key cellular components that control gene expression. They recognize specific DNA sequences, the TF bindi …
Binding site detection and druggability prediction of protein targets for structure-based drug design.
Yuan Y, Pei J, Lai L. Yuan Y, et al. Curr Pharm Des. 2013;19(12):2326-33. doi: 10.2174/1381612811319120019. Curr Pharm Des. 2013. PMID: 23082974 Review.
A brief summary of the established methods of binding sites detection and druggability(ligandability) prediction, as well as a detailed description of the CAVITY approach developed in the authors' group was given. CAVITY showed good performance on ligand-binding sit …
A brief summary of the established methods of binding sites detection and druggability(ligandability) prediction, as well as a detail …
Nucleus-localized circSLC39A5 suppresses hepatocellular carcinoma development by binding to STAT1 to regulate TDG transcription.
Liu M, Lai M, Li D, Zhang R, Wang L, Peng W, Yang J, He W, Sheng Y, Xiao S, Nan A, Zeng X. Liu M, et al. Cancer Sci. 2023 Oct;114(10):3884-3899. doi: 10.1111/cas.15906. Epub 2023 Aug 7. Cancer Sci. 2023. PMID: 37549641 Free PMC article.
Remarkably, circSLC39A5 is mainly localized in the nucleus and binds to the transcription factor signal transducer and activator of transcription 1 (STAT1), affecting its stabilization and expression. STAT1 binds to the promoter of thymine DNA glycosylase (TDG). Ove …
Remarkably, circSLC39A5 is mainly localized in the nucleus and binds to the transcription factor signal transducer and activator of t …
Phenylthiourea Binding to Human Tyrosinase-Related Protein 1.
Lai X, Wichers HJ, Soler-Lopez M, Dijkstra BW. Lai X, et al. Int J Mol Sci. 2020 Jan 30;21(3):915. doi: 10.3390/ijms21030915. Int J Mol Sci. 2020. PMID: 32019241 Free PMC article.
Here, we show, from an X-ray crystal structure determination, that phenylthiourea, a highly potent tyrosinase inhibitor, does neither coordinate the active site zinc ions, but binds differently from other structurally characterized TYRP1-inhibitor complexes. Its aromatic r …
Here, we show, from an X-ray crystal structure determination, that phenylthiourea, a highly potent tyrosinase inhibitor, does neither coordi …
The price of P2X7R freedom is neuroinflammation.
Fang M, Lai R. Fang M, et al. Immunity. 2024 Mar 12;57(3):401-403. doi: 10.1016/j.immuni.2024.02.009. Immunity. 2024. PMID: 38479354
Huang et al. demonstrate that the complex of sodium/potassium-transporting ATPase subunit alpha (NKAalpha1) and purinergic P2X7 receptor (P2X7R) maintains the resting state of microglial membranes. Stress increases free P2X7R that then binds to ATP to activate microglia, w …
Huang et al. demonstrate that the complex of sodium/potassium-transporting ATPase subunit alpha (NKAalpha1) and purinergic P2X7 receptor (P2 …
CsrA regulation via binding to the base-pairing small RNA Spot 42.
Lai YJ, Yakhnin H, Pannuri A, Pourciau C, Babitzke P, Romeo T. Lai YJ, et al. Mol Microbiol. 2022 Jan;117(1):32-53. doi: 10.1111/mmi.14769. Epub 2021 Jul 7. Mol Microbiol. 2022. PMID: 34107125 Free PMC article.
A second, independent mechanism by which CsrA represses srlA is by binding to and inhibiting translation of srlM mRNA, encoding a transcriptional activator of srlA. Our findings demonstrate a novel means of regulation, by CsrA binding to a sRNA, and indicate that su …
A second, independent mechanism by which CsrA represses srlA is by binding to and inhibiting translation of srlM mRNA, encoding a tra …
5,760 results