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EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor.
De Mol E, Fenwick RB, Phang CT, Buzón V, Szulc E, de la Fuente A, Escobedo A, García J, Bertoncini CW, Estébanez-Perpiñá E, McEwan IJ, Riera A, Salvatella X. De Mol E, et al. Among authors: garcia j. ACS Chem Biol. 2016 Sep 16;11(9):2499-505. doi: 10.1021/acschembio.6b00182. Epub 2016 Jul 14. ACS Chem Biol. 2016. PMID: 27356095 Free PMC article.
Regulation of Androgen Receptor Activity by Transient Interactions of Its Transactivation Domain with General Transcription Regulators.
De Mol E, Szulc E, Di Sanza C, Martínez-Cristóbal P, Bertoncini CW, Fenwick RB, Frigolé-Vivas M, Masín M, Hunter I, Buzón V, Brun-Heath I, García J, De Fabritiis G, Estébanez-Perpiñá E, McEwan IJ, Nebreda ÁR, Salvatella X. De Mol E, et al. Among authors: garcia j. Structure. 2018 Jan 2;26(1):145-152.e3. doi: 10.1016/j.str.2017.11.007. Epub 2017 Dec 7. Structure. 2018. PMID: 29225078 Free PMC article.
Small molecule inhibits α-synuclein aggregation, disrupts amyloid fibrils, and prevents degeneration of dopaminergic neurons.
Pujols J, Peña-Díaz S, Lázaro DF, Peccati F, Pinheiro F, González D, Carija A, Navarro S, Conde-Giménez M, García J, Guardiola S, Giralt E, Salvatella X, Sancho J, Sodupe M, Outeiro TF, Dalfó E, Ventura S. Pujols J, et al. Among authors: garcia j. Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):10481-10486. doi: 10.1073/pnas.1804198115. Epub 2018 Sep 24. Proc Natl Acad Sci U S A. 2018. PMID: 30249646 Free PMC article.
Side chain to main chain hydrogen bonds stabilize a polyglutamine helix in a transcription factor.
Escobedo A, Topal B, Kunze MBA, Aranda J, Chiesa G, Mungianu D, Bernardo-Seisdedos G, Eftekharzadeh B, Gairí M, Pierattelli R, Felli IC, Diercks T, Millet O, García J, Orozco M, Crehuet R, Lindorff-Larsen K, Salvatella X. Escobedo A, et al. Among authors: garcia j. Nat Commun. 2019 May 2;10(1):2034. doi: 10.1038/s41467-019-09923-2. Nat Commun. 2019. PMID: 31048691 Free PMC article.
Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor.
Eftekharzadeh B, Banduseela VC, Chiesa G, Martínez-Cristóbal P, Rauch JN, Nath SR, Schwarz DMC, Shao H, Marin-Argany M, Di Sanza C, Giorgetti E, Yu Z, Pierattelli R, Felli IC, Brun-Heath I, García J, Nebreda ÁR, Gestwicki JE, Lieberman AP, Salvatella X. Eftekharzadeh B, et al. Among authors: garcia j. Nat Commun. 2019 Aug 8;10(1):3562. doi: 10.1038/s41467-019-11594-y. Nat Commun. 2019. PMID: 31395886 Free PMC article.
Author Correction: Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor.
Eftekharzadeh B, Banduseela VC, Chiesa G, Martínez-Cristóbal P, Rauch JN, Nath SR, Schwarz DMC, Shao H, Marin-Argany M, Di Sanza C, Giorgetti E, Yu Z, Pierattelli R, Felli IC, Brun-Heath I, García J, Nebreda ÁR, Gestwicki JE, Lieberman AP, Salvatella X. Eftekharzadeh B, et al. Among authors: garcia j. Nat Commun. 2019 Oct 7;10(1):4605. doi: 10.1038/s41467-019-12578-8. Nat Commun. 2019. PMID: 31591399 Free PMC article.
Inhibition of α-Synuclein Aggregation and Mature Fibril Disassembling With a Minimalistic Compound, ZPDm.
Peña-Díaz S, Pujols J, Pinheiro F, Santos J, Pallarés I, Navarro S, Conde-Gimenez M, García J, Salvatella X, Dalfó E, Sancho J, Ventura S. Peña-Díaz S, et al. Among authors: garcia j. Front Bioeng Biotechnol. 2020 Oct 16;8:588947. doi: 10.3389/fbioe.2020.588947. eCollection 2020. Front Bioeng Biotechnol. 2020. PMID: 33178678 Free PMC article.
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