Identification, structure and agonist design of an androgen membrane receptor.
Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP
Cell (2025) [ Pubmed: 39884271 DOI: doi:10.1016/j.cell.2025.01.006 ]
- 5-alpha-dihydrotestosterone (290 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Bos taurus)
- Gs protein alpha subunit (41 kDa, Protein from Bos taurus)
- Complex of gpr133 with agonist and g protein trime (Complex from Bos taurus)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
- Adhesion g-protein coupled receptor d1 (65 kDa, Protein from Homo sapiens)
Identification, structure and agonist design of an androgen membrane receptor
Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP
Cell (2025) [ Pubmed: 39884271 DOI: doi:10.1016/j.cell.2025.01.006 ]
- Scfv16 (28 kDa, Protein from synthetic construct)
- Methyl 3-[2-(2,4-dimethylphenoxy)ethanoylamino]-4-(4-ethylpiperazin-1-yl)benzoate (425 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Bos taurus)
- Gs protein alpha subunit (41 kDa, Protein from Bos taurus)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
- Complex of gpr133 with agonist and g protein trimer (Complex from Bos taurus)
- Adhesion g-protein coupled receptor d1 (65 kDa, Protein from Homo sapiens)
Identification, structure and agonist design of an androgen membrane receptor
Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP
Cell (2025) [ Pubmed: 39884271 DOI: doi:10.1016/j.cell.2025.01.006 ]
- (5s,8r,9s,10s,13s,14s,17s)-17-hydroxy-1,10,13-trimethyl-4,5,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one (302 Da, Ligand)
- Scfv16 (28 kDa, Protein from synthetic construct)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Bos taurus)
- Complex of gpr133 with agonist and g protein trimer. (Complex from Rattus norvegicus)
- Gs protein alpha subunit (41 kDa, Protein from Bos taurus)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
- Adhesion g-protein coupled receptor d1 (65 kDa, Protein from Homo sapiens)
Resolution: 3.7 Å
EM Method: Single-particle
Fitted PDBs: 7try
Q-score: 0.338
Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE
Nat Commun (2022) 13 pp. 6670-6670 [ DOI: doi:10.1038/s41467-022-33851-3 Pubmed: 36335102 ]
- Urocortin (4 kDa, Protein from Homo sapiens)
- Corticotropin releasing factor receptor 2 (crf2r) bound to urocortin 1 (ucn1) and coupled with g11 proteins (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (43 kDa, Protein from Rattus norvegicus)
- Corticotropin-releasing factor receptor 2 (63 kDa, Protein from Homo sapiens)
- Scfv16 (26 kDa, Protein from synthetic construct)
- Guanine nucleotide-binding protein subunit alpha-11 (41 kDa, Protein from Homo sapiens)
- G protein gamma subunit (7 kDa, Protein from Rattus norvegicus)
Resolution: 2.8 Å
EM Method: Single-particle
Fitted PDBs: 7ts0
Q-score: 0.494
Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE
Nat Commun (2022) 13 pp. 6670-6670 [ DOI: doi:10.1038/s41467-022-33851-3 Pubmed: 36335102 ]
- Urocortin (4 kDa, Protein from Homo sapiens)
- Corticotropin-releasing factor receptor 2,corticotropin-releasing factor receptor 2,corticotropin-releasing factor receptor 2,corticotropin-releasing factor receptor 2,human corticotropin releasing factor receptor 2 (63 kDa, Protein from Homo sapiens)
- Corticotropin releasing factor receptor 2 (crf2r) bound to urocortin 1 (ucn1) and coupled with g11 proteins (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (43 kDa, Protein from Rattus norvegicus)
- Scfv16 (26 kDa, Protein from synthetic construct)
- Dominant negative go alpha subunit (40 kDa, Protein from Homo sapiens)
- G protein gamma subunit (7 kDa, Protein from Rattus norvegicus)
Resolution: 3.3 Å
EM Method: Single-particle
Fitted PDBs: 7eq1
Q-score: 0.463
Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP
Nature (2022) 604 pp. 763-770 [ Pubmed: 35418678 DOI: doi:10.1038/s41586-022-04619-y ]
- Scfv16 (26 kDa, Protein from synthetic construct)
- Adhesion g-protein coupled receptor g5 (33 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Bos taurus)
- Gs protein alpha subunit (41 kDa, Protein from Bos taurus)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
- Gpr114beta-gs-scfv16 complex (Complex from Homo sapiens)