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A Gate-Latch-Lock Mechanism for Hormone Signaling by Abscisic Acid Receptors
Crystal structures of apo and ABA-bound receptors as well as a ternary PYL2–ABA–PP2C complex are reported to identify a conserved gate–latch–lock mechanism underlying ABA signalling. Expand
Androgen receptor: structure, role in prostate cancer and drug discovery
An overview of androgen receptor structure and activity, its actions in prostate cancer, and how structural information and high-throughput screening have been or can be used for drug discovery are provided are provided. Expand
Molecular Mimicry Regulates ABA Signaling by SnRK2 Kinases and PP2C Phosphatases
Structural results provide a simple mechanism that directly couples ABA binding to SnRK2 kinase activation and highlight a new paradigm of kinase-phosphatase regulation through mutual packing of their catalytic sites. Expand
Filamin-A fragment localizes to the nucleus to regulate androgen receptor and coactivator functions
A negative regulatory domain in the AR hinge region was characterized, which interacted with filamin A (FLNa), an actin-binding cytoskeletal protein that interfered with AR interdomain interactions and competed with the coactivator transcriptional intermediary factor 2 to specifically down-regulate AR function. Expand
Long polyglutamine tracts in the androgen receptor are associated with reduced trans-activation, impaired sperm production, and male infertility.
The data indicate a direct relation between length of the AR polyglutamine tract and the risk of defective spermatogenesis that is attributable to the decreased functional competence of AR with longer glutamine tracts. Expand
Trinucleotide (CAG) repeat polymorphisms in the androgen receptor gene: molecular markers of risk for male infertility.
Long (> or =26) androgen receptor CAG alleles, which are found in up to 25% of azoospermic men, are associated with male infertility and defective spermatogenesis. Expand
Identification and Mechanism of 10-Carbon Fatty Acid as Modulating Ligand of Peroxisome Proliferator-activated Receptors*
Decanoic acid, a 10-carbon fatty acid and a major component of medium chain triglyceride oils, is a direct ligand of PPARγ, suggesting that DA is a modulating ligand for PPARs, and the structure can aid in designing better and safer PParγ-based drugs. Expand
AP‐2γ regulates oestrogen receptor‐mediated long‐range chromatin interaction and gene transcription
AP-2γ, which has been implicated in breast cancer oncogenesis, binds to ERBS in a ligand-independent manner and is suggested to be a novel collaborative factor in ERα-mediated transcription. Expand
Androgen receptor gene CAG trinucleotide repeats in anovulatory infertility and polycystic ovaries.
An association between short CAG repeat length and the subset of anovulatory patients with low serum androgens is indicated, suggesting that the pathogenic mechanism of polycystic ovaries in these patients could be due to the increased intrinsic androgenic activity associated with short AR alleles. Expand
Structural basis for basal activity and autoactivation of abscisic acid (ABA) signaling SnRK2 kinases
  • L.-M. Ng, F.-F. Soon, +10 authors H. Xu
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences
  • 12 December 2011
Crystal structures of full-length Arabidopsis thaliana SnRK2.3 and SnRk2.6 reveal a two-step mechanism of intramolecular kinase activation that resembles the intermolecular activation of cyclin-dependent kinases, and provide a structural framework that links ABA-mediated release of PP2C inhibition to activation of SnK2 kinases. Expand