Virtual screening identifies a PIN1 inhibitor with possible antiovarian cancer effects
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.28224
Abstract: Peptidyl‐prolyl cis–trans isomerase, NIMA‐interacting 1 (PIN1) is a peptidyl‐prolyl isomerase that binds phospho‐Ser/Thr‐Pro motifs in proteins and catalyzes the cis–trans isomerization of proline peptide bonds. PIN1 is overexpressed in several cancers including high‐grade serous ovarian… read more here.
Keywords: virtual screening; pin1 inhibitor; screening identifies; cancer ... See more keywords
Inhibition of the prolyl isomerase Pin1 improves endothelial function and attenuates vascular remodelling in pulmonary hypertension by inhibiting TGF-β signalling.
Sign Up to like & getrecommendations! Published in 2021 at "Angiogenesis"
DOI: 10.1007/s10456-021-09812-7
Abstract: Pulmonary arterial hypertension (PAH) is a devastating disease, characterized by obstructive pulmonary vascular remodelling ultimately leading to right ventricular (RV) failure and death. Disturbed transforming growth factor-β (TGF-β)/bone morphogenetic protein (BMP) signalling, endothelial cell dysfunction,… read more here.
Keywords: vascular remodelling; tgf signalling; inhibition; bmp signalling ... See more keywords
PIN1 facilitates ubiquitin-mediated degradation of serine/threonine kinase 3 and promotes melanoma development via TAZ activation.
Sign Up to like & getrecommendations! Published in 2020 at "Cancer letters"
DOI: 10.1016/j.canlet.2020.11.033
Abstract: The Hippo signaling pathway controls cellular processes including growth, homeostasis, and apoptosis. The kinase STK3 acts upstream in this pathway to activate LATS1/2 kinase, which phosphorylates and inactivates the transcriptional coactivators YAP/TAZ. The dysregulation of… read more here.
Keywords: degradation; hippo signaling; kinase; pin1 facilitates ... See more keywords
A novel controlled release formulation of the Pin1 inhibitor ATRA to improve liver cancer therapy by simultaneously blocking multiple cancer pathways
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Controlled Release"
DOI: 10.1016/j.jconrel.2017.11.031
Abstract: Abstract Hepatocellular carcinoma (HCC) is the second leading cause of cancer deaths worldwide largely due to lack of effective targeted drugs to simultaneously block multiple cancer‐driving pathways. The identification of all‐trans retinoic acid (ATRA) as… read more here.
Keywords: therapy; controlled release; formulation; cancer ... See more keywords
Acidic-basic properties of arginine-rich peptide fragments derived from the human Pin1 protein
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Molecular Liquids"
DOI: 10.1016/j.molliq.2020.113379
Abstract: Abstract The effects of arginine residues in peptide sequences on their specific acid-base properties were investigated. Two short original fragments of the human Pin1 WW domain (hPin1 14–24; hPin1 15–23) and one single point mutation… read more here.
Keywords: arginine rich; properties arginine; acidic basic; human pin1 ... See more keywords
Peptidyl-prolyl isomerase Pin1 deficiency attenuates angiotensin II-induced abdominal aortic aneurysm formation in ApoE-/- mice.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of molecular and cellular cardiology"
DOI: 10.1016/j.yjmcc.2017.12.006
Abstract: Peptidyl-prolyl isomerase Pin1 has been reported to be associated with endothelial dysfunction. However, the role of smooth muscle Pin1 in the vascular system remains unclear. Here, we examined the potential function of Pin1 in smooth… read more here.
Keywords: isomerase pin1; angiotensin induced; peptidyl prolyl; formation ... See more keywords
A Specific pSer/Thr-Pro Motif Generates Interdomain Communication Bifurcations of Two Modes of Pin1 in Solution Nuclear Magnetic Resonance.
Sign Up to like & getrecommendations! Published in 2022 at "Biochemistry"
DOI: 10.1021/acs.biochem.2c00255
Abstract: Peptides mediate the interdomain communication of Pin1 (peptidyl-prolyl cis-trans isomerase) and can regulate its conformation and biochemical functions, providing an idea for drug design using Pin1. Two template peptide sequences have been widely used in… read more here.
Keywords: pser thr; pin1; thr pro; specific pser ... See more keywords
Molecular Mechanism of the Pin1-Histone H1 Interaction.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry"
DOI: 10.1021/acs.biochem.8b01036
Abstract: Pin1 is an essential peptidyl-prolyl isomerase (PPIase) that catalyzes cis-trans prolyl isomerization in proteins containing pSer/Thr-Pro motifs. It has an N-terminal WW domain that targets these motifs and a C-terminal PPIase domain that catalyzes isomerization.… read more here.
Keywords: histone interaction; molecular mechanism; interaction; pin1 histone ... See more keywords
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1).
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01686
Abstract: The unique proline isomerase peptidyl-prolyl isomerase NIMA-interacting-1 (Pin1) is reported to activate numerous cancer-driving pathways simultaneously, and aberrant Pin1 activation is present in many human cancers. Here, we identified a novel hit compound, ZL-Pin01, that… read more here.
Keywords: isomerase nima; inhibitor; prolyl isomerase; pin1 ... See more keywords
PIN1 Protects Hair Cells and Auditory HEI-OC1 Cells against Senescence by Inhibiting the PI3K/Akt/mTOR Pathway
Sign Up to like & getrecommendations! Published in 2021 at "Oxidative Medicine and Cellular Longevity"
DOI: 10.1155/2021/9980444
Abstract: A growing amount of evidence has confirmed the crucial role of the prolyl isomerase PIN1 in aging and age-related diseases. However, the mechanism of PIN1 in age-related hearing loss (ARHL) remains unclear. Pathologically, ARHL is… read more here.
Keywords: oc1 cells; hei oc1; hair cells; senescence ... See more keywords
Inactivation of the Prolyl Isomerase Pin1 Sensitizes BRCA1-Proficient Breast Cancer to PARP Inhibition
Sign Up to like & getrecommendations! Published in 2020 at "Cancer Research"
DOI: 10.1158/0008-5472.can-19-2739
Abstract: PARP inhibitors has been limited to treat homologous recombination–deficient tumors. All-trans retinoic acid, by inhibiting Pin1 and destabilizing BRCA1, extends benefit of PARP inhibitors to patients with homologous recombination–proficient tumors. PARP inhibitor monotherapies are effective… read more here.
Keywords: pin1; cancer; parp inhibitors; brca1 ... See more keywords