#fkbp12 resultados de búsqueda
New plasmids Chen Lab #FKBP12-rapamycin-BD reqd for PK activity & G1 progression hubs.ly/H02Kwk30 @JBiolChem
#FKBP12 contributes to { alpha } #-synuclein #toxicity by regulating the calcineurin-dependent #phosphoproteome #[ ..goo.gl/RQEFJJ
The #ionchannel TRPM8 is a direct target of the immunosuppressant rapamycin in primary sensory neurons - Arcas #OpenAccess @BrJPharmacol buff.ly/3UG5hxZ
KB02-SLF is a #PROTAC based nuclear #FKBP12 degrader (#molecularglue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying #DCAF16 (E3 ligase). SLF binds ubiquitin E3 ligase ligand #KB02 via a linker to form KB02-SLF. #drugdiscovery. bit.ly/3mB9wJ8
最近の発見について日本語で概説しました。免疫抑制剤のレセプターである #FKBP12 は真菌ではアミノ酸合成を抑制する、というお話。#ケミカルバイオロジー の業界では知らない者はいないFKBP12タンパク質ですが、どうやら奥が深そうです。 a.u-tokyo.ac.jp/topics/topics_…
#dFKBP-1 is a #PROTAC-based FKBP12 degrader. dFKBP-1 decreases #FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. #drugdiscovery. bit.ly/3muRveK
We ran a full mechanism of action elucidation campaign to show that the efficacy target of our screening hit was #FKBP12 and designed using co-crystal structure a calcineurin-sparing #tacrolimus analogue that could show efficacy in a mice model of Acute Kidney Injury.
'Pay with a Tweet' Wednesday PPT download: Regulation of mTORC1 and mTORC2 scienceslides.com/NVmg #rag #fkbp12 #enac #fkbp38 #foxo3a
We hope that our new calcineurin-sparing analogue #oxtFK can be further progressed, as well as be used as a chemical probe for #FKBP12 inhibition in vitro and in vivo.
'Pay with a Tweet' Wednesday PPT download: TrkB receptor signaling in neurons scienceslides.com/8gGB #fkbp12 #crkl #pkcdelta #zdhhc8
'Pay with a Tweet' Wednesday PPT download: Regulation of mTORC1 and mTORC2 scienceslides.com/NVmg #rag #fkbp12 #enac #fkbp38 #foxo3a
The plasticity of #molecularglue #FKBP12 combined with modified #FK506 variants is capable of engaging with more targets than previously expected! Great @PNASNews article by @glostaman (Verdine) showing potent binding of an essentially flat coiled coil. pnas.org/content/early/…
The TOR Signaling Network in the Model Unicellular Green Alga Chlamydomonas reinhardtii sci.fo/3d5 #Rapamycin #FKBP12 #Algae
RapaLink-1, the #mTOR inhibitor, combines Rapamycin with MLN0128 (a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 binding to #FKBP12 results in targeted and durable inhibition of #mTORC1.
Check out the 1st first-author paper @Ingridql 🥳@NTNUikom @myelomatosenytt @NTNUNaturalSci @StOlavshospital @OACellBiology #myeloma #FKBP12 #ACVR1 with @Hamartinka @oddrunelise @JeromeJatzlau @Hausch_lab and Petra Knaus biosignaling.biomedcentral.com/articles/10.11…
We show that targeting #FKBP12 using #FK506 or siRNA potentiates ALK2 activating ligands such as BMP6 and BMP9.
The Preview by Dr. Felix Hausch @Hausch_lab at @TUDarmstadt highlights the work of @MarieLarraufie and colleagues describing how #FKBP12 inhibition can be a target for treatment of AKI via activation of #BMPsignaling dlvr.it/S7jXXg
cell.com
Break Away: FKBP12 sequestration as a target for increasing BMP activity
Bone morphogenetic protein (BMP) signaling contributes to acute kidney injury (AKI), a common disease without adequate treatment options. In this issue of Cell Chemical Biology, Larraufie, Gao and...
FKBP12はtauのリン酸化時、凝集の要となる2部位に結合しmouseのneuronでtauの凝集を抑制 ヒトのneuron-astrocytesの3次元培養でtauのoligomer化と神経変性を抑制 分子量の大きいtauでは抗体より小分子の方が戦術的に有利かも Open Access #FKBP12 #tau #papers 👇論文 science.org/doi/10.1126/sc…
抗Tau抗体TilavonemabはLOADの進行を抑制せず 細胞外凝集tauに対するヒト化IgG4抗体 Tilavonemabを、Aβ蓄積がPETで確認された軽度認知障害を有する435名に96週間、４週間毎の投与を行ったphse II studyにて認知機能低下を抑制せず Open Access #Alzheimers #papers
The #ionchannel TRPM8 is a direct target of the immunosuppressant rapamycin in primary sensory neurons - Arcas #OpenAccess @BrJPharmacol buff.ly/3UG5hxZ
Have a look at our last paper in @ACSCentSci! We describe diazonium #BODIPY for the labelling of Tyr in peptides and proteins and the first #fluorogenic analogue of immunophilin #FKBP12 for the detection of #tacrolimus! #Chemistry #Fluorescence pubs.acs.org/doi/10.1021/ac…
FKBP12はtauのリン酸化時、凝集の要となる2部位に結合しmouseのneuronでtauの凝集を抑制 ヒトのneuron-astrocytesの3次元培養でtauのoligomer化と神経変性を抑制 分子量の大きいtauでは抗体より小分子の方が戦術的に有利かも Open Access #FKBP12 #tau #papers 👇論文 science.org/doi/10.1126/sc…
抗Tau抗体TilavonemabはLOADの進行を抑制せず 細胞外凝集tauに対するヒト化IgG4抗体 Tilavonemabを、Aβ蓄積がPETで確認された軽度認知障害を有する435名に96週間、４週間毎の投与を行ったphse II studyにて認知機能低下を抑制せず Open Access #Alzheimers #papers
We show that targeting #FKBP12 using #FK506 or siRNA potentiates ALK2 activating ligands such as BMP6 and BMP9.
Check out the 1st first-author paper @Ingridql 🥳@NTNUikom @myelomatosenytt @NTNUNaturalSci @StOlavshospital @OACellBiology #myeloma #FKBP12 #ACVR1 with @Hamartinka @oddrunelise @JeromeJatzlau @Hausch_lab and Petra Knaus biosignaling.biomedcentral.com/articles/10.11…
最近の発見について日本語で概説しました。免疫抑制剤のレセプターである #FKBP12 は真菌ではアミノ酸合成を抑制する、というお話。#ケミカルバイオロジー の業界では知らない者はいないFKBP12タンパク質ですが、どうやら奥が深そうです。 a.u-tokyo.ac.jp/topics/topics_…
We hope that our new calcineurin-sparing analogue #oxtFK can be further progressed, as well as be used as a chemical probe for #FKBP12 inhibition in vitro and in vivo.
We ran a full mechanism of action elucidation campaign to show that the efficacy target of our screening hit was #FKBP12 and designed using co-crystal structure a calcineurin-sparing #tacrolimus analogue that could show efficacy in a mice model of Acute Kidney Injury.
#dFKBP-1 is a #PROTAC-based FKBP12 degrader. dFKBP-1 decreases #FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. #drugdiscovery. bit.ly/3muRveK
RapaLink-1, the #mTOR inhibitor, combines Rapamycin with MLN0128 (a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 binding to #FKBP12 results in targeted and durable inhibition of #mTORC1.
The plasticity of #molecularglue #FKBP12 combined with modified #FK506 variants is capable of engaging with more targets than previously expected! Great @PNASNews article by @glostaman (Verdine) showing potent binding of an essentially flat coiled coil. pnas.org/content/early/…
#dFKBP-1 is a #PROTAC-based FKBP12 degrader. dFKBP-1 decreases #FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. #drugdiscovery. bit.ly/3muRveK
New plasmids Chen Lab #FKBP12-rapamycin-BD reqd for PK activity & G1 progression hubs.ly/H02Kwk30 @JBiolChem
We hope that our new calcineurin-sparing analogue #oxtFK can be further progressed, as well as be used as a chemical probe for #FKBP12 inhibition in vitro and in vivo.
KB02-SLF is a #PROTAC based nuclear #FKBP12 degrader (#molecularglue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying #DCAF16 (E3 ligase). SLF binds ubiquitin E3 ligase ligand #KB02 via a linker to form KB02-SLF. #drugdiscovery. bit.ly/3mB9wJ8
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