(Q92955269)

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2 May 2020

title

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader (English)

1 reference

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2 May 2020

1

1 reference

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2 May 2020

Andrea Testa

series ordinal

2

1 reference

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2 May 2020

Alessio Ciulli

series ordinal

6

1 reference

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2 May 2020

Dario Alessi

series ordinal

7

1 reference

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2 May 2020

5

Claire Crafter

1 reference

2 May 2020

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4

Natalia Shpiro

1 reference

2 May 2020

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Houjiang Zhou

3

1 reference

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2 May 2020

publication date

5 September 2019

1 reference

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2 May 2020

1 reference

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2 May 2020

volume

14

1 reference

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2 May 2020

issue

9

1 reference

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2 May 2020

page(s)

2024-2034

1 reference

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Phosphoproteomics reveals that the hVPS34 regulated SGK3 kinase specifically phosphorylates endosomal proteins including Syntaxin-7, Syntaxin-12, RFIP4 and WDR44

2 May 2020

cites work

1 reference

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PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future

11 February 2021

1 reference

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Selective degradation of CDK6 by a palbociclib based PROTAC

11 February 2021

1 reference

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Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

11 February 2021

1 reference

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SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

11 February 2021

1 reference

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Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

11 February 2021

1 reference

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Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML

11 February 2021

1 reference

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Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

11 February 2021

1 reference

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Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase

11 February 2021

1 reference

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Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds

11 February 2021

1 reference

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3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Kinase inhibitors: the road ahead.

11 February 2021

1 reference

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PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery.

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.

11 February 2021

1 reference

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Mechanism of activation of SGK3 by growth factors via the Class 1 and Class 3 PI3Ks

11 February 2021

1 reference

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

11 February 2021

1 reference

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Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

11 February 2021

1 reference

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Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.

11 February 2021

1 reference

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Structural basis of PROTAC cooperative recognition for selective protein degradation

11 February 2021

1 reference

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Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

11 February 2021

1 reference

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The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth

11 February 2021

1 reference

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PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

11 February 2021

1 reference

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Identification and characterization of essential genes in the human genome.

11 February 2021

1 reference

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PI3K and AKT: Unfaithful Partners in Cancer

11 February 2021

1 reference

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Catalytic in vivo protein knockdown by small-molecule PROTACs.

11 February 2021

1 reference

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

11 February 2021

1 reference

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Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

11 February 2021

1 reference

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DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation

11 February 2021

1 reference

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Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors

11 February 2021

1 reference

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Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase

11 February 2021

1 reference

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Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

11 February 2021

1 reference

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Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Targeting PI3 kinase/AKT/mTOR signaling in cancer.

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

PI3K signalling: the path to discovery and understanding.

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background

11 February 2021

1 reference

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EMD638683, a novel SGK inhibitor with antihypertensive potency.

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer

11 February 2021

1 reference

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mTOR complex 2 (mTORC2) controls hydrophobic motif phosphorylation and activation of serum- and glucocorticoid-induced protein kinase 1 (SGK1)

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic.

11 February 2021

1 reference

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The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

11 February 2021

1 reference

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The selectivity of protein kinase inhibitors: a further update

11 February 2021

1 reference

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Assay of protein kinases using radiolabeled ATP: a protocol

11 February 2021

1 reference

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Role of the Phox homology domain and phosphorylation in activation of serum and glucocorticoid-regulated kinase-3.

11 February 2021

1 reference

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Identification of different specificity requirements between SGK1 and PKBalpha.

11 February 2021

1 reference

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The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB.

11 February 2021

1 reference

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Activation of serum- and glucocorticoid-regulated protein kinase by agonists that activate phosphatidylinositide 3-kinase is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDK1) and PDK2

11 February 2021

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6757289

10.1021/ACSCHEMBIO.9B00505

11 February 2021

Identifiers

DOI

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:31461270%20AND%20SRC:MED&resulttype=core&format=json

2 May 2020

1 reference

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2 May 2020

PubMed publication ID

31461270

1 reference