(Q34751984)

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Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone.

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22 January 2020

Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone (English)

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22 January 2020

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22 January 2020

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22 January 2020

Christopher P Austin

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22 January 2020

Jong Yeon Hwang

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22 January 2020

Jennifer Wichterman

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Indre Augustinaite

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Indre Augustinaite

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22 January 2020

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22 January 2020

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Ramy R Attia

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22 January 2020

Michele C Connelly

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22 January 2020

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Fangyi Zhu

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22 January 2020

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Ruili Huang

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22 January 2020

James Inglese

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22 January 2020

Ronald L Johnson

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22 January 2020

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14 February 2011

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22 January 2020

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14

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Journal of Biological Chemistry

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22 January 2020

286

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22 January 2020

14

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22 January 2020

11895-11908

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22 January 2020

Studies on the toxicity and efficacy of some ester analogues of dapsone in vitro using rat and human tissues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Molecular aspects of thyroid hormone actions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Regulation of pyruvate dehydrogenase kinase 4 (PDK4) by thyroid hormone: role of the peroxisome proliferator-activated receptor gamma coactivator (PGC-1 alpha)

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Thyroid hormones and the control of cell proliferation or cell differentiation: paradox or duality?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

In vivo interaction of steroid receptor coactivator (SRC)-1 and the activation function-2 domain of the thyroid hormone receptor (TR) beta in TRbeta E457A knock-in and SRC-1 knockout mice

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Ligand induced interaction of thyroid hormone receptor beta with its coregulators

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Complex actions of thyroid hormone receptor antagonist NH-3 on gene promoters in different cell lines

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Implications of the binding of tamoxifen to the coactivator recognition site of the estrogen receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Nuclear receptor drug discovery

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Access and binding of local anesthetics in the closed sodium channel

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Structural and Biochemical Basis for the Binding Selectivity of Peroxisome Proliferator-activated Receptor to PGC-1

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Activated pregnenolone X-receptor is a target for ketoconazole and its analogs.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Medicinal chemistry of hERG optimizations: Highlights and hang-ups

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

The nuclear receptor superfamily and drug discovery

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Biological evaluation and structure-activity relationships of bis-(3-aryl-3-oxo-propyl)-methylamine hydrochlorides and 4-aryl-3-arylcarbonyl-1-methyl-4-piperidinol hydrochlorides as potential cytotoxic agents and their alkylating ability towards cel

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

The nuclear receptor superfamily: a personal retrospect on the first two decades

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Principles for modulation of the nuclear receptor superfamily

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

The evolution of the nuclear receptor superfamily

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Evidence for a potent antiinflammatory effect of rosiglitazone

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Quantitative proteomics of the thyroid hormone receptor-coregulator interactions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

The coactivator LXXLL nuclear receptor recognition motif.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Bicalutamide (Casodex) in the treatment of prostate cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Voltage-gated K channels

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Review of the in vivo functions of the p160 steroid receptor coactivator family

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Design of thyroid hormone receptor antagonists from first principles

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Glitazones: clinical effects and molecular mechanisms

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Mechanism of thyroid hormone action

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

A thyroid hormone antagonist that inhibits thyroid hormone action in vivo

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Tissue-specific actions of thyroid hormone: insights from animal models

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Cloning and characterization of two novel thyroid hormone receptor beta isoforms

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Ion channels: from idea to reality

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Determinants of coactivator LXXLL motif specificity in nuclear receptor transcriptional activation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Structure and specificity of nuclear receptor-coactivator interactions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Voltage-gated ion channels and electrical excitability

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Molecular basis of thyroid hormone-dependent brain development

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

Analysis of the functional role of steroid receptor coactivator-1 in ligand-induced transactivation by thyroid hormone receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

CCAAT-enhancer-binding protein alpha (C/EBP alpha) is required for the thyroid hormone but not the retinoic acid induction of phosphoenolpyruvate carboxykinase (PEPCK) gene transcription

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

The nuclear receptor superfamily: the second decade

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

A biological profile of a nonsteroidal antiandrogen, SCH 13521 (4'-nitro-3'trifluoromethylisobutyranilide).

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

7 July 2018

An Evaluation of Bicalutamide in the Treatment of Prostate Cancer

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

SRC-p300 coactivator complex is required for thyroid hormone-induced amphibian metamorphosis.

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Nuclear receptor-binding sites of coactivators glucocorticoid receptor interacting protein 1 (GRIP1) and steroid receptor coactivator 1 (SRC-1): multiple motifs with different binding specificities

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Effects of the thyroid hormone receptor agonist GC-1 on metabolic rate and cholesterol in rats and primates: selective actions relative to 3,5,3'-triiodo-L-thyronine

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Steroid receptor coactivator peptidomimetics

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Nitrobenzene compounds inhibit expression of VCAM-1.

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Assay Optimization and Screening of RNA-Protein Interactions by AlphaScreen.

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Development of a versatile platform for nuclear receptor screening using AlphaScreen

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Molecular structure of the rat vitamin D receptor ligand binding domain complexed with 2-carbon-substituted vitamin D3 hormone analogues and a LXXLL-containing coactivator peptide

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

A new amino-masking group capable of pH-triggered amino-drug release

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

Inhalation toxicity studies of the alpha,beta-unsaturated ketones: ethyl vinyl ketone

1 reference

https://api.crossref.org/works/10.1074%2FJBC.M110.200436

21 January 2018

A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

26 October 2018

Cancer 2025: Radiotherapy

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3069392

9 December 2018

1 reference

https://pubmed.ncbi.nlm.nih.gov/21321127

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding

1 reference

https://pubmed.ncbi.nlm.nih.gov/21321127

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Inhibition of some mitochondrial functions by acrolein and methylvinylketone

1 reference

https://pubmed.ncbi.nlm.nih.gov/21321127

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

β-Aminoketones as prodrugs with pH-controlled activation

1 reference

https://pubmed.ncbi.nlm.nih.gov/21321127

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A correlation of thyroid hormone receptor gene expression with amphibian metamorphosis

1 reference

https://pubmed.ncbi.nlm.nih.gov/21321127

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1074/JBC.M110.200436

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:21321127%20AND%20SRC:MED&resulttype=core&format=json

22 January 2020

PMC publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:21321127%20AND%20SRC:MED&resulttype=core&format=json

22 January 2020

PubMed publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:21321127%20AND%20SRC:MED&resulttype=core&format=json

22 January 2020

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