(Q41860750)

English

Multifactorial resistance to aminopeptidase inhibitor prodrug CHR2863 in myeloid leukemia cells: down-regulation of carboxylesterase 1, drug sequestration in lipid droplets and pro-survival activation ERK/Akt/mTOR.

scientific article published on 19 October 2015

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scholarly article

1 reference

Europe PubMed Central

13 October 2017

Multifactorial resistance to aminopeptidase inhibitor prodrug CHR2863 in myeloid leukemia cells: down-regulation of carboxylesterase 1, drug sequestration in lipid droplets and pro-survival activation ERK/Akt/mTOR. (English)

1 reference

Europe PubMed Central

13 October 2017

object named as

Sarah Kammerer

4

0 references

Elisa Giovannetti

object named as

Elisa Giovannetti

8

0 references

Tanja D de Gruijl

12

object named as

Tanja D de Gruijl

1 reference

Europe PubMed Central

13 October 2017

author name string

Sue Ellen Verbrugge

1

1 reference

Europe PubMed Central

13 October 2017

Marjon Al

2

1 reference

Europe PubMed Central

13 October 2017

Yehuda G Assaraf

3

1 reference

Europe PubMed Central

13 October 2017

Durga M S H Chandrupatla

5

1 reference

Europe PubMed Central

13 October 2017

Richard Honeywell

6

1 reference

Europe PubMed Central

13 October 2017

Rene P J Musters

7

1 reference

Europe PubMed Central

13 October 2017

Tom O'Toole

9

1 reference

Europe PubMed Central

13 October 2017

George L Scheffer

10

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Europe PubMed Central

13 October 2017

David Krige

11

1 reference

Europe PubMed Central

13 October 2017

Hans W M Niessen

13

1 reference

Europe PubMed Central

13 October 2017

Willem F Lems

14

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Europe PubMed Central

13 October 2017

Pieternella A Kramer

15

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Europe PubMed Central

13 October 2017

Rik J Scheper

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Europe PubMed Central

13 October 2017

Jacqueline Cloos

17

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Europe PubMed Central

13 October 2017

Gert J Ossenkoppele

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13 October 2017

Godefridus J Peters

19

1 reference

Europe PubMed Central

13 October 2017

Gerrit Jansen

20

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Europe PubMed Central

13 October 2017

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publication date

19 October 2015

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Europe PubMed Central

13 October 2017

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Europe PubMed Central

13 October 2017

7

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Europe PubMed Central

13 October 2017

5

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13 October 2017

5240-5257

1 reference

Europe PubMed Central

13 October 2017

Inhibition of DNA methyltransferase as a novel therapeutic strategy to overcome acquired resistance to dual PI3K/mTOR inhibitors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Efficacy of dual PI-3K and mTOR inhibitors in vitro and in vivo in acute lymphoblastic leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Activity of the novel mTOR inhibitor Torin-2 in B-precursor acute lymphoblastic leukemia and its therapeutic potential to prevent Akt reactivation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Preclinical and early clinical evaluation of the oral AKT inhibitor, MK-2206, for the treatment of acute myelogenous leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Positioning of aminopeptidase inhibitors in next generation cancer therapy

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

A Tumor suppressor complex with GAP activity for the Rag GTPases that signal amino acid sufficiency to mTORC1

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Two dosing regimens of tosedostat in elderly patients with relapsed or refractory acute myeloid leukaemia (OPAL): a randomised open-label phase 2 study

1 reference

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5 June 2018

Role of endoplasmic reticulum aminopeptidases in health and disease: from infection to cancer

1 reference

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5 June 2018

Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance

1 reference

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5 June 2018

Identification of a novel intracellular cholesteryl ester hydrolase (carboxylesterase 3) in human macrophages: compensatory increase in its expression after carboxylesterase 1 silencing

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

mTOR signaling in growth control and disease

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers

1 reference

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5 June 2018

The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Endoplasmic reticulum aminopeptidase 1 (ERAP1) exhibits functionally significant interaction with HLA-B27 and relates to subtype specificity in ankylosing spondylitis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Inactivating PSMB5 mutations and P-glycoprotein (multidrug resistance-associated protein/ATP-binding cassette B1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno)proteasome inhibitors in mononuclear blood cells from patients

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Drug targeting to monocytes and macrophages using esterase-sensitive chemical motifs.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Interactomic study on interaction between lipid droplets and mitochondria

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The role of lipid droplets in metabolic disease in rodents and humans

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Lipid body function in eicosanoid synthesis: an update

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Aminopeptidase N (CD13) as a target for cancer chemotherapy

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

mTOR: from growth signal integration to cancer, diabetes and ageing

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

A Phase Ib dose-escalation study to evaluate safety and tolerability of the addition of the aminopeptidase inhibitor tosedostat (CHR-2797) to paclitaxel in patients with advanced solid tumours

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Phase I/II clinical study of Tosedostat, an inhibitor of aminopeptidases, in patients with acute myeloid leukemia and myelodysplasia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Perspectives on inhibiting mTOR as a future treatment strategy for hematological malignancies

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The phosphatidylinositol 3-kinase/Akt/mTOR signaling network as a therapeutic target in acute myelogenous leukemia patients.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Activity-based protein profiling identifies a host enzyme, carboxylesterase 1, which is differentially active during hepatitis C virus replication

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Lipid droplets finally get a little R-E-S-P-E-C-T.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Macrophage cholesteryl ester mobilization and atherosclerosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

ABC drug transporters and immunity: novel therapeutic targets in autoimmunity and cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

A first-in-man phase i and pharmacokinetic study on CHR-2797 (Tosedostat), an inhibitor of M1 aminopeptidases, in patients with advanced solid tumors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Human carboxylesterases: an update on CES1, CES2 and CES3.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Leukocyte lipid bodies - Biogenesis and functions in inflammation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Amino acid regulation of TOR complex 1.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Inhibition of carboxylesterase 1 is associated with cholesteryl ester retention in human THP-1 monocyte/macrophages.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

An 86-probe-set gene-expression signature predicts survival in cytogenetically normal acute myeloid leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

CHR-2797: an antiproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The gregarious lipid droplet

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The moonlighting enzyme CD13: old and new functions to target

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Molecular basis of bortezomib resistance: proteasome subunit beta5 (PSMB5) gene mutation and overexpression of PSMB5 protein

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Gene expression predicts differential capecitabine metabolism, impacting on both pharmacokinetics and antitumour activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

ATP-dependent transport of leukotrienes B4 and C4 by the multidrug resistance protein ABCC4 (MRP4).

1 reference

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5 June 2018

Roles and origins of leukocyte lipid bodies: proteomic and ultrastructural studies.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The role of neutral lipid nanospheres in Plasmodium falciparum haem crystallization.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Stable overexpression of human macrophage cholesteryl ester hydrolase results in enhanced free cholesterol efflux from human THP1 macrophages

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Structure, function and regulation of carboxylesterases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Substrate specificity of carboxylesterase isozymes and their contribution to hydrolase activity in human liver and small intestine

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Coexistence of multiple mechanisms of PT523 resistance in human leukemia cells harboring 3 reduced folate carrier alleles: transcriptional silencing, inactivating mutations, and allele loss

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Redistribution of macrophage cholesteryl ester hydrolase from cytoplasm to lipid droplets upon lipid loading

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Insights into unique physiological features of neutral lipids in Apicomplexa: from storage to potential mediation in parasite metabolic activities

1 reference

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5 June 2018

Mammalian carboxylesterases: from drug targets to protein therapeutics

1 reference

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5 June 2018

Pathway for degradation of peptides generated by proteasomes: a key role for thimet oligopeptidase and other metallopeptidases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Role of aminopeptidase in angiogenesis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Resistance to multiple novel antifolates is mediated via defective drug transport resulting from clustered mutations in the reduced folate carrier gene in human leukaemia cell lines

1 reference

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5 June 2018

Single amino acid (arginine) deprivation: rapid and selective death of cultured transformed and malignant cells

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5 June 2018

Characterization of CPT-11 hydrolysis by human liver carboxylesterase isoforms hCE-1 and hCE-2

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Aminopeptidases: structure and function

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

5 June 2018

Clinical trials of bestatin for leukemia and solid tumors

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5 June 2018

Aminopeptidase inhibition as a targeted treatment strategy in myeloma.

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18 August 2018

Targeting of mTOR is associated with decreased growth and decreased VEGF expression in acute myeloid leukaemia cells.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

18 August 2018

Bestatin, an inhibitor for aminopeptidases, modulates the production of cytokines and chemokines by activated monocytes and macrophages

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4868683

18 August 2018

Hydrolysis of capecitabine to 5'-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamide.

1 reference

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18 August 2018

Do cells need CDK2 and ... Bcr-Abl?

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18 August 2018

Randomized Double-Blind Placebo-Controlled Trial of Bestatin in Patients With Resected Stage I Squamous-Cell Lung Carcinoma

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18 August 2018

Cholesterol-modulating agents kill acute myeloid leukemia cells and sensitize them to therapeutics by blocking adaptive cholesterol responses

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18 August 2018

CD13/aminopeptidase N-induced lymphocyte involvement in inflamed joints of patients with rheumatoid arthritis

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18 August 2018

Specific detection of multidrug resistance proteins MRP1, MRP2, MRP3, MRP5, and MDR3 P-glycoprotein with a panel of monoclonal antibodies.

1 reference

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18 August 2018

Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia

1 reference

https://pubmed.ncbi.nlm.nih.gov/26496029

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Cholesterol esters as growth regulators of lymphocytic leukaemia cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/26496029

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Aminopeptidase N/CD13 is directly linked to signal transduction pathways in monocytes

1 reference

https://pubmed.ncbi.nlm.nih.gov/26496029

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Proteins under new management: lipid droplets deliver

1 reference

https://pubmed.ncbi.nlm.nih.gov/26496029

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.18632/ONCOTARGET.6169

1 reference

Europe PubMed Central

13 October 2017

1 reference

Europe PubMed Central

13 October 2017

1 reference

Europe PubMed Central

13 October 2017

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