(Q35543223)

English

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).

scientific article published on 15 January 2015

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scholarly article

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Europe PubMed Central

PubMed publication ID

8 August 2017

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). (English)

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Europe PubMed Central

PubMed publication ID

8 August 2017

author name string

J D Leverson

1

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8 August 2017

H Zhang

2

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8 August 2017

J Chen

3

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8 August 2017

S K Tahir

4

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8 August 2017

D C Phillips

5

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8 August 2017

J Xue

6

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8 August 2017

P Nimmer

7

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8 August 2017

S Jin

8

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8 August 2017

M Smith

9

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8 August 2017

Y Xiao

10

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8 August 2017

P Kovar

11

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8 August 2017

A Tanaka

12

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8 August 2017

M Bruncko

13

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8 August 2017

G S Sheppard

14

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8 August 2017

L Wang

15

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8 August 2017

S Gierke

16

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8 August 2017

L Kategaya

17

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8 August 2017

D J Anderson

18

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8 August 2017

C Wong

19

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8 August 2017

J Eastham-Anderson

20

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8 August 2017

M J C Ludlam

21

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8 August 2017

D Sampath

22

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8 August 2017

W J Fairbrother

23

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8 August 2017

I Wertz

24

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8 August 2017

S H Rosenberg

25

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8 August 2017

C Tse

26

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8 August 2017

S W Elmore

27

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8 August 2017

A J Souers

28

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8 August 2017

publication date

15 January 2015

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8 August 2017

Cell Death and Disease

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8 August 2017

6

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8 August 2017

e1590

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8 August 2017

copyright license

Creative Commons Attribution 4.0 International

1 January 2015

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April 2022 Public Data File from Crossref

copyright status

0 references

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity

1 reference

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12 July 2018

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

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12 July 2018

Structure-Guided Rescaffolding of Selective Antagonists of BCL-X L

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12 July 2018

Regulating cell death at, on, and in membranes.

1 reference

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12 July 2018

The cyclin-dependent kinase inhibitor SNS-032 induces apoptosis in breast cancer cells via depletion of Mcl-1 and X-linked inhibitor of apoptosis protein and displays antitumor activity in vivo

1 reference

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12 July 2018

Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Targeting of MCL-1 kills MYC-driven mouse and human lymphomas even when they bear mutations in p53

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy.

1 reference

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12 July 2018

Purported Mcl-1 inhibitor marinopyrrole A fails to show selective cytotoxicity for Mcl-1-dependent cell lines

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Structure-Guided Rational Design of α/β-Peptide Foldamers with High Affinity for BCL-2 Family Prosurvival Proteins

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Evaluation and critical assessment of putative MCL-1 inhibitors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Loss of MCL-1 leads to impaired autophagy and rapid development of heart failure

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Deletion of MCL-1 causes lethal cardiac failure and mitochondrial dysfunction

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Sabutoclax (BI97C1) and BI112D1, putative inhibitors of MCL-1, induce mitochondrial fragmentation either upstream of or independent of apoptosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Structure-guided design of a selective BCL-X(L) inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Delving deeper: MCL-1's contributions to normal and cancer biology

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

A competitive stapled peptide screen identifies a selective small molecule that overcomes MCL-1-dependent leukemia cell survival

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Rational Design of Proteolytically Stable, Cell-Permeable Peptide-Based Selective Mcl-1 Inhibitors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Anti-apoptotic MCL-1 localizes to the mitochondrial matrix and couples mitochondrial fusion to respiration

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Suppression of myeloid cell leukemia-1 (Mcl-1) enhances chemotherapy-associated apoptosis in gastric cancer cells

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Chemical genomics identifies small-molecule MCL1 repressors and BCL-xL as a predictor of MCL1 dependency

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Direct visualization of Bcl-2 family protein interactions using live cell fluorescent protein redistribution assays

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Anti-apoptotic Mcl-1 is essential for the development and sustained growth of acute myeloid leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

BH3 profiling--measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Identification of a novel Mcl-1 protein binding motif

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Multiple BH3 mimetics antagonize antiapoptotic MCL1 protein by inducing the endoplasmic reticulum stress response and up-regulating BH3-only protein NOXA.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Sensitivity to antitubulin chemotherapeutics is regulated by MCL1 and FBW7.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Mcl-1 is critical for survival in a subgroup of non-small-cell lung cancer cell lines

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Probing the probes: fitness factors for small molecule tools

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Mcl1 haploinsufficiency protects mice from Myc-induced acute myeloid leukemia.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

The landscape of somatic copy-number alteration across human cancers

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

The BCL-2 family reunion

1 reference

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12 July 2018

Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Mcl-1 and Bcl-xL cooperatively maintain integrity of hepatocytes in developing and adult murine liver

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Knockout of myeloid cell leukemia-1 induces liver damage and increases apoptosis susceptibility of murine hepatocytes.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Inducing apoptosis and enhancing chemosensitivity to gemcitabine via RNA interference targeting Mcl-1 gene in pancreatic carcinoma cell

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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A novel BH3 ligand that selectively targets Mcl-1 reveals that apoptosis can proceed without Mcl-1 degradation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

BCL-2 dependence and ABT-737 sensitivity 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=4669759

12 July 2018

Structural insights into the degradation of Mcl-1 induced by BH3 domains

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Programmed anuclear cell death delimits platelet life span.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Mcl-1 down-regulation potentiates ABT-737 lethality by cooperatively inducing Bak activation and Bax translocation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

'Seed' analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Mitochondria primed by death signals determine cellular addiction to antiapoptotic BCL-2 family members

1 reference

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12 July 2018

Puma(*)Mcl-1 interaction is not sufficient to prevent rapid degradation of Mcl-1.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

An inhibitor of Bcl-2 family proteins induces regression of solid tumours

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

12 July 2018

Mcl-1 regulates survival and sensitivity to diverse apoptotic stimuli in human non-small cell lung cancer cells.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

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Myeloid cell factor-1 is a critical survival factor for multiple myeloma

1 reference

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12 July 2018

In vitro and in vivo evaluations of intestinal barriers for the zwitterion L-767,679 and its carboxyl ester prodrug L-775,318. Roles of efflux and metabolism.

1 reference

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12 July 2018

Bcl-2 family proteins are essential for platelet survival.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

26 September 2018

Obligate role of anti-apoptotic MCL-1 in the survival of hematopoietic stem cells.

1 reference

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26 September 2018

Development and maintenance of B and T lymphocytes requires antiapoptotic MCL-1.

1 reference

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26 September 2018

The cyclin-dependent kinase inhibitor flavopiridol induces apoptosis in multiple myeloma cells through transcriptional repression and down-regulation of Mcl-1.

1 reference

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26 September 2018

Antisense strategy shows that Mcl-1 rather than Bcl-2 or Bcl-x(L) is an essential survival protein of human myeloma cells.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4669759

26 September 2018

Nonionic detergents induce dimerization among members of the Bcl-2 family

1 reference

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

1 reference

https://api.crossref.org/works/10.1038%2FCDDIS.2014.561

7 January 2021

based on heuristic

inferred from DOI database lookup

Identifiers

10.1038/CDDIS.2014.561

1 reference

Europe PubMed Central

PubMed publication ID

8 August 2017

Dimensions Publication ID

0 references

PMC publication ID

1 reference

Europe PubMed Central

PubMed publication ID

8 August 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

8 August 2017

ResearchGate publication ID

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