Structure-guided design of a selective BCL-X(L) inhibitor (Q27684453)

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

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instance of

scholarly article

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title

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

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author

Brad E Sleebs

object named as

Brad E Sleebs

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3

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Brian J. Smith

object named as

Brian J Smith

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17

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author name string

Guillaume Lessene

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1

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Peter E Czabotar

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2

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Kerry Zobel

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4

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Kym N Lowes

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5

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Jerry M Adams

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6

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Jonathan B Baell

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7

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Peter M Colman

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8

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Kurt Deshayes

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9

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Wayne J Fairbrother

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10

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John A Flygare

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11

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Paul Gibbons

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12

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Wilhelmus J A Kersten

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13

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Sanji Kulasegaram

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14

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Rebecca M Moss

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15

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John P Parisot

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16

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Ian P Street

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18

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Hong Yang

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19

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David C S Huang

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20

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Keith G Watson

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21

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publication date

June 2013

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published in

Nature Chemical Biology

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volume

9

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issue

6

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page(s)

390-7

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cites work

New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

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

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Still embedded together binding to membranes regulates Bcl-2 protein interactions.

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BCL-2 family antagonists for cancer therapy

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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inferred from PubMed ID database lookup

The combined functions of proapoptotic Bcl-2 family members bak and bax are essential for normal development of multiple tissues

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PubMed

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12 December 2020

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Phasercrystallographic software

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PubMed

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Bcl-2 family proteins as therapeutic targets

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Integration, scaling, space-group assignment and post-refinement

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

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PubMed

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

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PubMed

reference URL

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12 December 2020

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Differential targeting of prosurvival Bcl-2 proteins by their BH3-only ligands allows complementary apoptotic function

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PubMed

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12 December 2020

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

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PubMed

reference URL

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12 December 2020

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Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer

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PubMed

reference URL

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Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo

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Bcl-2 gene promotes haemopoietic cell survival and cooperates with c-myc to immortalize pre-B cells

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PubMed

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12 December 2020

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Bcl-2 family proteins are essential for platelet survival.

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Rationale for Bcl-xL/Bad peptide complex formation from structure, mutagenesis, and biophysical studies

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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The landscape of somatic copy-number alteration across human cancers

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Generation of a set of simple, interpretable ADMET rules of thumb

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Refinement of macromolecular structures by the maximum-likelihood method

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural biology of the Bcl-2 family of proteins

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Conformational Changes in Bcl-2 Pro-survival Proteins Determine Their Capacity to Bind Ligands

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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inferred from PubMed ID database lookup

Structural plasticity underpins promiscuous binding of the prosurvival protein A1

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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An informatics approach identifying markers of chemosensitivity in human cancer cell lines.

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Protein-protein interaction inhibitors get into the groove

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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PHENIX: a comprehensive Python-based system for macromolecular structure solution

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Programmed anuclear cell death delimits platelet life span.

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Apoptosis initiated when BH3 ligands engage multiple Bcl-2 homologs, not Bax or Bak

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Apoptosis is triggered when prosurvival Bcl-2 proteins cannot restrain Bax.

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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inferred from PubMed ID database lookup

Crystal structure of ABT-737 complexed with Bcl-xL: implications for selectivity of antagonists of the Bcl-2 family

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease

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PubMed

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12 December 2020

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inferred from PubMed ID database lookup

Vaccinia virus anti-apoptotic F1L is a novel Bcl-2-like domain-swapped dimer that binds a highly selective subset of BH3-containing death ligands

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

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Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

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The role of Bcl-2 and its pro-survival relatives in tumourigenesis and cancer therapy

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The structure of a Bcl-xL/Bim fragment complex: implications for Bim function

1 reference

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Crystal structure of the Bcl-XL-Beclin 1 peptide complex: Beclin 1 is a novel BH3-only protein

1 reference

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeting the Bcl-2-regulated apoptosis pathway by BH3 mimetics: a breakthrough in anticancer therapy?

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stated in

PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Megakaryocytes possess a functional intrinsic apoptosis pathway that must be restrained to survive and produce platelets

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Coot: model-building tools for molecular graphics

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PubMed

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https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

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Deciphering the rules of programmed cell death to improve therapy of cancer and other diseases

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Reaching for high-hanging fruit in drug discovery at protein-protein interfaces

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins

1 reference

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Embedded together: the life and death consequences of interaction of the Bcl-2 family with membranes

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

retrieved

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Cell death

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Proapoptotic Bak is sequestered by Mcl-1 and Bcl-xL, but not Bcl-2, until displaced by BH3-only proteins

1 reference

stated in

PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure of Bcl-xL-Bak peptide complex: recognition between regulators of apoptosis

1 reference

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Novel primitive lymphoid tumours induced in transgenic mice by cooperation between myc and bcl-2.

1 reference

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PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

stated in

PubMed

reference URL

https://pubmed.ncbi.nlm.nih.gov/23603658

retrieved

12 December 2020

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Processing of X-ray diffraction data collected in oscillation mode

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Crossref

reference URL

https://api.crossref.org/works/10.1038%2FNCHEMBIO.1246

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7 January 2021

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Identifiers

DOI

10.1038/NCHEMBIO.1246

1 reference

stated in

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

867334

Dimensions Publication ID

1044425895

0 references

OpenCitations bibliographic resource ID

867334

1 reference

stated in

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

867334

PubMed publication ID

23603658

1 reference

stated in

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

867334

ResearchGate publication ID

236252326

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