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

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med (2013) 8.89

BAX activation is initiated at a novel interaction site. Nature (2008) 6.07

The double-edged sword of autophagy modulation in cancer. Clin Cancer Res (2009) 5.46

Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease. J Clin Oncol (2011) 5.14

Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res (2009) 4.53

Targeting mitochondria for cancer therapy. Nat Rev Drug Discov (2010) 4.07

Rapamycin passes the torch: a new generation of mTOR inhibitors. Nat Rev Drug Discov (2011) 4.05

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. Lancet Oncol (2010) 3.76

Concurrent expression of MYC and BCL2 in diffuse large B-cell lymphoma treated with rituximab plus cyclophosphamide, doxorubicin, vincristine, and prednisone. J Clin Oncol (2012) 3.59

Control of mitochondrial apoptosis by the Bcl-2 family. J Cell Sci (2009) 3.54

Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer models. Cancer Cell (2012) 3.39

BIM expression in treatment-naive cancers predicts responsiveness to kinase inhibitors. Cancer Discov (2011) 3.34

Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors. J Clin Oncol (2011) 3.33

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer. Nat Chem Biol (2010) 3.17

Deciphering the rules of programmed cell death to improve therapy of cancer and other diseases. EMBO J (2011) 3.06

Selective BCL-2 inhibition by ABT-199 causes on-target cell death in acute myeloid leukemia. Cancer Discov (2013) 2.74

Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1. Blood (2010) 2.61

Translating p53 into the clinic. Nat Rev Clin Oncol (2010) 2.55

Relative mitochondrial priming of myeloblasts and normal HSCs determines chemotherapeutic success in AML. Cell (2012) 2.51

An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules. Cell (2013) 2.30

Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer. Clin Cancer Res (2012) 2.26

Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem (2012) 2.23

A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers. J Clin Invest (2012) 2.17

Mimicking the BH3 domain to kill cancer cells. Oncogene (2008) 2.14

Targeting the B-cell lymphoma/leukemia 2 family in cancer. J Clin Oncol (2012) 2.09

A20: from ubiquitin editing to tumour suppression. Nat Rev Cancer (2010) 2.08

Inhibition of α-helix-mediated protein-protein interactions using designed molecules. Nat Chem (2013) 2.02

Unleashing the power of inhibitors of oncogenic kinases through BH3 mimetics. Nat Rev Cancer (2009) 2.02

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells. Proc Natl Acad Sci U S A (2011) 2.01

Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. Chem Biol (2014) 1.95

A competitive stapled peptide screen identifies a selective small molecule that overcomes MCL-1-dependent leukemia cell survival. Chem Biol (2012) 1.94

Chemical genomics identifies small-molecule MCL1 repressors and BCL-xL as a predictor of MCL1 dependency. Cancer Cell (2012) 1.93

Clearance of senescent cells by ABT263 rejuvenates aged hematopoietic stem cells in mice. Nat Med (2015) 1.88

Bcl-2 antagonists interact synergistically with bortezomib in DLBCL cells in association with JNK activation and induction of ER stress. Cancer Biol Ther (2009) 1.88

A survey of the anti-apoptotic Bcl-2 subfamily expression in cancer types provides a platform to predict the efficacy of Bcl-2 antagonists in cancer therapy. Cell Death Dis (2010) 1.87

High mitochondrial priming sensitizes hESCs to DNA-damage-induced apoptosis. Cell Stem Cell (2013) 1.86

Getting TRAIL back on track for cancer therapy. Cell Death Differ (2014) 1.86

In vivo efficacy of the Bcl-2 antagonist ABT-737 against aggressive Myc-driven lymphomas. Proc Natl Acad Sci U S A (2008) 1.83

Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells. Blood (2012) 1.81

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). Cell Death Dis (2015) 1.77

Bcl2 family proteins in carcinogenesis and the treatment of cancer. Apoptosis (2009) 1.72

ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia. Blood (2013) 1.72

Structure-guided design of a selective BCL-X(L) inhibitor. Nat Chem Biol (2013) 1.68

BRAF inhibitor resistance mediated by the AKT pathway in an oncogenic BRAF mouse melanoma model. Proc Natl Acad Sci U S A (2015) 1.67

TORC1 suppression predicts responsiveness to RAF and MEK inhibition in BRAF-mutant melanoma. Sci Transl Med (2013) 1.67

Many players in BCL-2 family affairs. Trends Biochem Sci (2014) 1.64

A computationally designed inhibitor of an Epstein-Barr viral Bcl-2 protein induces apoptosis in infected cells. Cell (2014) 1.62

Delving deeper: MCL-1's contributions to normal and cancer biology. Trends Cell Biol (2012) 1.60

Actinomycin D synergistically enhances the efficacy of the BH3 mimetic ABT-737 by downregulating Mcl-1 expression. Cancer Biol Ther (2010) 1.57

BCL2A1: the underdog in the BCL2 family. Cell Death Differ (2011) 1.56

Building blocks of the apoptotic pore: how Bax and Bak are activated and oligomerize during apoptosis. Cell Death Differ (2013) 1.54

Combined Bcl-2/mammalian target of rapamycin inhibition leads to enhanced radiosensitization via induction of apoptosis and autophagy in non-small cell lung tumor xenograft model. Clin Cancer Res (2009) 1.53

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. J Biol Chem (2012) 1.53

Multiple functions of BCL-2 family proteins. Cold Spring Harb Perspect Biol (2013) 1.51

A threshold mechanism mediates p53 cell fate decision between growth arrest and apoptosis. Cell Death Differ (2013) 1.50

Apoptosis and molecular targeting therapy in cancer. Biomed Res Int (2014) 1.47

Distribution of Bim determines Mcl-1 dependence or codependence with Bcl-xL/Bcl-2 in Mcl-1-expressing myeloma cells. Blood (2011) 1.47

Bim upregulation by histone deacetylase inhibitors mediates interactions with the Bcl-2 antagonist ABT-737: evidence for distinct roles for Bcl-2, Bcl-xL, and Mcl-1. Mol Cell Biol (2009) 1.46

Sensitization of BCL-2-expressing breast tumors to chemotherapy by the BH3 mimetic ABT-737. Proc Natl Acad Sci U S A (2011) 1.45

Array comparative genomic hybridization-based characterization of genetic alterations in pulmonary neuroendocrine tumors. Proc Natl Acad Sci U S A (2010) 1.45

p21-activated kinase 1: PAK'ed with potential. Oncotarget (2011) 1.44

MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignancies. Cell Death Dis (2015) 1.44

Mitochondria: gatekeepers of response to chemotherapy. Trends Cell Biol (2013) 1.44

Alternative Treatments For Melanoma: Targeting BCL-2 Family Members to De-Bulk and Kill Cancer Stem Cells. J Invest Dermatol (2015) 1.43

Potent and specific peptide inhibitors of human pro-survival protein Bcl-xL. J Mol Biol (2014) 1.42

A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther (2013) 1.42

Thirty years of BCL-2: translating cell death discoveries into novel cancer therapies. Nat Rev Cancer (2016) 1.42

Intracellular delivery of a proapoptotic peptide via conjugation to a RAFT synthesized endosomolytic polymer. Mol Pharm (2010) 1.38

The BCL-2 protein family, BH3-mimetics and cancer therapy. Cell Death Differ (2015) 1.38

Autophagy suppresses RIP kinase-dependent necrosis enabling survival to mTOR inhibition. PLoS One (2012) 1.37

Determinants of BH3 binding specificity for Mcl-1 versus Bcl-xL. J Mol Biol (2010) 1.37

Decoding and unlocking the BCL-2 dependency of cancer cells. Nat Rev Cancer (2013) 1.36

Bim and Bmf in tissue homeostasis and malignant disease. Oncogene (2008) 1.36

Histone deacetylase inhibitor (HDACI) mechanisms of action: emerging insights. Pharmacol Ther (2014) 1.35

Emerging Bcl-2 inhibitors for the treatment of cancer. Expert Opin Emerg Drugs (2010) 1.32

Mitochondrial signaling in cell death via the Bcl-2 family. Cancer Biol Ther (2010) 1.30

MEK inhibition enhances ABT-737-induced leukemia cell apoptosis via prevention of ERK-activated MCL-1 induction and modulation of MCL-1/BIM complex. Leukemia (2011) 1.30

Direct and selective small-molecule activation of proapoptotic BAX. Nat Chem Biol (2012) 1.30

Robust generation of lead compounds for protein-protein interactions by computational and MCR chemistry: p53/Hdm2 antagonists. Angew Chem Int Ed Engl (2010) 1.29

The rheostat in the membrane: BCL-2 family proteins and apoptosis. Cell Death Differ (2013) 1.29

Navitoclax (ABT-263) accelerates apoptosis during drug-induced mitotic arrest by antagonizing Bcl-xL. Cancer Res (2011) 1.27

A phase I study of obatoclax mesylate, a Bcl-2 antagonist, plus topotecan in solid tumor malignancies. Cancer Chemother Pharmacol (2010) 1.26

Strategies for optimizing the response of cancer and normal tissues to radiation. Nat Rev Drug Discov (2013) 1.25

Noxa/Bcl-2 protein interactions contribute to bortezomib resistance in human lymphoid cells. J Biol Chem (2011) 1.24

Mcl-1-Bim complexes accommodate surprising point mutations via minor structural changes. Protein Sci (2010) 1.24

Small molecule Mcl-1 inhibitors for the treatment of cancer. Pharmacol Ther (2014) 1.23

NMR strategy for unraveling structures of bioactive sponge-derived oxy-polyhalogenated diphenyl ethers. J Nat Prod (2009) 1.23

BH3-only proteins in apoptosis at a glance. J Cell Sci (2012) 1.23

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett (2014) 1.23

The Role of BH3-Only Proteins in Tumor Cell Development, Signaling, and Treatment. Genes Cancer (2011) 1.23

BH3 mimetics antagonizing restricted prosurvival Bcl-2 proteins represent another class of selective immune modulatory drugs. Proc Natl Acad Sci U S A (2010) 1.22

mTOR inhibition specifically sensitizes colorectal cancers with KRAS or BRAF mutations to BCL-2/BCL-XL inhibition by suppressing MCL-1. Cancer Discov (2013) 1.21

Inhibition of a viral enzyme by a small-molecule dimer disruptor. Nat Chem Biol (2009) 1.21

Epidermal growth factor regulates Mcl-1 expression through the MAPK-Elk-1 signalling pathway contributing to cell survival in breast cancer. Oncogene (2011) 1.20

TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer Res (2009) 1.20

The Role of BCL2 Family of Apoptosis Regulator Proteins in Acute and Chronic Leukemias. Adv Hematol (2011) 1.20

Mitochondria-mediated apoptosis in mammals. Protein Cell (2014) 1.19

Mcl1 downregulation sensitizes neuroblastoma to cytotoxic chemotherapy and small molecule Bcl2-family antagonists. Cancer Biol Ther (2009) 1.18

Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy. PLoS One (2011) 1.18

Evading apoptosis in cancer. Trends Cell Biol (2013) 1.17

An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature (2005) 22.40

Linking long-term dietary patterns with gut microbial enterotypes. Science (2011) 17.30

Intestinal microbiota metabolism of L-carnitine, a nutrient in red meat, promotes atherosclerosis. Nat Med (2013) 9.44

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med (2013) 8.89

ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res (2007) 5.75

Sampling and pyrosequencing methods for characterizing bacterial communities in the human gut using 16S sequence tags. BMC Microbiol (2010) 4.97

Systematic identification of C. elegans miRISC proteins, miRNAs, and mRNA targets by their interactions with GW182 proteins AIN-1 and AIN-2. Mol Cell (2007) 4.22

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. Lancet Oncol (2010) 3.76

Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway. Science (2003) 3.59

Proinflammatory cytokine expression profile in degenerated and herniated human intervertebral disc tissues. Arthritis Rheum (2010) 3.45

The human gut virome: inter-individual variation and dynamic response to diet. Genome Res (2011) 3.32

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737. Cancer Res (2007) 3.24

siRNA-mediated off-target gene silencing triggered by a 7 nt complementation. Nucleic Acids Res (2005) 3.21

The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution. J Biol Chem (2004) 3.18

Microglia/macrophage polarization dynamics reveal novel mechanism of injury expansion after focal cerebral ischemia. Stroke (2012) 2.88

An open conformation of mammalian cytochrome P450 2B4 at 1.6-A resolution. Proc Natl Acad Sci U S A (2003) 2.74

Joint analysis of two microarray gene-expression data sets to select lung adenocarcinoma marker genes. BMC Bioinformatics (2004) 2.73

Functional materials for rechargeable batteries. Adv Mater (2011) 2.71

Structure of mammalian cytochrome P450 2B4 complexed with 4-(4-chlorophenyl)imidazole at 1.9-A resolution: insight into the range of P450 conformations and the coordination of redox partner binding. J Biol Chem (2004) 2.66

Disordered microbial communities in the upper respiratory tract of cigarette smokers. PLoS One (2010) 2.60

Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen. Nat Struct Mol Biol (2005) 2.54

The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther (2011) 2.48

Liver transplantation for hepatocellular carcinoma: Hangzhou experiences. Transplantation (2008) 2.48

Interactions between S4-S5 linker and S6 transmembrane domain modulate gating of HERG K+ channels. J Biol Chem (2002) 2.34

Novel synthesis of 1-aroyl-3-aryl-4-substituted imidazole-2-thiones. Org Lett (2003) 2.30

The structure of human cytochrome P450 2C9 complexed with flurbiprofen at 2.0-A resolution. J Biol Chem (2004) 2.24

Critical role of calpain I in mitochondrial release of apoptosis-inducing factor in ischemic neuronal injury. J Neurosci (2007) 2.23

Acute kidney injury during warfarin therapy associated with obstructive tubular red blood cell casts: a report of 9 cases. Am J Kidney Dis (2009) 2.21

Chk1 mediates S and G2 arrests through Cdc25A degradation in response to DNA-damaging agents. J Biol Chem (2003) 2.18

Enhanced oligodendrogenesis and recovery of neurological function by erythropoietin after neonatal hypoxic/ischemic brain injury. Stroke (2010) 2.18

The BMP-binding protein Crossveinless 2 is a short-range, concentration-dependent, biphasic modulator of BMP signaling in Drosophila. Dev Cell (2008) 2.17

Replacement of Oct4 by Tet1 during iPSC induction reveals an important role of DNA methylation and hydroxymethylation in reprogramming. Cell Stem Cell (2013) 2.17

Neuroprotective effects of leptin against ischemic injury induced by oxygen-glucose deprivation and transient cerebral ischemia. Stroke (2007) 2.15

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther (2005) 2.15

In Vivo Delivery of a Bcl-xL Fusion Protein Containing the TAT Protein Transduction Domain Protects against Ischemic Brain Injury and Neuronal Apoptosis. J Neurosci (2002) 2.12

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res (2008) 2.10

Relief of extrinsic pathway inhibition by the Bid-dependent mitochondrial release of Smac in Fas-mediated hepatocyte apoptosis. J Biol Chem (2002) 2.10

Efficacy of erythropoietin combined with enteral nutrition for the treatment of anemia in Crohn's disease: a prospective cohort study. Nutr Clin Pract (2012) 2.10

Correlation between resistance and field emission performance of individual ZnO one-dimensional nanostructures. ACS Nano (2008) 2.10

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem (2007) 2.09

Structure of human microsomal cytochrome P450 2C8. Evidence for a peripheral fatty acid binding site. J Biol Chem (2003) 2.09

Quasicrystalline order in self-assembled binary nanoparticle superlattices. Nature (2009) 2.08

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J Med Chem (2004) 2.05

Gastric intestinal metaplasia with basal gland atypia: a morphological and biologic evaluation in a large Chinese cohort. Hum Pathol (2012) 2.04

HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A (2007) 2.03

Waist circumference correlates with metabolic syndrome indicators better than percentage fat. Obesity (Silver Spring) (2006) 2.00

Calicivirus translation initiation requires an interaction between VPg and eIF 4 E. EMBO Rep (2005) 1.98

Mechanobiology of the intervertebral disc and relevance to disc degeneration. J Bone Joint Surg Am (2006) 1.96

Adaptations for the oxidation of polycyclic aromatic hydrocarbons exhibited by the structure of human P450 1A2. J Biol Chem (2007) 1.96

The oncoprotein LMO2 is expressed in normal germinal-center B cells and in human B-cell lymphomas. Blood (2006) 1.94

Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res (2011) 1.91

Human Chk1 expression is dispensable for somatic cell death and critical for sustaining G2 DNA damage checkpoint. Mol Cancer Ther (2003) 1.90

Navigating the kinome. Nat Chem Biol (2011) 1.88

Endothelial dysfunction in ischemic acute renal failure: rescue by transplanted endothelial cells. Am J Physiol Renal Physiol (2002) 1.85

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem (2008) 1.85

Practice guidelines for videoconferencing-based telemental health - October 2009. Telemed J E Health (2010) 1.83

Rechargeable Mg batteries with graphene-like MoS₂ cathode and ultrasmall Mg nanoparticle anode. Adv Mater (2010) 1.79

Breaking tolerance to the natural human liver autoantigen cytochrome P450 2D6 by virus infection. J Exp Med (2008) 1.76

Metal-air batteries: from oxygen reduction electrochemistry to cathode catalysts. Chem Soc Rev (2012) 1.75

Mechanism responsible for initiating carbon nanotube vacuum breakdown. Phys Rev Lett (2004) 1.74