D. Sampath

发表

Design of new anticancer therapies targeting cell cycle checkpoint pathways

W. Plunkett, D. Sampath, 2001, Current opinion in oncology.

Metabolite profiling stratifies pancreatic ductal adenocarcinomas into subtypes with distinct sensitivities to metabolic inhibitors

Anneleen Daemen, Deepak Sampath, Gerard Manning, 2015, Proceedings of the National Academy of Sciences.

Killing of Chronic Lymphocytic Leukemia by the Combination of Fludarabine and Oxaliplatin Is Dependent on the Activity of XPF Endonuclease

W. Plunkett, D. Sampath, Alma Zecevic, 2011, Clinical Cancer Research.

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

L. Lam, C. Tse, Cheol‐Min Park, 2013, Nature Medicine.

Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

D. Sampath, P. Dragovich, T. O'Brien, 2015, Toxicological sciences : an official journal of the Society of Toxicology.

Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Karl H. Clodfelter, P. Bauer, N. Kley, 2013, Bioorganic & medicinal chemistry letters.

Patterns for RANTES Secretion and Intercellular Adhesion Molecule 1 Expression Mediate Transepithelial T Cell Traffic Based on Analyses In Vitro and In Vivo

D. Sampath, M. Holtzman, D. Look, 1998, The Journal of experimental medicine.

Venetoclax plus R- or G-CHOP in non-Hodgkin lymphoma: results from the CAVALLI phase 1b trial.

G. Salles, L. Sehn, A. Zelenetz, 2019, Blood.

220 POSTER Combination of class I PI3K inhibitor, GDC-0941, with standard of care therapeutics results in enhanced anti-tumor responses in human cancer models in vitro and in vivo

M. Belvin, L. Friedman, D. Sampath, 2008 .

217 POSTER Pre-clinical evaluation of efficacy and PK/PD biomarkers of GDC-0941, a potent class 1 PI3K inhibitor

M. Belvin, L. Friedman, H. Stern, 2008 .

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

C. Li, R. Rowntree, BinQing Wei, 2019, Bioorganic & medicinal chemistry letters.

The one-two of T helper cells: does interferon-gamma knock out the Th2 hypothesis for asthma?

D. Sampath, M. Holtzman, D. Look, 1996, American journal of respiratory cell and molecular biology.

Anti-tumor NAMPT inhibitor, KPT-9274, mediates gender-dependent murine anemia and nephrotoxicity by regulating SIRT3-mediated SOD deacetylation

J. Byrd, D. Sampath, Pu Zhang, 2021, Journal of Hematology & Oncology.

HSP90 inhibition depletes DNA repair proteins to sensitize acute myelogenous leukemia to nucleoside analog chemotherapeutics

J. Byrd, V. Puduvalli, W. Plunkett, 2019, Leukemia and Lymphoma.

The spectrum of incomplete N-linked oligosaccharides synthesized by endothelial cells in the presence of brefeldin A.

A. Varki, H. Freeze, D. Sampath, 1992, The Journal of biological chemistry.

Cyr61, a Member of the CCN Family, Is Required for MCF-7 Cell Proliferation: Regulation by 17β-Estradiol and Overexpression in Human Breast Cancer.

R. Winneker, D. Sampath, Zhiming Zhang, 2001, Endocrinology.

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Jane R Kenny, Michael Siu, Deepak Sampath, 2012, Journal of medicinal chemistry.

Abstract A20: Development and validation of a novel acute myeloid leukemia xenograft model that is dependent on the JAK2V617F mutation for growth in vivo

Leslie B. Lee, Christine Chang, D. Sampath, 2009 .

H2AX phosphorylation marks gemcitabine-induced stalled replication forks and their collapse upon S-phase checkpoint abrogation

W. Plunkett, D. Sampath, B. Ewald, 2007, Molecular Cancer Therapeutics.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors.

M. Belvin, L. Friedman, Leslie B. Lee, 2010, Cancer research.

Vorinostat modulates cell cycle regulatory proteins in glioma cells and human glioma slice cultures

G. Fuller, G. Rao, F. Lang, 2011, Journal of Neuro-Oncology.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

C. Ly, S. Sideris, S. Malek, 2012, Journal of medicinal chemistry.

Distinct resistance mechanisms arise to allosteric vs. ATP-competitive AKT inhibitors

Scott E. Martin, F. Gnad, Zhaoshi Jiang, 2022, Nature Communications.

HDAC1 regulates the chromatin landscape to establish transcriptional dependencies in chronic lymphocytic leukemia

J. Byrd, P. Gasparini, G. Nigita, 2020, bioRxiv.

Souers AJ, Leverson JD, Boghaert ER et al.ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med 19:202-208

L. Lam, C. Tse, Cheol‐Min Park, 2013 .

Tumour‐secreted miR‐9 promotes endothelial cell migration and angiogenesis by activating the JAK‐STAT pathway

Zhaoshi Jiang, I. Kasman, Z. Modrušan, 2012, The EMBO journal.

Convergent genetic aberrations in murine and human T lineage acute lymphoblastic leukemias

J. Downing, B. Taylor, A. Daemen, 2019, PLoS genetics.

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

Monitoring and Targeting Anti-VEGF Induced Hypoxia within the Viable Tumor by 19F–MRI and Multispectral Analysis

M. Hedehus, F. Peale, R. Carano, 2017, Neoplasia.

Preclinical Development The Bcl-2 / Bcl-XL / Bcl-w Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

The role of c-Jun kinase in the apoptotic response to nucleoside analogue-induced DNA damage.

W. Plunkett, D. Sampath, 2000, Cancer research.

BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.

Lindsey T. Brinton, J. Byrd, G. Habets, 2018, Cancer discovery.

Cancer Therapy: Preclinical TargetingActivatedAktwithGDC-0068, aNovel SelectiveAkt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013 .

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Jun Liang, J. Blake, B. Brandhuber, 2012, Journal of medicinal chemistry.

A Novel Mutagenesis Strategy Identifies Distantly Spaced Amino Acid Sequences That Are Required for the Phosphorylation of Both the Oligosaccharides of Procathepsin D by N-Acetylglucosamine 1-Phosphotransferase (*)

Michael Loran Dustin, T. Baranski, S. Kornfeld, 1995, The Journal of Biological Chemistry.

Alpha- and beta-xylosides alter glycolipid synthesis in human melanoma and Chinese hamster ovary cells.

A. Varki, H. Freeze, D. Sampath, 1993, The Journal of biological chemistry.

Neutralization of BCL-2/XL Enhances the Cytotoxicity of T-DM1 In Vivo

R. Bronson, D. Dillon, J. Brugge, 2019, Molecular Cancer Therapeutics.

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

An anti-B7-H4 antibody-drug conjugate for the treatment of breast cancer.

J. DeVoss, T. Pham, Cécile Chalouni, 2015, Molecular pharmaceutics.

Aberrant expression of Cyr61, a member of the CCN (CTGF/Cyr61/Cef10/NOVH) family, and dysregulation by 17 beta-estradiol and basic fibroblast growth factor in human uterine leiomyomas.

R. Winneker, D. Sampath, Z. Zhang, 2001, The Journal of clinical endocrinology and metabolism.

Cyr61, a member of the CCN family, is required for MCF-7 cell proliferation: regulation by 17beta-estradiol and overexpression in human breast cancer.

R. Winneker, D. Sampath, Z. Zhang, 2001, Endocrinology.

Therapeutic Strategies that Overcome Resistance to Nucleoside Analogues: Dysregulating Checkpoint Response and Survival Pathways by UCN-01

W. Plunkett, D. Sampath, Zheng Shi, 2003 .

Inhibition of cyclin-dependent kinase 2 by the Chk1-Cdc25A pathway during the S-phase checkpoint activated by fludarabine: dysregulation by 7-hydroxystaurosporine.

W. Plunkett, D. Sampath, Zheng Shi, 2002, Molecular pharmacology.

Uncoupling of chondroitin sulfate glycosaminoglycan synthesis by brefeldin A

H. Freeze, D. Sampath, R. C. Spiro, 1991, The Journal of cell biology.

Control of epithelial immune-response genes and implications for airway immunity and inflammation.

D. Sampath, M. Holtzman, D. Look, 1998, Proceedings of the Association of American Physicians.

Cotargeting BCL-2 and PI3K Induces BAX-Dependent Mitochondrial Apoptosis in AML Cells.

S. Grant, J. Leverson, M. Rahmani, 2018, Cancer research.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Nuclear Phospho-Akt Increase Predicts Synergy of PI3K Inhibition and Doxorubicin in Breast and Ovarian Cancer

M. Belvin, L. Friedman, D. Sampath, 2010, Science Translational Medicine.

Venetoclax Increases Intratumoral Effector T Cells and Antitumor Efﬁ cacy in Combination with Immune Checkpoint Blockade

Salem, P. Ellis, J. Leverson, 2020 .

Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2020, ACS medicinal chemistry letters.

MAC-321, a novel taxane with greater efficacy than paclitaxel and docetaxel in vitro and in vivo.

F. Loganzo, D. Sampath, C. Discafani, 2003, Molecular cancer therapeutics.

S-Phase arrest by nucleoside analogues and abrogation of survival without cell cycle progression by 7-hydroxystaurosporine.

W. Plunkett, P. Huang, Ye Li, 2001, Cancer research.

Mapping in vivo tumor oxygenation within viable tumor by 19F-MRI and multispectral analysis.

N. van Bruggen, M. Hedehus, F. Peale, 2013, Neoplasia.

Mapping In Vivo Tumor Oxygenation within Viable

M. Hedehus, F. Peale, N. Bruggen, 2013 .

Abstract S6-04: The PI3K inhibitor, taselisib, has enhanced potency in PIK3CA mutant models through a unique mechanism of action

Kyung Song, L. Friedman, D. Sampath, 2016 .

Shielding p53 from destruction.

D. Sampath, 2018, Blood.

Antitumor activity of ipatasertib combined with chemotherapy: results from a phase Ib study in solid tumors.

J. Soria, J. Bendell, D. Sampath, 2020, Annals of oncology : official journal of the European Society for Medical Oncology.

Dialing resistance up a Notch

V. Gandhi, D. Sampath, 2009, Leukemia & lymphoma.

The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.

Lisa L. Smith, J. Byrd, F. Awan, 2018, Cancer discovery.

Targeting BTK through microRNA in chronic lymphocytic leukemia.

Lisa L. Smith, J. Byrd, A. Bottoni, 2016, Blood.

LYMPHOID NEOPLASIA Targeting BTK through microRNA in chronic lymphocytic leukemia

Lisa L. Smith, J. Byrd, A. Bottoni, 2016 .

TP53‐altered chronic lymphocytic leukemia treated with firstline Bruton's tyrosine kinase inhibitor‐based therapy: A retrospective analysis

Z. Estrov, R. Kanagal-Shamanna, M. Keating, 2022, American journal of hematology.

Coding and noncoding: the CLL mix.

G. Calin, D. Sampath, 2010, Blood.

Therapy for older patients with acute myeloblastic leukemia: a problem in search of a solution

G. Garcia-Manero, D. Sampath, 2012, Leukemia & lymphoma.

Supplementation of nicotinic acid with NAMPT inhibitors results in loss of in vivo efficacy in NAPRT1-deficient tumor models.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

Targeting OXPHOS de novo purine synthesis as the nexus of FLT3 inhibitor–mediated synergistic antileukemic actions

J. Blachly, R. Baiocchi, D. Sampath, 2022, Science advances.

MYELOID NEOPLASIA Preclinical ef ﬁ cacy of MEK inhibition in Nras -mutant AML

S. Lowe, J. Zuber, Jin Xu, 2014 .

Expression of PRMT5 in B-Cell Chronic Lymphocytic Leukemia and Its Significance in Disease Progression and Richter's Transformation

J. Byrd, Lianbo Yu, R. Baiocchi, 2014 .

Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Inhibition and Biomarker Modulation by the Novel PI3K Inhibitor 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4- morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941)

M. Belvin, D. Sampath, K. Edgar, 2010 .

86OPI3 kinase/mTOR inhibition increases sensitivity of ER positive breast cancers to CDK4/6 inhibition by blocking cell cycle re-entry driven by cyclinD1 and inducing apoptosis

M. Dowsett, D. Sampath, U. Asghar, 2015 .

Preclinical assessment of the ADME, efficacy and drug-drug interaction potential of a novel NAMPT inhibitor

D. Sampath, P. Dragovich, B. Liederer, 2019, Xenobiotica; the fate of foreign compounds in biological systems.

Cardiotoxicity Associated with Nicotinamide Phosphoribosyltransferase Inhibitors in Rodents and in Rat and Human-Derived Cells Lines

A. Bruening-Wright, D. Sampath, P. Dragovich, 2017, Cardiovascular Toxicology.

Preclinical evaluation of combination nemtabrutinib and venetoclax in chronic lymphocytic leukemia

J. Byrd, Lianbo Yu, D. Sampath, 2022, Journal of Hematology & Oncology.

Multimodal microvascular imaging reveals that selective inhibition of class I PI3K is sufficient to induce an antivascular response.

N. van Bruggen, H. Koeppen, L. Friedman, 2013, Neoplasia.

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)

C. Tse, D. Anderson, Daniel J. Anderson, 2015, Cell Death and Disease.

Evaluation of allogeneic and autologous membrane-bound IL-21–expanded NK cells for chronic lymphocytic leukemia therapy

D. Sampath, X. Mo, K. Rogers, 2022, Blood advances.

Abstract 964: Inhibiting glycolysis with an LDHA inhibitor: A new solution to an old problem

Marie Evangelista, G. Hatzivassiliou, D. Sampath, 2014 .

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013, Clinical Cancer Research.

Modulation of Ara-C Metabolism to Improve AML Response

M. Ayers, W. Plunkett, M. Keating, 1998 .

Assays on DNA Damage and Repair in CLL.

D. Sampath, Tzung-Huei Lai, 2018, Methods in molecular biology.

The role of DNA repair in chronic lymphocytic leukemia pathogenesis and chemotherapy resistance

W. Plunkett, D. Sampath, 2007, Current Oncology Reports.

miRs: fine-tuning prognosis in CLL.

G. Calin, D. Sampath, 2009, Blood.

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.

Marie Evangelista, A. Daemen, W. Sandoval, 2018, Cell metabolism.

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

D. Sutherlin, S. Sideris, Leslie B. Lee, 2011, Bioorganic & medicinal chemistry letters.

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

M. Ultsch, C. Eigenbrot, Leslie B. Lee, 2013, Bioorganic & medicinal chemistry letters.

Selective targeting of NAMPT by KPT-9274 in acute myeloid leukemia.

J. Byrd, Pratibha Sharma, E. Baloglu, 2019, Blood advances.

Phosphoproteomic Analysis Implicates the mTORC2-FoxO1 Axis in VEGF Signaling and Feedback Activation of Receptor Tyrosine Kinases

Zhaoshi Jiang, Deepak Sampath, Elizabeth Blackwood, 2013, Science Signaling.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

D. Sutherlin, L. Friedman, Leslie B. Lee, 2010, Bioorganic & medicinal chemistry letters.

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Dolores Diaz, Jun Chen, Deepak Sampath, 2015, Science Translational Medicine.

Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3′ Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models

M. Belvin, D. Guhathakurta, L. Amler, 2010, Clinical Cancer Research.

Nucleoside analogs: molecular mechanisms signaling cell death

W. Plunkett, D. Sampath, B. Ewald, 2008, Oncogene.

Human melanoma and Chinese hamster ovary cells galactosylate n-alkyl-β-glucosides using UDP gal:GlcNAc β1,4 galactosyltransferase

H. Freeze, D. Sampath, J. Etchison, 1996 .

Loss of oncogenic Notch1 with resistance to a PI3K inhibitor in T-cell leukaemia

J. Downing, J. Aster, W. Pear, 2014, Nature.

Preclinical Pharmacologic Evaluation of MST-997, an Orally Active Taxane with Superior In vitro and In vivo Efficacy in Paclitaxel- and Docetaxel-Resistant Tumor Models

Deepak Sampath, Carol Rios, D. Sampath, 2006, Clinical Cancer Research.

XPO1 Inhibition using Selinexor Synergizes with Chemotherapy in Acute Myeloid Leukemia by Targeting DNA Repair and Restoring Topoisomerase IIα to the Nucleus

R. Garzon, D. Sampath, W. Blum, 2016, Clinical Cancer Research.

Mechanisms of apoptosis induction by nucleoside analogs

W. Plunkett, D. Sampath, V. A. Rao, 2003, Oncogene.

microRNA fingerprinting of CLL patients with chromosome 17p deletion identify a miR-21 score that stratifies early survival.

George A Calin, Kevin R Coombes, Muller Fabbri, 2010, Blood.

Phase I clinical, pharmacokinetic, and pharmacodynamic study of the Akt-inhibitor triciribine phosphate monohydrate in patients with advanced hematologic malignancies.

H. Kantarjian, G. Garcia-Manero, S. Verstovsek, 2013, Leukemia research.

Fludarabine increases oxaliplatin cytotoxicity in normal and chronic lymphocytic leukemia lymphocytes by suppressing interstrand DNA crosslink removal.

W. Plunkett, M. Keating, D. Sampath, 2006, Blood.

Machine-Learning and Chemicogenomics Approach Defines and Predicts Cross-Talk of Hippo and MAPK Pathways

Thijs J. Hagenbeek, Mamie Yu, Z. Modrušan, 2021 .

Hippo pathway dysregulation occurs in multiple cancers through genetic and non-genetic alterations resulting in translocation of YAP to the nucleus and activation of the TEAD family of transcription

Zora, Thijs J. Hagenbeek, Mamie Yu, 2020 .

Bcl-2/Bcl-xL Inhibition Increases the Efficacy of MEK Inhibition Alone and in Combination with PI3 Kinase Inhibition in Lung and Pancreatic Tumor Models

J. Settleman, Leslie B. Lee, W. Fairbrother, 2013, Molecular Cancer Therapeutics.

MicroRNA in Leukemias

D. Sampath, 2013 .

Association of a microRNA/TP53 feedback circuitry with pathogenesis and outcome of B-cell chronic lymphocytic leukemia.

George A Calin, Muller Fabbri, Massimo Negrini, 2011, JAMA.

Association of a MicroRNA / TP 53 Feedback Circuitry With Pathogenesis and Outcome of B-Cell Chronic Lymphocytic Leukemia

D. Amadori, C. Croce, R. Spizzo, 2010 .

HDAC Inhibition Induces MicroRNA-182, which Targets RAD51 and Impairs HR Repair to Sensitize Cells to Sapacitabine in Acute Myelogenous Leukemia

R. Garzon, W. Plunkett, J. Blachly, 2016, Clinical Cancer Research.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility

Mamie Yu, A. Daemen, R. Houtman, 2019, Cell.

Inhibition of nicotinamide phosphoribosyltransferase, the rate-limiting enzyme of the nicotinamide adenine dinucleotide salvage pathway, to target glioma heterogeneity through mitochondrial oxidative stress.

Pratibha Sharma, F. Lang, R. Lonser, 2021, Neuro-oncology.

Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas

F. S. Abas, M. Gurcan, J. Gumin, 2017, Clinical Cancer Research.

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011, Molecular Cancer Therapeutics.

GDC-0980IsaNovelClassIPI3K/mTORKinaseInhibitorwith RobustActivityinCancerModelsDrivenbythePI3KPathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011 .

Evaluation and Clinical Analyses of Downstream Targets of the Akt Inhibitor GDC-0068

G. Hampton, J. Baselga, J. Tabernero, 2013, Clinical Cancer Research.

Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941.

M. Sliwkowski, L. Friedman, D. Sampath, 2009, Cancer cell.

Histone deacetylases mediate the silencing of miR-15a, miR-16, and miR-29b in chronic lymphocytic leukemia.

V. Puduvalli, M. Keating, D. Sampath, 2012, Blood.

VCAM-1 Density and Tumor Perfusion Predict T-cell Infiltration and Treatment Response in Preclinical Models12

M. Hedehus, R. Carano, D. Sampath, 2019, Neoplasia.

Found in Translation: How Preclinical Research Is Guiding the Clinical Development of the BCL2-Selective Inhibitor Venetoclax.

A. Letai, M. Amiot, M. Konopleva, 2017, Cancer discovery.

Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models

M. Amiot, F. Peale, Leslie B. Lee, 2016, Molecular Cancer Therapeutics.

KRAS Allelic Imbalance Enhances Fitness and Modulates MAP Kinase Dependence in Cancer

B. Taylor, S. Asthana, M. L. Beau, 2017, Cell.

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Siew K. Yeap, M. Ultsch, C. Eigenbrot, 2022, Journal of medicinal chemistry.

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

W. Forrest, Kyung Song, L. Friedman, 2021, bioRxiv.

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

M. Belvin, A. Daemen, BinQing Wei, 2016, Nature chemical biology.

Flavopiridol enhances ABT-199 sensitivity in unfavourable-risk multiple myeloma cells in vitro and in vivo

S. Grant, R. Orlowski, J. Leverson, 2017, British Journal of Cancer.

Expression of Bcl-2 Pro-Survival Family Proteins Predicts Pharmacological Responses to ABT-199, a Novel and Selective Bcl-2 Antagonist, in Multiple Myeloma Models

F. Peale, Leslie B. Lee, W. Fairbrother, 2012 .

Resistance To Taxanes

D. Sampath, L. Greenberger, 2006 .

The Kinase Activity of Hematopoietic Progenitor Kinase 1 Is Essential for the Regulation of T Cell Function.

I. Mellman, S. Warming, Min Xu, 2018, Cell reports.

Amphiregulin and PTEN evoke a multimodal mechanism of acquired resistance to PI3K inhibition

R. Neve, M. Belvin, T. Wilson, 2014, Genes & cancer.

Phosphoinositide 3-Kinase (PI3K) Pathway Alterations Are Associated with Histologic Subtypes and Are Predictive of Sensitivity to PI3K Inhibitors in Lung Cancer Preclinical Models

G. Hampton, J. Fridlyand, J. Spoerke, 2012, Clinical Cancer Research.

GDC-0941, a Novel Class I Selective PI3K Inhibitor, Enhances the Efficacy of Docetaxel in Human Breast Cancer Models by Increasing Cell Death In Vitro and In Vivo

M. Belvin, H. Koeppen, L. Friedman, 2012, Clinical Cancer Research.

Cancer Therapy: Preclinical GDC-0941, a Novel Class I Selective PI3K Inhibitor, Enhances the Efficacy of Docetaxel in Human Breast CancerModels by Increasing Cell Death In Vitro and In Vivo

M. Belvin, H. Koeppen, L. Friedman, 2012 .

Explaining Gene Expression Using Twenty-One MicroRNAs

Amir H. Asiaee, Zachary B. Abrams, K. Coombes, 2019, J. Comput. Biol..

miRNAs and their potential for use against cancer and other diseases.

G. Calin, W. Plunkett, V. Gandhi, 2007, Future oncology.

PLC-γ and PI3K Link Cytokines to ERK Activation in Hematopoietic Cells with Normal and Oncogenic Kras

K. Shokat, K. Shannon, G. Bollag, 2013, Science Signaling.

PI 3 K Link Cytokines to ERK Activation in Hematopoietic Cells with Normal and Oncogenic Kras

K. Shokat, K. Shannon, G. Bollag, 2013 .

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer.

Deepak Sampath, Tanja S. Zabka, D. Sampath, 2015, Pharmacology & therapeutics.

Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway renders them sensitive to NAMPT inhibition with GNE-618.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

Concomitant targeting of BCL2 with venetoclax and MAPK signaling with cobimetinib in acute myeloid leukemia models

Jing Wang, M. Konopleva, M. Andreeff, 2019, Haematologica.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents in vitro and in vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

Systems analysis of apoptotic priming in ovarian cancer identifies vulnerabilities and predictors of drug response

G. Mills, R. Drapkin, J. Brugge, 2017, Nature Communications.

Navitoclax Enhances the Efficacy of Taxanes in Non–Small Cell Lung Cancer Models

J. Zha, W. Fairbrother, L. Berry, 2011, Clinical Cancer Research.

Pharmacodynamics of cytarabine alone and in combination with 7-hydroxystaurosporine (UCN-01) in AML blasts in vitro and during a clinical trial.

Z. Estrov, M. Andreeff, J. Cortes, 2006, Blood.

Preclinical evaluation of the Hsp90 inhibitor SNX-5422 in ibrutinib resistant CLL

J. Byrd, R. Baiocchi, D. Sampath, 2021, Journal of Hematology & Oncology.

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

K. Walter, Andiliy G. Lai, J. Giltnane, 2016, eLife.

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

D. Sutherlin, S. Sideris, Irina S. Chuckowree, 2010, Bioorganic & medicinal chemistry letters.

Venetoclax combines synergistically with FLT3 inhibition to effectively target leukemic cells in FLT3-ITD+ acute myeloid leukemia models

M. Konopleva, D. Sampath, Qi Zhang, 2020, Haematologica.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011, Molecular Cancer Therapeutics.

Single-Cell Dynamics Determines Response to CDK4/6 Inhibition in Triple-Negative Breast Cancer

C. Bakal, J. Giltnane, A. Barr, 2017, Clinical Cancer Research.

Targeting deubiquitinases in CLL.

D. Sampath, 2017, Blood.

Identification and comparison of genes differentially regulated by transcription factors and miRNAs

Amir H. Asiaee, Zachary B. Abrams, K. Coombes, 2019, bioRxiv.

Eμ-TCL1xMyc: A Novel Mouse Model for Concurrent CLL and B-Cell Lymphoma

Lisa L. Smith, J. Byrd, R. Bundschuh, 2019, Clinical Cancer Research.

The long noncoding RNA, treRNA, decreases DNA damage and is associated with poor response to chemotherapy in chronic lymphocytic leukemia

M. Grever, K. Coombes, I. Flinn, 2017, OncoTarget.

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Siew K. Yeap, N. C. Ray, Jun Liang, 2021, Journal of medicinal chemistry.

Disruption of DNA Repair and Survival Pathways through Heat Shock Protein inhibition by Onalespib to Sensitize Malignant Gliomas to Chemoradiation therapy.

F. Lang, J. Elder, R. Lonser, 2022, Clinical cancer research : an official journal of the American Association for Cancer Research.

The angiogenic factor Cyr61 is induced by the progestin R5020 and is necessary for mammary adenocarcinoma cell growth

R. Winneker, D. Sampath, Zhiming Zhang, 2002, Endocrine.

Preclinical efficacy of MEK inhibition in Nras-mutant AML.

S. Lowe, J. Zuber, Jin Xu, 2014, Blood.

Resistance of Natural Killer and T Cells to Venetoclax Allows for Combination Treatment with Cancer Immunotherapy Agents

M. Belvin, L. Molinero, D. Sampath, 2018, Blood.

VIP152 is a selective CDK9 inhibitor with pre-clinical in vitro and in vivo efficacy in chronic lymphocytic leukemia

J. Byrd, A. Johnson, J. Blachly, 2022, Leukemia.

Targeting the PI3K/Akt pathway in murine MDS/MPN driven by hyperactive Ras

L. Friedman, D. Sampath, B. Braun, 2016, Leukemia.

Targeting MCL‐1 and BCL‐2 with polatuzumab vedotin and venetoclax overcomes treatment resistance in R/R non‐Hodgkin lymphoma: Results from preclinical models and a Phase Ib study

Dhara N. Amin, N. Johnson, M. Krem, 2023, American journal of hematology.

Discovery and Development of Venetoclax, a Selective Antagonist ofBCL‐2

W. Fairbrother, J. Leverson, D. Sampath, 2019, Successful Drug Discovery.

Development and comparison of nonradioactive in vitro kinase assays for NIMA-related kinase 2.

R. Kriz, D. Sampath, J. Pocas, 2006, Analytical biochemistry.

ATM and the Mre11-Rad50-Nbs1 complex respond to nucleoside analogue-induced stalled replication forks and contribute to drug resistance.

W. Plunkett, D. Sampath, B. Ewald, 2008, Cancer research.

Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Inhibition and Biomarker Modulation by the Novel Phosphatidylinositol 3-Kinase Inhibitor GDC-0941

Deepak Sampath, Harvey Wong, M. Belvin, 2010, Drug Metabolism and Disposition.

Metabolic response of prostate cancer to nicotinamide phophoribosyltransferase inhibition in a hyperpolarized MR/PET compatible bioreactor

J. Kurhanewicz, David M. Wilson, H. VanBrocklin, 2015, The Prostate.

Constitutive activation of an epithelial signal transducer and activator of transcription (STAT) pathway in asthma.

D. Sampath, M. Holtzman, D. Look, 1999, The Journal of clinical investigation.

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors.

J. Baselga, T. Wilson, J. Ware, 2017, Cancer discovery.

Targeting DNA Damage Repair Functions of Two Histone Deacetylases, HDAC8 and SIRT6, Sensitizes Acute Myeloid Leukemia to NAMPT Inhibition

J. Byrd, S. Kulp, J. Blachly, 2021, Clinical Cancer Research.

Phase I Dose Escalation Study of Taselisib (GDC-0032), an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors

Sandra, J. Baselga, T. Wilson, 2017 .

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.

N. Skelton, D. Sampath, K. Bair, 2016, Journal of medicinal chemistry.

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Karl H. Clodfelter, N. Skelton, D. Sampath, 2015, Bioorganic & medicinal chemistry letters.

Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human

Leslie B. Lee, D. Sampath, E. Plise, 2012, Drug Metabolism and Disposition.

Novel BCL2 mutations in venetoclax-resistant, ibrutinib-resistant CLL patients with BTK/PLCG2 mutations.

J. Byrd, G. Lozanski, J. Blachly, 2020, Blood.

Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Yang Xiao, Lei Zhang, Deepak Sampath, 2013, Bioorganic & medicinal chemistry letters.

Venetoclax increases intra-tumoral effector T cells and anti-tumor efficacy in combination with immune checkpoint blockade.

P. Ellis, J. Leverson, T. Uziel, 2020, Cancer Discovery.

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

Xiaohong Song, Z. Tao, P. Kovar, 2020, ACS medicinal chemistry letters.

Venetoclax, Obinutuzumab and Atezolizumab (PD-L1 Checkpoint Inhibitor) for Treatment for Patients with Richter Transformation

Naveen Garg, Xiaoping Su, M. Konopleva, 2021, Blood.

Loss of glucocorticoid receptor expression mediates in vivo dexamethasone resistance in T-cell acute lymphoblastic leukemia

J. Downing, B. Taylor, J. Aster, 2020, Leukemia.

Combined MEK and BCL-2/XL Inhibition Is Effective in High-Grade Serous Ovarian Cancer Patient–Derived Xenograft Models and BIM Levels Are Predictive of Responsiveness

G. Mills, V. Velculescu, R. Drapkin, 2019, Molecular Cancer Therapeutics.

Structure-based Optimization of Hydroxylactam as Potent, Cell-Active Inhibitors of Lactate Dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2022, Bioorganic & medicinal chemistry letters.

Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2021, Bioorganic & medicinal chemistry letters.

Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development

M. Belvin, Kyung Song, L. Friedman, 2017 .

Chemical Therapeutics Bcl-2 / Bcl-xL Inhibition Increases the Ef fi cacy of MEK InhibitionAlone and inCombinationwith PI 3 Kinase Inhibition in Lung and Pancreatic Tumor Models

J. Settleman, Leslie B. Lee, W. Fairbrother, 2013 .

Preclinical models of nicotinamide phosphoribosyltransferase inhibitor-mediated hematotoxicity and mitigation by co-treatment with nicotinic acid

Dolores Diaz, Deepak Sampath, Hirdesh Uppal, 2015, Toxicology mechanisms and methods.

Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors

D. Sampath, K. Bair, Weiru Wang, 2014, PloS one.

Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes

A. Daemen, J. Giltnane, L. Friedman, 2019, Poster Session Abstracts.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Steve Price, M. Belvin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.

Jun Liang, J. Nwachukwu, K. Nettles, 2019, Bioorganic & medicinal chemistry letters.

Targeting Venetoclax Resistant CLL Using a Protac-Based BCL-2/BCL-XL Degrader

D. Sampath, N. Jain, W. Wierda, 2022, Blood.

Abstract 1648: Discovery and evolution of orally bioavailable selective estrogen receptor degraders for ER+ breast cancer: From GDC-0810 to GDC-0927

Jun Liang, A. Daemen, Andiliy G. Lai, 2018, Cancer Chemistry.

Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.

R. Rowntree, B. Vollmar, I. Wertz, 2018, Chemistry.

An Anti-GDNF Family Receptor Alpha 1 (GFRA1) Antibody–Drug Conjugate for the Treatment of Hormone Receptor–Positive Breast Cancer

R. Scheller, Robert Piskol, D. Sampath, 2017, Molecular Cancer Therapeutics.

Abstract P2-17-01: The PI3K inhibitor GDC-0032 is selectively potent against PIK3CA mutant breast cancer cell lines and tumors

M. Belvin, L. Friedman, D. Sampath, 2013 .

FLT3-ITD Activation Mediates Resistance to the BCL-2 Selective Antagonist, Venetoclax, in FLT3-ITD Mutant AML Models

J. Leverson, D. Sampath, E. A. Lasater, 2017 .

Role and regulation of microRNAs targeting BTK in acute myelogenous leukemia

C. Bloomfield, J. Byrd, A. Bottoni, 2018, Leukemia & lymphoma.

Venetoclax, Obinutuzumab and Atezolizumab (PD-L1 Checkpoint Inhibitor) for First-Line Treatment for Patients with Chronic Lymphocytic Leukemia (CLL)

Naveen Garg, Xiaoping Su, M. Konopleva, 2021, Blood.

Characterization of LP-118, a Novel Small Molecule Inhibitor of Bcl-2 and Bcl-Xl in Chronic Lymphocytic Leukemia Resistant to Venetoclax

J. Byrd, D. Sampath, S. Anthony, 2021, Blood.

The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t(11;14) multiple myeloma

M. Amiot, C. Pellat-deceunynck, M. Béné, 2013, Leukemia.

HDAC1 regulates the chromatin landscape to control transcriptional dependencies in chronic lymphocytic leukemia

P. Gasparini, G. Nigita, S. Shukla, 2022, Blood advances.

Targeting MAPK Signaling Pathway with Cobimetinib (GDC-0973) Enhances Anti-Leukemia Efficacy of Venetoclax (ABT-199/GDC-0199) in Acute Myeloid Leukemia Models

M. Konopleva, M. Andreeff, H. Kantarjian, 2016 .

Combination of the glycoengineered Type II CD20 antibody obinutuzumab (GA101) and The novel Bcl-2 selective Inhibitor GDC-0199 Results in superior In Vitro and In Vivo Anti-tumor activity in models Of B-Cell Malignancies

C. Klein, M. Bacac, W. Fairbrother, 2013 .

MiRly regulating metabolism.

D. Sampath, 2012, Blood.

Abstract CT133: Targeting BCL-2 and MCL-1 overcomes treatment resistance in relapsed and refractory non-Hodgkin lymphoma: Pre-clinical rationale and results from an open-label phase 1b study

Dhara N. Amin, C. Flowers, M. Krem, 2020 .

Abstract A245: Combination of the glycoengineered Type II CD20 antibody obinutuzumab (GA101), and the novel Bcl-2 selective inhibitor, ABT-199 (GDC-0199), results in superior in vitro and in vivo anti-tumor activity in models of B-cell malignancies.

C. Klein, M. Bacac, W. Fairbrother, 2013 .

Abstract P4-15-02: The PI3K inhibitor GDC-0032 enhances the efficacy of standard of care therapeutics in PI3K alpha mutant breast cancer models

M. Belvin, L. Friedman, D. Sampath, 2013 .

Histone deacetylases mediate the silencing of miR-15a, miR-16, and miR-29b in chronic lymphocytic leukemia.

V. Puduvalli, M. Keating, D. Sampath, 2012, Blood.

Response: Context-dependent actions of miR-106b in CLL

W. Plunkett, D. Sampath, 2009 .

Combined MEK and BCL-2/XL Inhibition Is Effective in High-Grade Serous Ovarian Cancer Patient–Derived Xenograft Models and BIM Levels Are Predictive of Responsiveness

G. Mills, V. Velculescu, R. Drapkin, 2019, Molecular Cancer Therapeutics.

Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models

M. Amiot, F. Peale, Leslie B. Lee, 2016, Molecular Cancer Therapeutics.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

H. Maecker, S. Rosenberg, J. Leverson, 2011, Molecular Cancer Therapeutics.

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.

A. Daemen, W. Sandoval, G. Hatzivassiliou, 2018, Cell metabolism.

Machine learning and chemico-genomics approach defines and predicts cross-talk of Hippo and MAPK pathways.

Thijs J. Hagenbeek, Mamie Yu, Z. Modrušan, 2020, Cancer discovery.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility

Mamie Yu, A. Daemen, R. Houtman, 2019, Cell.

Phosphoinositide 3-Kinase (PI3K) Pathway Alterations Are Associated with Histologic Subtypes and Are Predictive of Sensitivity to PI3K Inhibitors in Lung Cancer Preclinical Models

G. Hampton, J. Fridlyand, J. Spoerke, 2012, Clinical Cancer Research.

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer.

D. Sampath, P. Dragovich, T. O'Brien, 2015, Pharmacology & therapeutics.

Metabolic response of prostate cancer to nicotinamide phophoribosyltransferase inhibition in a hyperpolarized MR/PET compatible bioreactor

J. Kurhanewicz, David M. Wilson, H. VanBrocklin, 2015, The Prostate.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Phase I Study of the Akt-Inhibitor Triciribine Phosphate Monohydrate in Patients with Advanced Hematologic Malignancy

H. Kantarjian, G. Garcia-Manero, S. Verstovsek, 2008 .

Comparison of clinical and molecular characteristics of patients with acute myeloid leukemia and either TP73 or TP53 mutations

C. Bloomfield, J. Byrd, J. Kolitz, 2020, Leukemia.

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors.

J. Baselga, J. Ware, D. Juric, 2017, Cancer discovery.

Evaluation and Clinical Analyses of Downstream Targets of the Akt Inhibitor GDC-0068

G. Hampton, J. Baselga, J. Tabernero, 2013, Clinical Cancer Research.