S. Kasibhatla

发表

Why target apoptosis in cancer treatment?

S. Kasibhatla, B. Tseng, Shailaja Kasibhatla, 2003, Molecular cancer therapeutics.

DNA damaging agents induce expression of Fas ligand and subsequent apoptosis in T lymphocytes via the activation of NF-kappa B and AP-1.

D. Green, S. Kasibhatla, T. Brunner, 1998, Molecular cell.

Regulation of FasL by NF-κB and AP-1 in Fas-dependent Thymineless Death of Human Colon Carcinoma Cells*

D. Green, J. Houghton, F. G. Harwood, 2000, The Journal of Biological Chemistry.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.

William E. Kemnitzer, H. Gourdeau, S. Kasibhatla, 2008, Journal of medicinal chemistry.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 7- and 5-, 6-, 8-positions.

William E. Kemnitzer, H. Gourdeau, S. Kasibhatla, 2005, Bioorganic & medicinal chemistry letters.

Discovery and mechanism of action of a novel series of apoptosis inducers with potential vascular targeting activity.

L. Qiu, K. Meerovitch, H. Gourdeau, 2004, Molecular cancer therapeutics.

A conserved domainofthelarge subunit of replication factor CbindsPCNAandactslike a dominant negative inhibitor ofDNA replication in

G. Maga, U. Hübscher, S. Kasibhatla, 1996 .

31st Annual Meeting and Associated Programs of the Society for Immunotherapy of Cancer (SITC 2016): part two

Manish R. Patel, Charles J. Vaske, Joe Y. Chang, 2016, Journal for Immunotherapy of Cancer.

MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity

S. Kasibhatla, S. Cai, Jin-Cheng Huang, 2003, British journal of pharmacology.

Antivascular and antitumor evaluation of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4H-chromenes, a novel series of anticancer agents.

H. Gourdeau, S. Kasibhatla, L. Geerts, 2004, Molecular cancer therapeutics.

Discovery of 4-aryl-2-oxo-2H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay.

William E. Kemnitzer, H. Gourdeau, S. Kasibhatla, 2008, Bioorganic & medicinal chemistry letters.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 3. Structure-activity relationships of fused rings at the 7,8-positions.

William E. Kemnitzer, H. Gourdeau, S. Kasibhatla, 2007, Journal of medicinal chemistry.

Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors.

Jennifer L. Harris, S. Kasibhatla, D. Han, 2016, ACS medicinal chemistry letters.

MPC-6827: a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps.

S. Skvortsov, S. Kasibhatla, V. Baichwal, 2007, Cancer research.

Transforming Growth Factor β1 Inhibits Fas Ligand Expression and Subsequent Activation-induced Cell Death in T Cells via Downregulation of c-Myc

D. Green, S. Kasibhatla, T. Brunner, 1999, The Journal of experimental medicine.

Synthesis of caged 2,3,3a,7a-tetrahydro-3,6-methanobenzofuran-7(6H)-ones: Evaluating the minimum structure for apoptosis induction by gambogic acid.

S. Kasibhatla, S. Cai, J. Drewe, 2008, Bioorganic & medicinal chemistry.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based HTS assay. Part 5: modifications of the 2- and 3-positions.

William E. Kemnitzer, H. Gourdeau, S. Kasibhatla, 2008, Bioorganic & medicinal chemistry letters.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.

William E. Kemnitzer, K. Meerovitch, H. Gourdeau, 2004, Journal of medicinal chemistry.

Propidium Iodide (PI) Uptake Assay to Detect Apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

N-Ac-DEVD-N'-(Polyfluorobenzoyl)-R110: novel cell-permeable fluorogenic caspase substrates for the detection of caspase activity and apoptosis.

S. Kasibhatla, S. Cai, J. Drewe, 2003, Bioconjugate chemistry.

Simultaneous involvement of all six predicted antigen binding loops of the T cell receptor in recognition of the MHC/antigenic peptide complex.

A. Rao, S. Kasibhatla, E. A. Nalefski, 1993, Journal of immunology.

Analysis of DNA fragmentation using agarose gel electrophoresis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay.

S. Kasibhatla, J. Herich, S. Cai, 2004, Bioorganic & medicinal chemistry.

Protein kinase ctheta cooperates with calcineurin to induce Fas ligand expression during activation-induced T cell death.

D. Green, A. Altman, S. Kasibhatla, 1999, Journal of immunology.

Synergistic action of protein kinase C θ and calcineurin is sufficient for Fas ligand expression and induction of a crmA‐sensitive apoptosis pathway in Jurkat T cells

R. Greil, D. Green, I. Tinhofer, 1999, European journal of immunology.

A ‘non-canonical’ DNA-binding element mediates the response of the Fas-ligand promoter to c-Myc

D. Green, S. Kasibhatla, T. Brunner, 2000, Current Biology.

Expression of Fas Ligand in Activated T Cells Is Regulated by c-Myc*

D. Green, N. Yoo, S. Kasibhatla, 2000, The Journal of Biological Chemistry.

Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. Part 1: Structure-activity relationships of the 1- and 3-positions.

William E. Kemnitzer, S. Kasibhatla, Candace Crogan-Grundy, 2008, Bioorganic & medicinal chemistry letters.

During Activation-Induced T Cell Death Calcineurin to Induce Fas Ligand Expression Cooperates with q Protein Kinase C

D. Green, A. Altman, S. Kasibhatla, 1999 .

TUNEL Staining of Tissue Sections to Detect Apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

Analysis of DNA Fragmentation Using Propidium Iodide (PI) Fluorescence of Individual Nuclei.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

MET gene amplification is a mechanism of resistance to entrectinib in ROS1+ NSCLC

T. Wilson, R. Doebele, A. Le, 2022, Thoracic cancer.

Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.

William E. Kemnitzer, S. Kasibhatla, S. Cai, 2009, Bioorganic & medicinal chemistry letters.

Discovery and structure-activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers.

L. Qiu, A. Estevez, P. Sabbatini, 2006, Bioorganic & medicinal chemistry letters.

Analysis of TUNEL Staining by Flow Cytometry to Detect Apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

TUNEL Staining of Adherent Cells to Detect Apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents.

L. Qiu, William E. Kemnitzer, S. Kasibhatla, 2005, Journal of medicinal chemistry.

Discovery of 5-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-(E)-2,3,6,7-tetrahydro-1,4-thiazepines as a new series of apoptosis inducers using a cell- and caspase-based HTS assay.

S. Kasibhatla, S. Cai, David Sperandio, 2007, Bioorganic & Medicinal Chemistry Letters.

Selective activation of apoptosis by a novel set of 4-aryl-3-(3-aryl-1-oxo-2-propenyl)-2(1H)-quinolinones through a Myc-dependent pathway.

M. Vaillancourt, S. Kasibhatla, Candace Crogan-Grundy, 2009, Cancer letters.

Discovery of substituted 4-anilino-2-(2-pyridyl)pyrimidines as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. Part 1: structure-activity relationships of the 4-anilino group.

S. Kasibhatla, Yang Wang, S. Cai, 2006, Bioorganic & medicinal chemistry.

A chemical genetics approach for the discovery of apoptosis inducers: from phenotypic cell based HTS assay and structure-activity relationship studies, to identification of potential anticancer agents and molecular targets.

S. Kasibhatla, S. Cai, J. Drewe, 2006, Current medicinal chemistry.

Discovery of substituted N-phenyl nicotinamides as potent inducers of apoptosis using a cell- and caspase-based high throughput screening assay.

S. Kasibhatla, J. Herich, S. Cai, 2003, Journal of medicinal chemistry.

The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.

Makoto Nishio, Peter McNamara, Ryohei Katayama, 2014, Cancer discovery.

Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.

Mark B. Anderson, S. Kasibhatla, S. Cai, 2009, Journal of medicinal chemistry.

Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.

William E. Kemnitzer, S. Kasibhatla, Candace Crogan-Grundy, 2009, Bioorganic & medicinal chemistry letters.

Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.

Mark B. Anderson, S. Kasibhatla, V. Baichwal, 2008, Journal of medicinal chemistry.

Discovery and SAR of indole-2-carboxylic acid benzylidene-hydrazides as a new series of potent apoptosis inducers using a cell-based HTS assay.

S. Kasibhatla, S. Cai, J. Drewe, 2004, Bioorganic & medicinal chemistry.

Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.

William E. Kemnitzer, S. Kasibhatla, Candace Crogan-Grundy, 2009, Bioorganic & medicinal chemistry letters.

Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the carboxamide group.

William E. Kemnitzer, S. Kasibhatla, Candace Crogan-Grundy, 2009, Bioorganic & medicinal chemistry letters.

Staining of suspension cells with hoechst 33258 to detect apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

Acridine Orange/Ethidium Bromide (AO/EB) Staining to Detect Apoptosis.

D. Green, E. Bossy‐Wetzel, S. Kasibhatla, 2006, CSH protocols.

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Ce

Chun Xing Li, S. Bender, G. Spraggon, 2016, Journal of medicinal chemistry.

A role for transferrin receptor in triggering apoptosis when targeted with gambogic acid.

D. Green, L. Qiu, S. Kasibhatla, 2005, Proceedings of the National Academy of Sciences of the United States of America.

Quantitative Systems Pharmacology Modeling of Avadomide-Induced Neutropenia Enables Virtual Clinical Dose and Schedule Finding Studies

C. C. Santini, M. Trotter, A. Ratushny, 2021, The AAPS Journal.

Inhibition of tumor growth progression by antiandrogens and mTOR inhibitor in a Pten-deficient mouse model of prostate cancer.

P. Majumder, S. Kasibhatla, M. Angagaw, 2009, Cancer research.

PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models.

K. Kunii, R. Bronson, M. Scott, 2011, Cancer research.

Therapeutics , Targets , and Chemical Biology PDK 1 Attenuation Fails to Prevent Tumor Formation in PTEN-Deficient Transgenic Mouse Models

Hare, K. Kunii, R. Bronson, 2011 .

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974

W. Sellers, P. Schultz, Jennifer L. Harris, 2013, Proceedings of the National Academy of Sciences.

Phosphoglycerate dehydrogenase is dispensable for breast tumor maintenance and growth

S. Jaeger, Guizhi Yang, S. Kasibhatla, 2013, Oncotarget.

Combined ALK and MDM2 inhibition increases antitumor activity and overcomes resistance in human ALK mutant neuroblastoma cell lines and xenograft models

W. Sellers, Nanxin Li, D. Ruddy, 2017, eLife.

EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

J. Barretina, Jennifer L. Harris, J. Engelman, 2016, Cancer research.

Jun Kinase Phosphorylates and Regulates the DNA Binding Activity of an Octamer Binding Protein, T-Cell Factor β1

T. Mustelin, A. Fotedar, A. Altman, 1999, Molecular and Cellular Biology.

Partial Cleavage of RasGAP by Caspases Is Required for Cell Survival in Mild Stress Conditions

Seamus J. Martin, D. Michod, C. Widmann, 2004, Molecular and Cellular Biology.

Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma.

Nanxin Li, J. Shaffer, S. Kasibhatla, 2020, ACS medicinal chemistry letters.

Regulation of Fas-Ligand Expression during Activation-induced Cell Death in T Lymphocytes via Nuclear Factor κB*

D. Green, S. Kasibhatla, L. Genestier, 1999, The Journal of Biological Chemistry.

Functional Analysis of the Antigen Binding Site on the T Cell Receptor c ~ Chain

A. Rao, S. Kasibhatla, E. A. Nalefski, 2003 .

Functional analysis of the antigen binding site on the T cell receptor alpha chain

A. Rao, S. Kasibhatla, E. A. Nalefski, 1992, The Journal of experimental medicine.

The c-Jun N-terminal kinase cascade plays a role in stress-induced apoptosis in Jurkat cells by up-regulating Fas ligand expression.

D. Green, A. Nel, G. Koretzky, 1998, Journal of immunology.

Up-Regulating Fas Ligand Expression Role in Stress-Induced Apoptosis in Jurkat Cells The c-Jun N-Terminal Kinase Cascade Plays a

D. Green, A. Nel, G. Koretzky, 1997 .

A conserved domain of the large subunit of replication factor C binds PCNA and acts like a dominant negative inhibitor of DNA replication in mammalian cells.

G. Maga, R. Fotedar, A. Fotedar, 1996, The EMBO journal.

Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.

Mark B. Anderson, S. Kasibhatla, S. Cai, 2010, Bioorganic & medicinal chemistry letters.

Abstract 4128: Identification and characterization of LHC165, a TLR7 agonist designed for localized intratumoral therapies

S. Bender, N. Parikh, S. Kasibhatla, 2019, Immunology.

Abstract 2585: Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816

C. Li, S. Kasibhatla, I. Matushansky, 2015 .

Abstract 1734:In vitrocharacterization of EGF816, a third-generation mutant-selective EGFR inhibitor

Jennifer L. Harris, S. Bender, N. Pathan, 2014 .

Abstract 1733: EGF816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes T790M-mediated resistance in NSCLC

S. Bender, M. Vaillancourt, S. Kasibhatla, 2014 .

The discovery and mechanism of action of novel tumor-selective and apoptosis-inducing 3,5-diaryl-1,2,4-oxadiazole series using a chemical genetics approach

L. Qiu, S. Kasibhatla, S. Cai, 2005, Molecular Cancer Therapeutics.

Why target apoptosis in cancer treatment?

S. Kasibhatla, B. Tseng, 2003, Molecular cancer therapeutics.

31st Annual Meeting and Associated Programs of the Society for Immunotherapy of Cancer (SITC 2016): part two

Charles J. Vaske, Joe Y. Chang, Scott R. Presnell, 2016, Journal for ImmunoTherapy of Cancer.

Transforming Growth Factor β1 Inhibits Fas Ligand Expression and Subsequent Activation-induced Cell Death in T Cells via Downregulation of c-Myc

D. Green, S. Kasibhatla, T. Brunner, 1999, The Journal of experimental medicine.

Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors.

Nanxin Li, J. Shaffer, S. Kasibhatla, 2021, ACS medicinal chemistry letters.