S. Gross

发表

Small molecule activation of PKM2 in cancer cells induces serine auxotrophy.

L. Cantley, C. Kung, J. Hixon, 2012, Chemistry & biology.

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

L. Liau, M. V. Heiden, L. Cantley, 2009, Nature.

Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations

Tak W. Mak, Lenny Dang, Masato Sasaki, 2010, The Journal of experimental medicine.

Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.

Shaomeng Wang, S. Gross, J. Stuckey, 2021, Journal of Medicinal Chemistry.

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis.

A. Kernytsky, S. Choe, K. Marks, 2016, Cell reports.

Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells

S. Gross, Z. Estrov, M. Andreeff, 2009, Leukemia.

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.

Hua Yang, Fang Wang, Zenon Konteatis, 2017, Cancer discovery.

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

S. Gross, Giovanni Cianchetta, Cheng Fang, 2018, ACS medicinal chemistry letters.

A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model

A. Kernytsky, Yaguang Si, S. Gross, 2016, Journal of Inherited Metabolic Disease.

ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells

Mindy I. Davis, S. Gross, L. Dang, 2013 .

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

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

ALDH2(E487K) mutation increases protein turnover and promotes murine hepatocarcinogenesis

T. Mak, C. Kung, J. Hixon, 2015, Proceedings of the National Academy of Sciences.

A potential therapeutic target for FLT3-ITD AML: PIM1 kinase.

J. E. Robinson, S. Gross, M. Levis, 2012, Leukemia research.

Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.

K. Marks, S. Gross, Z. Sui, 2022, Journal of Medicinal Chemistry.

Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo.

S. Gross, J. Blake, K. Davies, 2011, Oncology research.

Chk1 inhibition and Wee1 inhibition combine synergistically to impede cellular proliferation

S. Gross, K. Davies, J. Garrus, 2011, Cancer biology & therapy.

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

L. Liau, M. V. Heiden, L. Cantley, 2010, Nature.

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.

Discovery and SAR of spirochromane Akt inhibitors.

Tyler T. Risom, S. Gross, J. Blake, 2011, Bioorganic & medicinal chemistry letters.

Selective Inhibition of Mutant Isocitrate Dehydrogenase 1 (IDH1) via Disruption of a Metal Binding Network by an Allosteric Small Molecule

Dietmar Hoffmann, Jean-Pierre Marquette, Magali Mathieu, 2014, The Journal of Biological Chemistry.

Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Tyler Risom, Zhaoyang Wen, Ignacio Aliagas, 2011, ACS medicinal chemistry letters.

Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

S. Gross, Giovanni Cianchetta, Cheng Fang, 2019, Nature Communications.

Preclinical toxicology profile of squalene epoxidase inhibitors.

S. Gross, T. Roddy, A. Olaharski, 2020, Toxicology and applied pharmacology.

Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

S. Gross, Giovanni Cianchetta, Cheng Fang, 2019, Nature Communications.

AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency.

Yaguang Si, C. Kung, J. Hixon, 2017, Blood.

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

Fang Wang, Erica Hansen, Francesco G. Salituro, 2013, Science.

Transformation by the R Enantiomer of 2-Hydroxyglutarate Linked to EglN Activation

R. Verhaak, K. Ligon, Hai Yan, 2012, Nature.

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.

S. Gross, Shunqi Yan, J. Saunders, 2012, ACS medicinal chemistry letters.

Mutant IDH is sufficient to initiate enchondromatosis in mice

B. Alman, S. Inoue, T. Mak, 2015, Proceedings of the National Academy of Sciences.

MAT2A inhibition blocks the growth of MTAP-deleted cancer cells by reducing PRMT5-dependent mRNA splicing and inducing DNA damage.

W. Liu, K. Marks, S. Gross, 2021, Cancer cell.

Biological Characterization of ARRY-142886 (AZD6244), a Potent, Highly Selective Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor

Vivienne Marsh, S. Gross, B. Brandhuber, 2007, Clinical Cancer Research.

Targeting cancer with kinase inhibitors.

Nicolas Stransky, Christoph Lengauer, Nicolas Stransky, 2015, The Journal of clinical investigation.

PIM inhibitors target CD25-positive AML cells through concomitant suppression of STAT5 activation and degradation of MYC oncogene.

S. Gross, Q. Gao, D. Wiederschain, 2014, Blood.

suppression of STAT 5 activation and degradation of MYC oncogene PIM inhibitors target CD 25-positive AML cells through concomitant

S. Gross, Q. Gao, D. Wiederschain, 2014 .

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Tyler T. Risom, S. Gross, J. Blake, 2011, Bioorganic & medicinal chemistry letters.

Mesenchymal Phenotype Predisposes Lung Cancer Cells to Impaired Proliferation and Redox Stress in Response to Glutaminase Inhibition

Abhishek K. Jha, S. Choe, S. Gross, 2014, Cancer & Metabolism.

Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia.

K. Pradhan, S. Gross, A. Verma, 2016, Cancer research.

Distinct Hepatic PKA and CDK Signaling Pathways Control Activity-Independent Pyruvate Kinase Phosphorylation and Hepatic Glucose Production.

Karl W Barber, Kshitiz, G. Shulman, 2019, Cell reports.

Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

S. Gross, Giovanni Cianchetta, Cheng Fang, 2019, Nature Communications.

A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition

S. Choe, K. Marks, S. Gross, 2019, Nature Communications.

Abstract 3504: A chemical biology screen identifies a unique vulnerability of neuroendocrine cancer cells to SQLE inhibition

S. Choe, S. Gross, Giovanni Cianchetta, 2018, Molecular and Cellular Biology / Genetics.

Biochemical, Cellular, and Biophysical Characterization of a Potent Inhibitor of Mutant Isocitrate Dehydrogenase IDH1*

Mindy I. Davis, S. Gross, B. Delabarre, 2014, The Journal of Biological Chemistry.

Mutant Isocitrate Dehydrogenase IDH 1 Characterization of a Potent Inhibitor of Biochemical , Cellular , and Biophysical Molecular Bases of Disease

S. Gross, B. Delabarre, L. Dang, 2014 .

Metal Binding Network by an Allosteric Dehydrogenase 1 ( IDH 1 ) via Disruption of Selective Inhibition of Mutant Isocitrate Enzymology

S. Gross, Q. Gao, D. Wiederschain, 2014 .

Full-length human glutaminase in complex with an allosteric inhibitor.

Abhishek K. Jha, S. Gross, B. Delabarre, 2011, Biochemistry.

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.

K. Marks, S. Gross, B. Delabarre, 2021, Journal of medicinal chemistry.

Mesenchymal phenotype predisposes lung cancer cells to impaired proliferation and redox stress in response to glutaminase inhibition

Abhishek K. Jha, S. Choe, S. Gross, 2014, Cancer & Metabolism.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Tyler T. Risom, S. Gross, J. Blake, 2010, Bioorganic & medicinal chemistry letters.

Abstract 2515: Preclinical Development of ARRY-162, A Potent and Selective MEK 1/2 Inhibitor

S. Gross, J. Lyssikatos, K. Koch, 2010 .

Preclinical development of ARRY-142886, a potent and selective MEK inhibitor

S. Gross, B. Brandhuber, T. Morales, 2004 .

Human squalene epoxidase (SQLE, squalene monooxygenase) structure with FAD and NB-598

S. Gross, Giovanni Cianchetta, Cheng Fang, 2019 .