Ker Yu

发表

Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

N. Brooijmans, L. Toral-Barza, K. Curran, 2009, Journal of medicinal chemistry.

Dual Mechanisms of Novel CD73-Targeted Antibody and Antibody–Drug Conjugate in Inhibiting Lung Tumor Growth and Promoting Antitumor Immune-Effector Function

Jing-kang Shen, Yun Xing, Xin Wang, 2020, Molecular Cancer Therapeutics.

Targeting mTOR globally in cancer: Thinking beyond rapamycin

R. Abraham, J. Gibbons, Ker Yu, 2009, Cell cycle.

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.

R. Abraham, N. Brooijmans, J. Gibbons, 2009, Journal of medicinal chemistry.

Novel sulfur-containing rapamycin analogs prepared by precursor-directed biosynthesis.

E. Graziani, G. Carter, M. Summers, 2003, Organic letters.

Identification and characterization of a constitutively T-loop phosphorylated and active recombinant S6K1: expression, purification, and enzymatic studies in a high capacity non-radioactive TR-FRET Lance assay.

Wei-guo Zhang, Ker Yu, Boris Shor, 2006, Protein expression and purification.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

Kevin Curran, Judy Lucas, John Ellingboe, 2009, Cancer research.

Novel-smoothened inhibitors for therapeutic targeting of naïve and drug-resistant hedgehog pathway-driven cancers

Hui Zhao, Ker Yu, Xuesai Zhang, 2019, Acta Pharmacologica Sinica.

mTOR complex-2 stimulates acetyl-CoA and de novo lipogenesis through ATP citrate lyase in HER2/PIK3CA-hyperactive breast cancer

L. Toral-Barza, Hui Zhao, Jianchang Qian, 2016, Oncotarget.

4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, N. Zhang, L. Toral-Barza, 2010, Bioorganic & medicinal chemistry letters.

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, L. Toral-Barza, J. Bard, 2010, Bioorganic & medicinal chemistry letters.

Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.

A. Zask, J. Verheijen, D. J. Richard, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, L. Toral-Barza, A. Zask, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.

K. Curran, A. Zask, Joshua A Kaplan, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.

L. Toral-Barza, A. Zask, J. Verheijen, 2010, Bioorganic & medicinal chemistry letters.

Discovery of lactoquinomycin and related pyranonaphthoquinones as potent and allosteric inhibitors of AKT/PKB: mechanistic involvement of AKT catalytic activation loop cysteines

R. Abraham, P. Cai, J. Levin, 2007, Molecular Cancer Therapeutics.

PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors

P. Frost, J. Skotnicki, P. Cai, 2005, Cancer biology & therapy.

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.

L. Toral-Barza, J. Lucas, M. Young, 2008, Journal of medicinal chemistry.

BCL9/BCL9L promotes tumorigenicity through immune-dependent and independent mechanisms in triple negative breast cancer

Z. Shao, Yi Xiao, Di Zhu, 2021, Oncogene.

mTOR-targeted therapy: differential perturbation to mitochondrial membrane potential and permeability transition pore plays a role in therapeutic response.

Jae Eun Kim, Ker Yu, C. Shi, 2014, Biochemical and biophysical research communications.

mTOR Inhibitors in Oncology

A. Zask, J. Verheijen, Ker Yu, 2008 .

Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.

J. Gibbons, J. Lucas, Jianxin Gu, 2010, Journal of medicinal chemistry.

Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models.

J. Skotnicki, P. Cai, J. Gibbons, 2006, Journal of medicinal chemistry.

Isolation and structure of homotemsirolimuses A, B, and C.

T. Pagano, Ker Yu, Fangming Kong, 2011, Journal of natural products.

Identification of pyrimidine derivatives as hSMG-1 inhibitors.

A. Gopalsamy, J. Bard, Wei-guo Zhang, 2012, Bioorganic & medicinal chemistry letters.

Mechanism of Regulation of Big-Conductance Ca2+-Activated K+ Channels by mTOR Complex 2 in Podocytes

Xudong Xu, Xuemei Zhang, Weiguang Zhang, 2019, Frontiers in Physiology.

BK ablation attenuates osteoblast bone formation via integrin pathway

Jibin Dong, Xuemei Zhang, H. Xin, 2019, Cell Death & Disease.

Sphingomyelin synthase 2 is a positive regulator of the CSF1R-STAT3 pathway in pancreatic cancer-associated macrophage

Jibin Dong, Ting-bo Ding, Deyong Ye, 2022, Frontiers in Pharmacology.

Non-immunogenic, low-toxicity and effective glioma targeting MTI-31 liposomes.

D. Burgess, W. Lu, C. Zhan, 2019, Journal of controlled release : official journal of the Controlled Release Society.

Abstract 723: Beyond temsirolimus: Discovery of PKI-587 a highly efficacious dual PI3K/mTOR inhibitor

R. Abraham, N. Brooijmans, L. Feldberg, 2010 .

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

N. Brooijmans, L. Toral-Barza, J. Lucas, 2009, Journal of medicinal chemistry.

Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2010, Journal of medicinal chemistry.

Rolloamides A and B, cytotoxic cyclic heptapeptides isolated from the Caribbean marine sponge Eurypon laughlini.

David E. Williams, R. Andersen, Ker Yu, 2009, Journal of natural products.

5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.

N. Brooijmans, N. Zhang, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.

Production of Novel Rapamycin Analogs by Precursor-Directed Biosynthesis

E. Graziani, G. Carter, M. Summers, 2005, Applied and Environmental Microbiology.

Culicinin D, an antitumor peptaibol produced by the fungus Culicinomyces clavisporus, strain LL-12I252.

J. Janso, Hai-yin He, Hui Y. Yang, 2006, Journal of natural products.

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Journal of medicinal chemistry.

Sphingomyelin synthase 2 facilitates M2-like macrophage polarization and tumor progression in a mouse model of triple-negative breast cancer

Ting-bo Ding, Deyong Ye, Xian-cheng Jiang, 2020, Acta Pharmacologica Sinica.

Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.

D. Powell, J. Levin, L. Toral-Barza, 2009, Journal of medicinal chemistry.

Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.

R. Abraham, J. Gibbons, L. Toral-Barza, 2010, Cancer research.

Mammalian target of rapamycin: discovery of rapamycin reveals a signaling pathway important for normal and cancer cell growth.

R. Abraham, J. Gibbons, Ker Yu, 2009, Seminars in oncology.

A novel lead compound CM-118

C. Liang, Hui Zhao, Ker Yu, 2014, Cancer biology & therapy.

Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer

Jing-kang Shen, Xin Wang, Lan-ping Ma, 2016, Oncotarget.

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

L. Feldberg, R. Mallon, J. Lucas, 2010, Bioorganic & medicinal chemistry letters.

Requirement of the mTOR Kinase for the Regulation of Maf1 Phosphorylation and Control of RNA Polymerase III-dependent Transcription in Cancer Cells

M. Follettie, L. Toral-Barza, Jiang Wu, 2010, The Journal of Biological Chemistry.

Response and determinants of cancer cell susceptibility to PI3K inhibitors: Combined targeting of PI3K and Mek1 as an effective anticancer strategy

L. Toral-Barza, Wei-guo Zhang, A. Zask, 2008, Cancer biology & therapy.

A new pharmacologic action of CCI-779 involves FKBP12-independent inhibition of mTOR kinase activity and profound repression of global protein synthesis.

R. Abraham, J. Gibbons, L. Toral-Barza, 2008, Cancer research.

Ammonia Derived from Glutaminolysis Is a Diffusible Regulator of Autophagy

Judy Lucas, Eileen White, Robert T. Abraham, 2010, Science Signaling.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2011, Bioorganic & medicinal chemistry letters.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.

Judy Lucas, Irwin Hollander, Robert Mallon, 2010, Journal of medicinal chemistry.

A Novel mTORC1/2 Inhibitor (MTI-31) Inhibits Tumor Growth, Epithelial–Mesenchymal Transition, Metastases, and Improves Antitumor Immunity in Preclinical Models of Lung Cancer

Jianchang Qian, Ker Yu, Ya-qing Chen, 2019, Clinical Cancer Research.

A novel mTORC1/2 inhibitor (MTI-31) inhibits tumor growth, epithelial-mesenchymal transition, metastases and improves cancer immunity in preclinical lung cancer models

Jianchang Qian, Ker Yu, Ya-qing Chen, 2019 .

Pathological expression of tissue factor confers promising antitumor response to a novel therapeutic antibody SC1 in triple negative breast cancer and pancreatic adenocarcinoma

Hui Zhao, Jing-kang Shen, Lan-ping Ma, 2017, Oncotarget.

Characterization of the cloned full-length and a truncated human target of rapamycin: activity, specificity, and enzyme inhibition as studied by a high capacity assay.

J. Gibbons, L. Toral-Barza, J. Larocque, 2005, Biochemical and biophysical research communications.

Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.

L. Toral-Barza, J. Lucas, K. Curran, 2009, Bioorganic & medicinal chemistry letters.

BCL9 regulates CD226 and CD96 checkpoints in CD8+ T cells to improve PD-1 response in cancer

D. Lambrechts, Zhongen Wu, Ming-Wei Wang, 2021, Signal Transduction and Targeted Therapy.

mTOR Promotes Tissue Factor Expression and Activity in EGFR-Mutant Cancer

Ker Yu, Ying Cong, Ya-qing Chen, 2020, Frontiers in Oncology.

Biochemical and pharmacological inhibition of mTOR by rapamycin and an ATP-competitive mTOR inhibitor.

L. Toral-Barza, Ker Yu, L. Toral‐Barza, 2012, Methods in molecular biology.

Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.

Joshua Kaplan, Irwin Hollander, Natasja Brooijmans, 2009, Journal of medicinal chemistry.

mTOR, a novel target in breast cancer: the effect of CCI-779, an mTOR inhibitor, in preclinical models of breast cancer.

P. Frost, J. Skotnicki, C. Discafani, 2001, Endocrine-related cancer.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

R. Abraham, J. Gibbons, J. Lucas, 2009, Cancer Research.

A new pharmacologic action of CCI-779 involves FKBP12-independent inhibition of mTOR kinase activity and profound repression of global protein synthesis.

R. Abraham, J. Gibbons, Ker Yu, 2008, Cancer research.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.

Novel-smoothened inhibitors for therapeutic targeting of naïve and drug-resistant hedgehog pathway-driven cancers

Hui Zhao, Ker Yu, Qingrou Li, 2018, Acta Pharmacologica Sinica.