Y. Qian

发表

The Geranylgeranyltransferase I Inhibitor GGTI-298 Induces Hypophosphorylation of Retinoblastoma and Partner Switching of Cyclin-dependent Kinase Inhibitors

S. Sebti, A. Hamilton, Jiazhi Sun, 1999, The Journal of Biological Chemistry.

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

C. Crews, Y. Qian, K. Coleman, 2015, Chemistry & biology.

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

C. Crews, Y. Qian, K. Coleman, 2016, Proceedings of the National Academy of Sciences.

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.

Jing Wang, Yimin Qian, George M Burslem, 2017, Cell chemical biology.

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53.

C. Crews, Y. Qian, J. Hines, 2018, Cancer research.

Potent, selective MCH-1 receptor antagonists.

S. Berthel, S. Mischke, Y. Qian, 2008, Bioorganic & medicinal chemistry letters.

Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors.

J. Marugan, S. Sebti, A. Hamilton, 1999, Bioorganic & medicinal chemistry.

Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells.

A. Vasudevan, S. Sebti, A. Hamilton, 1998, American journal of physiology. Lung cellular and molecular physiology.

Inhibition of Protein Geranylgeranylation Causes a Superinduction of Nitric-oxide Synthase-2 by Interleukin-1β in Vascular Smooth Muscle Cells*

S. Sebti, A. Hamilton, T. Mcguire, 1997, The Journal of Biological Chemistry.

Farnesyltransferase as a target for anticancer drug design.

S. Sebti, A. Hamilton, Y. Qian, 1997, Biopolymers.

Peptidomimetic inhibitors of farnesyltransferase

S. Sebti, A. Hamilton, Y. Qian, 1997 .

Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.

S. Sebti, A. Hamilton, Jiazhi Sun, 1995, Cancer research.

A Non-peptide Mimetic of Ras-CAAX: Selective Inhibition of Farnesyltransferase and Ras Processing (*)

S. Sebti, A. Hamilton, Y. Qian, 1995, The Journal of Biological Chemistry.

Peptidomimetic inhibitors of p21ras farnesyltransferase: Hydrophobic functionalization leads to disruption of p21ras membrane association in whole cells

S. Sebti, A. Hamilton, Y. Qian, 1994 .

Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs.

S. So, Y. Qian, Yonglin Ren, 2013, Bioorganic & medicinal chemistry letters.

Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes.

R. Muschel, S. Sebti, E. Bernhard, 1998, Cancer research.

Interdomain Interactions in the Tumor Suppressor Discs Large Regulate Binding to the Synaptic Protein GukHolder*

Y. Qian, K. Prehoda, 2006, Journal of Biological Chemistry.

Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors.

S. So, Shaoqing Chen, Nam T Le, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of 2-N-substituted indazolone derivatives as non-carboxylic acid glycogen synthase activators.

Qing Xiang, Xiaolei Zhang, Y. Qian, 2013, Bioorganic & medicinal chemistry letters.

N-substituted sultam carboxylic acids as novel glycogen synthase activators

Qing Xiang, Xiaolei Zhang, Y. Qian, 2013 .

Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.

S. Sebti, A. Hamilton, Jiazhi Sun, 1999, Cancer research.

Activated Drosophila Ras1 is selectively suppressed by isoprenyl transferase inhibitors.

S. Sebti, A. Hamilton, R. Carthew, 1995, Proceedings of the National Academy of Sciences of the United States of America.

Development of a tripeptide mimetic strategy for the inhibition of protein farnesyltransferase

S. Sebti, A. Hamilton, Y. Qian, 2000 .

Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.

S. Berthel, Y. Qian, D. Choi, 2013, ACS medicinal chemistry letters.

Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.

C. Rondinone, Yingsi Chen, Y. Qian, 2011, Journal of medicinal chemistry.

Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML

P. Qiu, K. Rajapakshe, C. Coarfa, 2018, Leukemia.

Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors.

Yingsi Chen, Y. Qian, R. Taub, 2011, Bioorganic & medicinal chemistry letters.

Comparing the differential effects of LPA on the barrier function of human pulmonary endothelial cells.

J. Allard, R. Hamid, Y. Qian, 2013, Microvascular research.

Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts.

Christopher S. Stevenson, C. Stevenson, A. Narayanan, 2012, Journal of medicinal chemistry.

Development of lysophosphatidic acid pathway modulators as therapies for fibrosis.

Y. Qian, D. Budd, 2013, Future medicinal chemistry.

Cytotoxic Agents Cisplatin , Taxol , and Gemcitabine Geranylgeranyltransferase I : Combination Therapy with the Peptidomimetic Inhibitors of Farnesyltransferase and Antitumor Efficacy of a Novel Class of Non-thiol-containing Updated Version

S. Sebti, A. Hamilton, Jiazhi Sun, 1999 .

Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells.

A. Vasudevan, S. Sebti, A. Hamilton, 1998, The American journal of physiology.

Deconstructing estradiol: removal of B-ring generates compounds which are potent and subtype-selective estrogen receptor agonists.

J. Katzenellenbogen, K. Carlson, Y. Qian, 2009, Bioorganic & medicinal chemistry letters.

Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.

S. Sebti, A. Hamilton, Jiazhi Sun, 2006, Organic & biomolecular chemistry.

Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors.

S. Sebti, A. Hamilton, Y. Qian, 1996, Journal of medicinal chemistry.

Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.

S. Sebti, A. Hamilton, Y. Qian, 2002, Journal of medicinal chemistry.

Discovery of novel non-carboxylic acid 5-amino-4-cyanopyrazole derivatives as potent and highly selective LPA1R antagonists.

C. Stevenson, V. Roongta, A. Sidduri, 2014, Bioorganic & medicinal chemistry letters.

Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.

S. So, I. Klein, Y. Qian, 2014, Journal of medicinal chemistry.

The Geranylgeranyltransferase-I Inhibitor GGTI-298 Arrests Human Tumor Cells in G0/G1 and Induces p21WAF1/CIP1/SDI1 in a p53-independent Manner*

S. Sebti, A. Hamilton, Jiazhi Sun, 1997, The Journal of Biological Chemistry.

Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer

J. Flanagan, C. Crews, Y. Qian, 2021, Experimental and Molecular Therapeutics.

BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells

M. Wang, K. Rajapakshe, C. Coarfa, 2018, Leukemia.

Novel BET protein Proteolysis Targeting Chimera (BET-PROTAC) exerts superior lethal activity than Bromodomain Inhibitor (BETi) against post-myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells

P. Qiu, K. Rajapakshe, C. Coarfa, 2016, Leukemia.

RUNX1 targeted therapy for AML expressing somatic or germline mutation in RUNX1.

Michael R. Green, K. Rajapakshe, C. Coarfa, 2019, Blood.

Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer

J. Flanagan, I. Taylor, C. Crews, 2019, Poster Session Abstracts.

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1.

Yevgeniy V. Serebrenik, D. Vigil, C. Crews, 2017, Journal of medicinal chemistry.

p21WAF1/CIP1 Is Upregulated by the Geranylgeranyltransferase I Inhibitor GGTI-298 through a Transforming Growth Factor β- and Sp1-Responsive Element: Involvement of the Small GTPase RhoA

S. Sebti, Y. Qian, F. Bizouarn, 1998, Molecular and Cellular Biology.

Involvement of the Small GTPase RhoA-and Sp 1-Responsive Element : β Factor GGTI-298 through a Transforming Growth Geranylgeranyltransferase I Inhibitor Is Upregulated by the WAF 1 / CIP 1 p 21

S. Sebti, Y. Qian, Andrew, 1998 .

Inhibitor GGTI-298 through a Transforming Growth Factor b- and Sp1-Responsive Element: Involvement of the Small GTPase RhoA

S. Sebti, A. Hamilton, Y. Qian, 1998 .

Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts

S. Sebti, A. Hamilton, Jiazhi Sun, 1998, Oncogene.

Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.

S. Sebti, A. Hamilton, Y. Qian, 1993, The Journal of biological chemistry.

Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts.

S. Sebti, A. Hamilton, T. Mcguire, 1996, Oncogene.

Platelet-derived Growth Factor Receptor Tyrosine Phosphorylation Requires Protein Geranylgeranylation but not Farnesylation*

S. Sebti, A. Hamilton, T. Mcguire, 1996, The Journal of Biological Chemistry.

Ras CAAX Peptidomimetic FTI-277 Selectively Blocks Oncogenic Ras Signaling by Inducing Cytoplasmic Accumulation of Inactive Ras-Raf Complexes (*)

C. Der, S. Sebti, A. Hamilton, 1995, The Journal of Biological Chemistry.

Disruption of Oncogenic K-Ras4B Processing and Signaling by a Potent Geranylgeranyltransferase I Inhibitor(*)

S. Sebti, A. Hamilton, Y. Qian, 1995, The Journal of Biological Chemistry.

Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines

S. Sebti, A. Hamilton, Y. Qian, 1997, Oncogene.

GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.

S. Sebti, G. Favre, A. Hamilton, 1997, Cancer research.

Protein Targeting Chimeric Molecules Specific for Bromodomain and Extra-terminal Motif Family Proteins are Active Against Pre-Clinical Models of Multiple Myeloma

V. Baladandayuthapani, R. Orlowski, C. Crews, 2018, Leukemia.

BETP degradation simultaneously targets acute myelogenous leukemia stem cells and the microenvironment.

R. Davis, M. Konopleva, M. Andreeff, 2019, The Journal of clinical investigation.

Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics.

A. Vasudevan, S. Sebti, A. Hamilton, 1998, Bioorganic & medicinal chemistry.

Design and structural requirements of potent peptidomimetic inhibitors of p21ras farnesyltransferase.

S. Sebti, A. Hamilton, Y. Qian, 1994, The Journal of biological chemistry.

CAAX peptidomimetic FTI-244 decreases platelet-derived growth factor receptor tyrosine phosphorylation levels and inhibits stimulation of phosphatidylinositol 3-kinase but not mitogen-activated protein kinase.

S. Corey, A. Hamilton, T. Mcguire, 1995, Biochemical and biophysical research communications.

Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.

A. Vasudevan, S. Sebti, A. Hamilton, 1999, Journal of medicinal chemistry.

Abstract P4-04-04: Identification and development of oral estrogen receptor PROTAC degraders for breast cancer

J. Flanagan, I. Taylor, C. Crews, 2018 .

Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML

P. Qiu, K. Rajapakshe, C. Coarfa, 2018, Leukemia.

Burkitt lymphoma Daudi cells contain two distinct farnesyltransferases with different divalent cation requirements.

S. Sebti, A. Hamilton, Y. Qian, 1995, Biochemistry.