S. Biller

发表

Ras farnesylation as a target for novel antitumor agents: Potent and selective farnesyl diphosphate analog inhibitors of farnesyltransferase

M. Barbacid, S. Robinson, B. Seizinger, 1995 .

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

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

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.

Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.

R. Lawrence, T. Harrity, L. Kunselman, 2003, Bioorganic & medicinal chemistry letters.

Microsomal Triglyceride Transfer Protein

H. Jamil, C. Chu, R. Gregg, 1995, The Journal of Biological Chemistry.

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

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

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

Weiqi Wang, A. Doweyko, W. Humphreys, 2005, Journal of medicinal chemistry.

An inhibitor of the microsomal triglyceride transfer protein inhibits apoB secretion from HepG2 cells.

H. Jamil, C. Chu, R. Gregg, 1996, Proceedings of the National Academy of Sciences of the United States of America.

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.

L. Hamann, A. Fura, R. Seethala, 2007, Bioorganic & medicinal chemistry letters.

Evidence that microsomal triglyceride transfer protein is limiting in the production of apolipoprotein B-containing lipoproteins in hepatic cells.

H. Jamil, C. Chu, R. Gregg, 1998, Journal of lipid research.

A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.

H. Jamil, D. Gordon, T. Harrity, 2001, Journal of medicinal chemistry.

A solid phase synthesis of miconazole analogs via an iodoetherification reaction

D. Tortolani, S. Biller, 1996 .

Evaluation of Pharmacokinetic-Pharmacodynamic (PKPD) Relationship of an Oral, Selective, First-in-Class, Potent IDH2 Inhibitor, AG-221, from a Phase 1 Trial in Patients with Advanced IDH2 Mutant Positive Hematologic Malignancies

Hua Yang, K. Yen, Fang Wang, 2014 .

Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor activator, improves diabetes and other metabolic abnormalities and preserves beta-cell function in db/db mice.

R. Gregg, W. Fenderson, Wen-pin Yang, 2006, Diabetes.

Isoprenoid (phosphinylmethyl)phosphonates as inhibitors of squalene synthetase.

E. Gordon, T. Harrity, C. Ciosek, 1988, Journal of medicinal chemistry.

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.

Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.

R. Gregg, T. Harrity, K. Mookhtiar, 1996, Journal of medicinal chemistry.

Farnesyl diphosphate-based inhibitors of Ras farnesyl protein transferase.

E. Gordon, V. Manne, D. Patel, 1995, Journal of medicinal chemistry.

Tetrazole based amides as growth hormone secretagogues.

R. Seethala, G. Grover, P. Sleph, 2008, Bioorganic & medicinal chemistry letters.

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

R. Parker, L. Hamann, M. Kirby, 2005, Journal of medicinal chemistry.

Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.

K. Dickinson, R. Seethala, G. Grover, 2007, Bioorganic & medicinal chemistry letters.

Aromatic isosteres as conformational probes for an isoprenyl subunit: application to inhibitors of squalene synthase

J. Abt, C. Ciosek, S. Biller, 1993 .

The synthesis of isoprenoid (phosphinylmethyl)phosphonates

S. Biller, C. Forster, 1990 .

Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.

E. Gordon, T. Harrity, C. Ciosek, 1991, Journal of medicinal chemistry.

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

W. Humphreys, K. Dickinson, R. Seethala, 2007, Journal of medicinal chemistry.

Dapagliflozin, a Selective SGLT2 Inhibitor, Improves Glucose Homeostasis in Normal and Diabetic Rats

Li Xin, Joseph R. Taylor, Songping Han, 2008, Diabetes.

Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

W. Humphreys, O. Flint, E. Janovitz, 2008, Journal of medicinal chemistry.

The total synthesis of (±)-naphthyridinomycin. I. Preparation of a key tricyclic lactam intermediate.

Davidr . Evans, S. Biller, 1985 .

The total synthesis of (±)-naphthyridinomycin. II. Construction of the pentacyclic carbon skeleton.

Davidr . Evans, S. Biller, 1985 .

Enantioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors: Chiral Recognition in the Interactions of an α-Phosphono Sulfonate Inhibitor with Squalene Synthase

R. Lawrence, T. Harrity, S. Lan, 1996 .

Free-radical cyclization of bromo acetals. Use in the construction of bicyclic acetals and lactones

R. Mook, S. Rychnovsky, G. Stork, 1983 .

Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.

E. Gordon, T. Harrity, M. Sofia, 1990, Journal of medicinal chemistry.

Conformational Switching and the Synthesis of Spiro[2H-indol]-3(1H)-ones by Radical Cyclization.

S. Biller, R. Sulsky, J. Gougoutas, 1999, The Journal of organic chemistry.

Automated Synthesis and Purification of Amides: Exploitation of Automated Solid Phase Extraction in Organic Synthesis

M. Poss, R. Lawrence, S. Biller, 1997 .

Stereospecific vicinal oxyamination of olefins by alkylimidoosmium compounds

K. Sharpless, L. Truesdale, K. B. Sharpless, 1978 .

Synthesis of Isoprenoid (Phosphinylmethyl)phosphonates.

S. Biller, C. Forster, 1991 .

An approach to gelsemine

M. E. Krafft, G. Stork, S. Biller, 1987 .

New reaction. Stereospecific vicinal oxyamination of olefins by alkyl imido osmium compounds

K. Sharpless, L. Truesdale, K. B. Sharpless, 1975 .

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

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

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

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

Electrophilic properties of itaconate and derivatives regulate the IκBζ–ATF3 inflammatory axis

Maxim N. Artyomov, E. Klechevsky, S. Akira, 2018, Nature.

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.

Dong Cheng, Ramesh Padmanabha, Kristen Pike, 2007, Bioorganic & medicinal chemistry letters.

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

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

An Inhibitor of Mutant IDH1 Delays Growth and Promotes Differentiation of Glioma Cells

Fang Wang, Timothy A. Chan, Evangelia Komisopoulou, 2013, Science.

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

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

IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition.

Wei Liu, Fang Wang, Hua Yang, 2014, Blood.

Molecular mechanisms mediating relapse following ivosidenib monotherapy in IDH1-mutant relapsed or refractory AML.

S. Choe, K. Marks, Wei Liu, 2020, Blood advances.

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

I. Mellinghoff, Cheng Fang, Hua Yang, 2020, ACS medicinal chemistry letters.

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.

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.

Potent, Rationally Designed Inhibitors of Squalene Synthase

J. Abt, E. Gordon, T. Harrity, 1992 .

The first potent inhibitor of squalene synthase : a profound contribution of an ether oxygen to inhibitor-enzyme interaction

E. Gordon, T. Harrity, M. Sofia, 1991 .

An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.

H. Jamil, C. Chu, R. Gregg, 1998, Science.

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.

Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations

Steven K. Albanese, Ariën S. Rustenburg, G. Petsko, 2018, Nature.

Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations

Bo Wang, John D. Chodera, Steven K. Albanese, 2018, Nature.

Longitudinal Pharmacokinetic/Pharmacodynamic Profile of AG-120, a Potent Inhibitor of the IDH1 Mutant Protein, in a Phase 1 Study of IDH1-Mutant Advanced Hematologic Malignancies

Hua Yang, S. Agresta, K. Le, 2015 .

Muraglitazar, a Novel Dual (α/γ) Peroxisome Proliferator–Activated Receptor Activator, Improves Diabetes and Other Metabolic Abnormalities and Preserves β-Cell Function in db/db Mice

Michael Cap, R. Gregg, W. Fenderson, 2006 .

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.

E. Sieber-McMaster, R. Lawrence, T. Harrity, 1996, Journal of medicinal chemistry.

High-content micronucleus assay in genotoxicity profiling: initial-stage development and some applications in the investigative/lead-finding studies in drug discovery.

Dejan Bojanic, Wilfried Frieauff, D. Bojanic, 2010, Toxicological sciences : an official journal of the Society of Toxicology.

Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

G. Lenz, S. Choe, K. Marks, 2020, Molecular Cancer Therapeutics.

Automated Synthesis and Purification of Amides: Exploitation of Automated Solid Phase Extraction in Organic Synthesis.

M. Poss, R. Lawrence, S. Biller, 1997 .

Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

W. Humphreys, K. Dickinson, R. Seethala, 2008, Bioorganic & medicinal chemistry letters.

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.

1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate.

R. Lawrence, T. Harrity, C. Ciosek, 1995, Journal of medicinal chemistry.

Phosphorus-Containing Inhibitors of HMG-CoA Reductase. Part 1. 4-((2- Arylethyl)hydroxyphosphinyl)-3-hydroxybutanoic Acids: A New Class of Cell-Selective Inhibitors of Cholesterol Biosynthesis.

E. Gordon, T. Harrity, M. Sofia, 1991 .

5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.

T. Harrity, L. Kunselman, J. Robl, 2004, Bioorganic & medicinal chemistry letters.

Abstract B126: AG-881, a brain penetrant, potent, pan-mutant IDH (mIDH) inhibitor for use in mIDH solid and hematologic malignancies

I. Mellinghoff, Hua Yang, K. Yen, 2018 .

Preclinical Drug Metabolism, Pharmacokinetic, and Pharmacodynamic Profiles of Ivosidenib, an Inhibitor of Mutant Isocitrate Dehydrogenase 1 for Treatment of Isocitrate Dehydrogenase 1-Mutant Malignancies

Hua Yang, S. Su, L. Dang, 2021, Drug Metabolism and Disposition.

Differentiation of Glioma Cells An Inhibitor of Mutant IDH 1 Delays Growth and Promotes

A. Kernytsky, C. Brennan, T. Graeber, 2013 .

AG-221 Offers a Survival Advantage In a Primary Human IDH2 Mutant AML Xenograft Model

S. Choe, Hua Yang, K. Yen, 2013 .

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

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

Synthesis of d3-cerivastatin for use as internal standard in a LC/MS/MS method developed for quantitation of the drug in human serum

J. Barrish, M. Jemal, J. Robl, 2006 .

Osmium-catalyzed vicinal oxyamination of olefins by N-chloro-N-argentocarbamates

K. Sharpless, K. B. Sharpless, S. Biller, 1978 .