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Items: 35

1.

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

Mahoney CE, Pirman D, Chubukov V, Sleger T, Hayes S, Fan ZP, Allen EL, Chen Y, Huang L, Liu M, Zhang Y, McDonald G, Narayanaswamy R, Choe S, Chen Y, Gross S, Cianchetta G, Padyana AK, Murray S, Liu W, Marks KM, Murtie J, Dorsch M, Jin S, Nagaraja N, Biller SA, Roddy T, Popovici-Muller J, Smolen GA.

Nat Commun. 2019 Jan 9;10(1):96. doi: 10.1038/s41467-018-07959-4.

2.

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

Padyana AK, Gross S, Jin L, Cianchetta G, Narayanaswamy R, Wang F, Wang R, Fang C, Lv X, Biller SA, Dang L, Mahoney CE, Nagaraja N, Pirman D, Sui Z, Popovici-Muller J, Smolen GA.

Nat Commun. 2019 Jan 9;10(1):97. doi: 10.1038/s41467-018-07928-x.

3.

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

Intlekofer AM, Shih AH, Wang B, Nazir A, Rustenburg AS, Albanese SK, Patel M, Famulare C, Correa FM, Takemoto N, Durani V, Liu H, Taylor J, Farnoud N, Papaemmanuil E, Cross JR, Tallman MS, Arcila ME, Roshal M, Petsko GA, Wu B, Choe S, Konteatis ZD, Biller SA, Chodera JD, Thompson CB, Levine RL, Stein EM.

Nature. 2018 Jul;559(7712):125-129. doi: 10.1038/s41586-018-0251-7. Epub 2018 Jun 27.

4.

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

Bambouskova M, Gorvel L, Lampropoulou V, Sergushichev A, Loginicheva E, Johnson K, Korenfeld D, Mathyer ME, Kim H, Huang LH, Duncan D, Bregman H, Keskin A, Santeford A, Apte RS, Sehgal R, Johnson B, Amarasinghe GK, Soares MP, Satoh T, Akira S, Hai T, de Guzman Strong C, Auclair K, Roddy TP, Biller SA, Jovanovic M, Klechevsky E, Stewart KM, Randolph GJ, Artyomov MN.

Nature. 2018 Apr;556(7702):501-504. doi: 10.1038/s41586-018-0052-z. Epub 2018 Apr 18.

5.

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

Yen K, Travins J, Wang F, David MD, Artin E, Straley K, Padyana A, Gross S, DeLaBarre B, Tobin E, Chen Y, Nagaraja R, Choe S, Jin L, Konteatis Z, Cianchetta G, Saunders JO, Salituro FG, Quivoron C, Opolon P, Bawa O, Saada V, Paci A, Broutin S, Bernard OA, de Botton S, Marteyn BS, Pilichowska M, Xu Y, Fang C, Jiang F, Wei W, Jin S, Silverman L, Liu W, Yang H, Dang L, Dorsch M, Penard-Lacronique V, Biller SA, Su SM.

Cancer Discov. 2017 May;7(5):478-493. doi: 10.1158/2159-8290.CD-16-1034. Epub 2017 Feb 13.

6.

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

Marjon K, Cameron MJ, Quang P, Clasquin MF, Mandley E, Kunii K, McVay M, Choe S, Kernytsky A, Gross S, Konteatis Z, Murtie J, Blake ML, Travins J, Dorsch M, Biller SA, Marks KM.

Cell Rep. 2016 Apr 19;15(3):574-587. doi: 10.1016/j.celrep.2016.03.043. Epub 2016 Apr 7.

7.

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

Kernytsky A, Wang F, Hansen E, Schalm S, Straley K, Gliser C, Yang H, Travins J, Murray S, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, Liu W, Yen KE.

Blood. 2015 Jan 8;125(2):296-303. doi: 10.1182/blood-2013-10-533604. Epub 2014 Nov 14.

8.

Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation.

Wang F, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, Straley K, Kernytsky A, Liu W, Gliser C, Yang H, Gross S, Artin E, Saada V, Mylonas E, Quivoron C, Popovici-Muller J, Saunders JO, Salituro FG, Yan S, Murray S, Wei W, Gao Y, Dang L, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, de Botton S, Yen KE.

Science. 2013 May 3;340(6132):622-6. doi: 10.1126/science.1234769. Epub 2013 Apr 4.

9.

An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.

Rohle D, Popovici-Muller J, Palaskas N, Turcan S, Grommes C, Campos C, Tsoi J, Clark O, Oldrini B, Komisopoulou E, Kunii K, Pedraza A, Schalm S, Silverman L, Miller A, Wang F, Yang H, Chen Y, Kernytsky A, Rosenblum MK, Liu W, Biller SA, Su SM, Brennan CW, Chan TA, Graeber TG, Yen KE, Mellinghoff IK.

Science. 2013 May 3;340(6132):626-30. doi: 10.1126/science.1236062. Epub 2013 Apr 4.

10.

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

Popovici-Muller J, Saunders JO, Salituro FG, Travins JM, Yan S, Zhao F, Gross S, Dang L, Yen KE, Yang H, Straley KS, Jin S, Kunii K, Fantin VR, Zhang S, Pan Q, Shi D, Biller SA, Su SM.

ACS Med Chem Lett. 2012 Sep 17;3(10):850-5. doi: 10.1021/ml300225h. eCollection 2012 Oct 11.

11.

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

Mondal MS, Gabriels J, McGinnis C, Magnifico M, Marsilje TH, Urban L, Collis A, Bojanic D, Biller SA, Frieauff W, Martus HJ, Suter W, Bentley P.

Toxicol Sci. 2010 Nov;118(1):71-85. doi: 10.1093/toxsci/kfq181. Epub 2010 Jul 14.

PMID:
20631060
12.

Tetrazole based amides as growth hormone secretagogues.

Li JJ, Wang H, Li J, Qu F, Swartz SG, Hernández AS, Biller SA, Robl JA, Tino JA, Slusarchyk D, Seethala R, Sleph P, Yan M, Grover G, Flynn N, Murphy BJ, Gordon D.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2536-9. doi: 10.1016/j.bmcl.2008.03.059. Epub 2008 Mar 22.

PMID:
18378446
13.

Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats.

Han S, Hagan DL, Taylor JR, Xin L, Meng W, Biller SA, Wetterau JR, Washburn WN, Whaley JM.

Diabetes. 2008 Jun;57(6):1723-9. doi: 10.2337/db07-1472. Epub 2008 Mar 20.

14.

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

Hernández AS, Swartz SG, Slusarchyk D, Yan M, Seethala RK, Sleph P, Grover G, Dickinson K, Giupponi L, Harper TW, Humphreys WG, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2067-72. doi: 10.1016/j.bmcl.2008.01.100. Epub 2008 Jan 31.

PMID:
18282707
15.

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

Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN.

J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q. Epub 2008 Feb 9.

PMID:
18260618
16.

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).

Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA.

J Med Chem. 2007 Nov 29;50(24):5890-3. Epub 2007 Oct 31.

PMID:
17973363
17.

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

Hernández AS, Cheng PT, Musial CM, Swartz SG, George RJ, Grover G, Slusarchyk D, Seethala RK, Smith M, Dickinson K, Giupponi L, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5928-33. Epub 2007 Aug 23.

PMID:
17869100
18.

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

Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. Epub 2007 Jan 27.

PMID:
17292608
19.

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.

Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG.

J Med Chem. 2005 Jul 28;48(15):5025-37.

PMID:
16033281
20.

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.

Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R, Cheng L, Sleph P, Sun W, Tieman A, Wetterau JR, Doweyko A, Chandrasena G, Chang SY, Humphreys WG, Sasseville VG, Biller SA, Ryono DE, Selan F, Hariharan N, Cheng PT.

J Med Chem. 2005 Mar 24;48(6):2248-50.

PMID:
15771468
21.

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

Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.

PMID:
15380200
22.

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

Magnin DR, Biller SA, Wetterau J, Robl JA, Dickson JK Jr, Taunk P, Harrity TW, Lawrence RM, Sun CQ, Wang T, Logan J, Fryszman O, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1337-40.

PMID:
12657277
23.

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

Sulsky R, Gougoutas JZ, DiMarco J, Biller SA.

J Org Chem. 1999 Jul 23;64(15):5504-5510.

PMID:
11674614
24.

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

Robl JA, Sulsky R, Sun CQ, Simpkins LM, Wang T, Dickson JK Jr, Chen Y, Magnin DR, Taunk P, Slusarchyk WA, Biller SA, Lan SJ, Connolly F, Kunselman LK, Sabrah T, Jamil H, Gordon D, Harrity TW, Wetterau JR.

J Med Chem. 2001 Mar 15;44(6):851-6.

PMID:
11300866
25.

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

Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA.

Science. 1998 Oct 23;282(5389):751-4.

26.

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

Jamil H, Chu CH, Dickson JK Jr, Chen Y, Yan M, Biller SA, Gregg RE, Wetterau JR, Gordon DA.

J Lipid Res. 1998 Jul;39(7):1448-54.

27.

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

Jamil H, Gordon DA, Eustice DC, Brooks CM, Dickson JK Jr, Chen Y, Ricci B, Chu CH, Harrity TW, Ciosek CP Jr, Biller SA, Gregg RE, Wetterau JR.

Proc Natl Acad Sci U S A. 1996 Oct 15;93(21):11991-5.

28.

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

Dickson JK Jr, Biller SA, Magnin DR, Petrillo EW Jr, Hillyer JW, Hsieh DC, Lan SJ, Rinehart JK, Gregg RE, Harrity TW, Jolibois KG, Kalinowski SS, Kunselman LK, Mookhtiar KA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):661-4. No abstract available.

PMID:
8576906
29.

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

Magnin DR, Biller SA, Chen Y, Dickson JK Jr, Fryszman OM, Lawrence RM, Logan JV, Sieber-McMaster ES, Sulsky RB, Traeger SC, Hsieh DC, Lan SJ, Rinehart JK, Harrity TW, Jolibois KG, Kunselman LK, Rich LC, Slusarchyk DA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):657-60. No abstract available.

PMID:
8576905
30.

Farnesyl diphosphate-based inhibitors of Ras farnesyl protein transferase.

Patel DV, Schmidt RJ, Biller SA, Gordon EM, Robinson SS, Manne V.

J Med Chem. 1995 Jul 21;38(15):2906-21.

PMID:
7636851
31.

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

Magnin DR, Biller SA, Dickson JK Jr, Logan JV, Lawrence RM, Chen Y, Sulsky RB, Ciosek CP Jr, Harrity TW, Jolibois KG, et al.

J Med Chem. 1995 Jul 7;38(14):2596-605.

PMID:
7629799
32.

Microsomal triglyceride transfer protein. Specificity of lipid binding and transport.

Jamil H, Dickson JK Jr, Chu CH, Lago MW, Rinehart JK, Biller SA, Gregg RE, Wetterau JR.

J Biol Chem. 1995 Mar 24;270(12):6549-54.

33.

Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.

Biller SA, Forster C, Gordon EM, Harrity T, Rich LC, Marretta J, Ciosek CP Jr.

J Med Chem. 1991 Jun;34(6):1912-4. No abstract available.

PMID:
2061928
34.

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.

Karanewsky DS, Badia MC, Ciosek CP Jr, Robl JA, Sofia MJ, Simpkins LM, DeLange B, Harrity TW, Biller SA, Gordon EM.

J Med Chem. 1990 Nov;33(11):2952-6. No abstract available.

PMID:
2231594
35.

Isoprenoid (phosphinylmethyl)phosphonates as inhibitors of squalene synthetase.

Biller SA, Forster C, Gordon EM, Harrity T, Scott WA, Ciosek CP Jr.

J Med Chem. 1988 Oct;31(10):1869-71. No abstract available.

PMID:
3172121

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