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Items: 25

1.

Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer.

Petros AM, Korepanova A, Jakob CG, Qiu W, Panchal SC, Wang J, Dietrich JD, Brewer JT, Pohlki F, Kling A, Wilcox K, Lakics V, Bahnassawy L, Reinhardt P, Partha SK, Bodelle PM, Lake M, Charych EI, Stoll VS, Sun C, Mohler EG.

J Med Chem. 2019 Apr 25;62(8):4120-4130. doi: 10.1021/acs.jmedchem.9b00178. Epub 2019 Apr 12.

PMID:
30933499
2.

PARP1 Trapping by PARP Inhibitors Drives Cytotoxicity in Both Cancer Cells and Healthy Bone Marrow.

Hopkins TA, Ainsworth WB, Ellis PA, Donawho CK, DiGiammarino EL, Panchal SC, Abraham VC, Algire MA, Shi Y, Olson AM, Johnson EF, Wilsbacher JL, Maag D.

Mol Cancer Res. 2019 Feb;17(2):409-419. doi: 10.1158/1541-7786.MCR-18-0138. Epub 2018 Nov 14.

PMID:
30429212
3.

ABT-165, a Dual Variable Domain Immunoglobulin (DVD-Ig) Targeting DLL4 and VEGF, Demonstrates Superior Efficacy and Favorable Safety Profiles in Preclinical Models.

Li Y, Hickson JA, Ambrosi DJ, Haasch DL, Foster-Duke KD, Eaton LJ, DiGiammarino EL, Panchal SC, Jiang F, Mudd SR, Zhang C, Akella SS, Gao W, Ralston SL, Naumovski L, Gu J, Morgan-Lappe SE.

Mol Cancer Ther. 2018 May;17(5):1039-1050. doi: 10.1158/1535-7163.MCT-17-0800. Epub 2018 Mar 28.

4.

Characterization of ABBV-221, a Tumor-Selective EGFR-Targeting Antibody Drug Conjugate.

Phillips AC, Boghaert ER, Vaidya KS, Falls HD, Mitten MJ, DeVries PJ, Benatuil L, Hsieh CM, Meulbroek JA, Panchal SC, Buchanan FG, Durbin KR, Voorbach MJ, Reuter DR, Mudd SR, Loberg LI, Ralston SL, Cao D, Gan HK, Scott AM, Reilly EB.

Mol Cancer Ther. 2018 Apr;17(4):795-805. doi: 10.1158/1535-7163.MCT-17-0710. Epub 2018 Feb 26.

5.

Treating Hallucinations and Delusions Associated With Parkinson's Disease Psychosis.

Panchal SC, Ondo WG.

Curr Psychiatry Rep. 2018 Jan 27;20(1):3. doi: 10.1007/s11920-018-0869-z. Review.

PMID:
29374325
6.

Fragment-based discovery of a potent NAMPT inhibitor.

Korepanova A, Longenecker KL, Pratt SD, Panchal SC, Clark RF, Lake M, Gopalakrishnan SM, Raich D, Sun C, Petros AM.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):437-440. doi: 10.1016/j.bmcl.2017.12.023. Epub 2017 Dec 12.

PMID:
29287958
7.

Are We There Yet? Applying Thermodynamic and Kinetic Profiling on Embryonic Ectoderm Development (EED) Hit-to-Lead Program.

Wang Y, Edalji RP, Panchal SC, Sun C, Djuric SW, Vasudevan A.

J Med Chem. 2017 Oct 26;60(20):8321-8335. doi: 10.1021/acs.jmedchem.7b00576. Epub 2017 Oct 5.

PMID:
28926243
8.

Erratum: The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.

He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN.

Nat Chem Biol. 2017 Jul 18;13(8):922. doi: 10.1038/nchembio0817-922b. No abstract available.

PMID:
28853738
9.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF.

J Med Chem. 2017 May 11;60(9):3828-3850. doi: 10.1021/acs.jmedchem.7b00017. Epub 2017 Apr 21.

PMID:
28368119
10.

Methylpyrrole inhibitors of BET bromodomains.

Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF.

Bioorg Med Chem Lett. 2017 May 15;27(10):2225-2233. doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24.

PMID:
28268136
11.

The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.

He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN.

Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Erratum in: Nat Chem Biol. 2017 Jul 18;13(8):922.

PMID:
28135237
12.

Mechanistic Dissection of PARP1 Trapping and the Impact on In Vivo Tolerability and Efficacy of PARP Inhibitors.

Hopkins TA, Shi Y, Rodriguez LE, Solomon LR, Donawho CK, DiGiammarino EL, Panchal SC, Wilsbacher JL, Gao W, Olson AM, Stolarik DF, Osterling DJ, Johnson EF, Maag D.

Mol Cancer Res. 2015 Nov;13(11):1465-77. doi: 10.1158/1541-7786.MCR-15-0191-T. Epub 2015 Jul 27.

13.

Cracking the molecular weight barrier: fragment screening of an aminotransferase using an NMR-based functional assay.

Mendoza R, Petros AM, Liu Y, Thimmapaya R, Surowy CS, Leise WF, Pereda-Lopez A, Panchal SC, Sun C.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5248-50. doi: 10.1016/j.bmcl.2011.07.039. Epub 2011 Jul 21.

PMID:
21840712
14.

Hierarchical regulation of WASP/WAVE proteins.

Padrick SB, Cheng HC, Ismail AM, Panchal SC, Doolittle LK, Kim S, Skehan BM, Umetani J, Brautigam CA, Leong JM, Rosen MK.

Mol Cell. 2008 Nov 7;32(3):426-38. doi: 10.1016/j.molcel.2008.10.012.

15.

Structural basis of actin filament nucleation and processive capping by a formin homology 2 domain.

Otomo T, Tomchick DR, Otomo C, Panchal SC, Machius M, Rosen MK.

Nature. 2005 Feb 3;433(7025):488-94. Epub 2005 Jan 5.

PMID:
15635372
16.
17.

A conserved amphipathic helix in WASP/Scar proteins is essential for activation of Arp2/3 complex.

Panchal SC, Kaiser DA, Torres E, Pollard TD, Rosen MK.

Nat Struct Biol. 2003 Aug;10(8):591-8.

PMID:
12872157
18.

A novel protocol based on HN(C)N for rapid resonance assignment in ((15)N, (13)C) labeled proteins: implications to structural genomics.

Chatterjee A, Bhavesh NS, Panchal SC, Hosur RV.

Biochem Biophys Res Commun. 2002 Apr 26;293(1):427-32.

PMID:
12054618
19.
20.

An efficient high-throughput resonance assignment procedure for structural genomics and protein folding research by NMR.

Bhavesh NS, Panchal SC, Hosur RV.

Biochemistry. 2001 Dec 11;40(49):14727-35.

PMID:
11732891
22.

Real time NMR monitoring of local unfolding of HIV-1 protease tethered dimer driven by autolysis.

Panchal SC, Bhavesh NS, Hosur RV.

FEBS Lett. 2001 May 18;497(1):59-64.

23.

Solution structure and dynamics of GCN4 cognate DNA: NMR investigations.

Khandelwal P, Panchal SC, Radha PK, Hosur RV.

Nucleic Acids Res. 2001 Jan 15;29(2):499-505.

24.

Cloning, expression and purification of the DNA binding domain of RFX protein.

Panchal SC, Madan A, Hosur RV.

Indian J Biochem Biophys. 1999 Dec;36(6):429-32.

PMID:
10844997
25.

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