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The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.
Kauppi B, Jakob C, Färnegårdh M, Yang J, Ahola H, Alarcon M, Calles K, Engström O, Harlan J, Muchmore S, Ramqvist AK, Thorell S, Ohman L, Greer J, Gustafsson JA, Carlstedt-Duke J, Carlquist M. Kauppi B, et al. Among authors: harlan j. J Biol Chem. 2003 Jun 20;278(25):22748-54. doi: 10.1074/jbc.M212711200. Epub 2003 Apr 9. J Biol Chem. 2003. PMID: 12686538 Free article.
Discovery of potent inhibitors of dihydroneopterin aldolase using CrystaLEAD high-throughput X-ray crystallographic screening and structure-directed lead optimization.
Sanders WJ, Nienaber VL, Lerner CG, McCall JO, Merrick SM, Swanson SJ, Harlan JE, Stoll VS, Stamper GF, Betz SF, Condroski KR, Meadows RP, Severin JM, Walter KA, Magdalinos P, Jakob CG, Wagner R, Beutel BA. Sanders WJ, et al. Among authors: harlan je. J Med Chem. 2004 Mar 25;47(7):1709-18. doi: 10.1021/jm030497y. J Med Chem. 2004. PMID: 15027862
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Gu WZ, Joseph I, Wang YC, Frost D, Sullivan GM, Wang L, Lin NH, Cohen J, Stoll VS, Jakob CG, Muchmore SW, Harlan JE, Holzman T, Walten KA, Ladror US, Anderson MG, Kroeger P, Rodriguez LE, Jarvis KP, Ferguson D, Marsh K, Ng S, Rosenberg SH, Sham HL, Zhang H. Gu WZ, et al. Among authors: harlan je. Anticancer Drugs. 2005 Nov;16(10):1059-69. doi: 10.1097/00001813-200511000-00004. Anticancer Drugs. 2005. PMID: 16222147
Design and characterization of an engineered gp41 protein from human immunodeficiency virus-1 as a tool for drug discovery.
Stewart KD, Steffy K, Harris K, Harlan JE, Stoll VS, Huth JR, Walter KA, Gramling-Evans E, Mendoza RR, Severin JM, Richardson PL, Barrett LW, Matayoshi ED, Swift KM, Betz SF, Muchmore SW, Kempf DJ, Molla A. Stewart KD, et al. Among authors: harlan je. J Comput Aided Mol Des. 2007 Jan-Mar;21(1-3):121-30. doi: 10.1007/s10822-007-9107-1. Epub 2007 Feb 9. J Comput Aided Mol Des. 2007. PMID: 17294246
From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae.
Lerner CG, Hajduk PJ, Wagner R, Wagenaar FL, Woodall C, Gu YG, Searle XB, Florjancic AS, Zhang T, Clark RF, Cooper CS, Mack JC, Yu L, Cai M, Betz SF, Chovan LE, McCall JO, Black-Schaefer CL, Kakavas SJ, Schurdak ME, Comess KM, Walter KA, Edalji R, Dorwin SA, Smith RA, Hebert EJ, Harlan JE, Metzger RE, Merta PJ, Baranowski JL, Coen ML, Thornewell SJ, Shivakumar AG, Saiki AY, Soni N, Bui M, Balli DJ, Sanders WJ, Nilius AM, Holzman TF, Fesik SW, Beutel BA. Lerner CG, et al. Among authors: harlan je. Chem Biol Drug Des. 2007 Jun;69(6):395-404. doi: 10.1111/j.1747-0285.2007.00521.x. Chem Biol Drug Des. 2007. PMID: 17581233
A high throughput fluorescent assay for measuring the activity of fatty acid amide hydrolase.
Kage KL, Richardson PL, Traphagen L, Severin J, Pereda-Lopez A, Lubben T, Davis-Taber R, Vos MH, Bartley D, Walter K, Harlan J, Solomon L, Warrior U, Holzman TF, Faltynek C, Surowy CS, Scott VE. Kage KL, et al. Among authors: harlan j. J Neurosci Methods. 2007 Mar 30;161(1):47-54. doi: 10.1016/j.jneumeth.2006.10.006. Epub 2006 Nov 2. J Neurosci Methods. 2007. PMID: 17083980
331 results