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Items: 1 to 50 of 58

1.

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.

Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A.

J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30.

PMID:
30423248
2.

Correction to Discovery of the Hemifumarate and (α-l-Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group.

Robinson RP, Reiter LA, Barth WE, Campeta AM, Cooper K, Cronin BJ, Destito R, Donahue KM, Falkner FC, Fiese EF, Johnson DL, Kuperman AV, Liston TE, Malloy D, Martin JJ, Mitchell DY, Rusek FW, Shamblin SL, Wright CF.

J Med Chem. 2018 Apr 12;61(7):3237. doi: 10.1021/acs.jmedchem.8b00306. Epub 2018 Mar 28. No abstract available.

PMID:
29589934
3.

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.

J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23.

PMID:
29298069
4.

Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue.

Fadeyi OO, Hoth LR, Choi C, Feng X, Gopalsamy A, Hett EC, Kyne RE Jr, Robinson RP, Jones LH.

ACS Chem Biol. 2017 Aug 18;12(8):2015-2020. doi: 10.1021/acschembio.7b00403. Epub 2017 Jul 20.

PMID:
28718624
5.

Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis.

Fadeyi O, Parikh MD, Chen MZ, Kyne RE Jr, Taylor AP, O'Doherty I, Kaiser SE, Barbas S, Niessen S, Shi M, Weinrich SL, Kath JC, Jones LH, Robinson RP.

Chembiochem. 2016 Oct 17;17(20):1925-1930. doi: 10.1002/cbic.201600427. Epub 2016 Aug 30.

PMID:
27504718
6.

Modern advances in heterocyclic chemistry in drug discovery.

Taylor AP, Robinson RP, Fobian YM, Blakemore DC, Jones LH, Fadeyi O.

Org Biomol Chem. 2016 Jul 12;14(28):6611-37. doi: 10.1039/c6ob00936k. Review.

PMID:
27282396
8.

Suboptimal Component Position Leading to Severe Wear of an Alumina-Alumina Total Hip Coupling: Biomechanical Analysis and Documentation of Limited Tissue Response.

Carvajal Alba JA, Elpers ME, Rosenberg AE, Robinson RP.

HSS J. 2015 Jul;11(2):166-71. doi: 10.1007/s11420-015-9443-y. Epub 2015 May 27. No abstract available.

9.

A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS.

Xu H, Hett EC, Gopalsamy A, Parikh MD, Geoghegan KF, Kyne RE Jr, Menard CA, Narayanan A, Robinson RP, Johnson DS, Tones MA, Jones LH.

Mol Biosyst. 2015 Oct;11(10):2709-12. doi: 10.1039/c5mb00288e.

PMID:
25959423
10.

2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.

Chantigny YA, Murray JC, Kleinman EF, Robinson RP, Plotkin MA, Reese MR, Buckbinder L, McNiff PA, Millham ML, Schaefer JF, Abramov YA, Bordner J.

J Med Chem. 2015 Mar 26;58(6):2658-77. doi: 10.1021/jm501601b. Epub 2015 Mar 17.

PMID:
25706100
11.

Rational targeting of active-site tyrosine residues using sulfonyl fluoride probes.

Hett EC, Xu H, Geoghegan KF, Gopalsamy A, Kyne RE Jr, Menard CA, Narayanan A, Parikh MD, Liu S, Roberts L, Robinson RP, Tones MA, Jones LH.

ACS Chem Biol. 2015 Apr 17;10(4):1094-8. doi: 10.1021/cb5009475. Epub 2015 Jan 29.

PMID:
25571984
12.

The effect of viscosity on cement penetration in total knee arthroplasty, an application of the squeeze film effect.

Silverman EJ, Landy DC, Massel DH, Kaimrajh DN, Latta LL, Robinson RP.

J Arthroplasty. 2014 Oct;29(10):2039-42. doi: 10.1016/j.arth.2014.05.010. Epub 2014 May 24.

PMID:
25007724
13.

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y.

J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31.

PMID:
23234271
14.

From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.

Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5.

PMID:
23177788
15.

Pharmacodynamic model of sodium-glucose transporter 2 (SGLT2) inhibition: implications for quantitative translational pharmacology.

Maurer TS, Ghosh A, Haddish-Berhane N, Sawant-Basak A, Boustany-Kari CM, She L, Leininger MT, Zhu T, Tugnait M, Yang X, Kimoto E, Mascitti V, Robinson RP.

AAPS J. 2011 Dec;13(4):576-84. doi: 10.1208/s12248-011-9297-2. Epub 2011 Aug 26.

16.

Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus.

Kalgutkar AS, Tugnait M, Zhu T, Kimoto E, Miao Z, Mascitti V, Yang X, Tan B, Walsky RL, Chupka J, Feng B, Robinson RP.

Drug Metab Dispos. 2011 Sep;39(9):1609-19. doi: 10.1124/dmd.111.040675. Epub 2011 Jun 20.

PMID:
21690265
17.

Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.

Robinson RP, Bartlett JA, Bertinato P, Bessire AJ, Cosgrove J, Foley PM, Manion TB, Minich ML, Ramos B, Reese MR, Schmahai TJ, Swick AG, Tess DA, Vaz A, Wolford A.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. doi: 10.1016/j.bmcl.2011.05.099. Epub 2011 Jun 2.

PMID:
21684740
18.

Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.

Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T.

J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30.

PMID:
21449606
19.

Eleven-year implant survival rates of the all-polyethylene and metal-backed modular Optetrak posterior stabilized knee in bilateral simultaneous cases.

Robinson RP, Green TM.

J Arthroplasty. 2011 Dec;26(8):1165-9. doi: 10.1016/j.arth.2011.01.009. Epub 2011 Mar 16.

PMID:
21414746
20.

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

McClure KF, Darout E, Guimarães CR, DeNinno MP, Mascitti V, Munchhof MJ, Robinson RP, Kohrt J, Harris AR, Moore DE, Li B, Samp L, Lefker BA, Futatsugi K, Kung D, Bonin PD, Cornelius P, Wang R, Salter E, Hornby S, Kalgutkar AS, Chen Y.

J Med Chem. 2011 Mar 24;54(6):1948-52. doi: 10.1021/jm200003p. Epub 2011 Mar 1.

PMID:
21361292
21.

Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.

Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25.

PMID:
21310611
22.

Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro.

Kalgutkar AS, Mascitti V, Sharma R, Walker GW, Ryder T, McDonald TS, Chen Y, Preville C, Basak A, McClure KF, Kohrt JT, Robinson RP, Munchhof MJ, Cornelius P.

Chem Res Toxicol. 2011 Feb 18;24(2):269-78. doi: 10.1021/tx100429x. Epub 2011 Feb 3.

PMID:
21288051
23.

C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.

Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21.

PMID:
20149653
24.

Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.

Robinson RP, Buckbinder L, Haugeto AI, McNiff PA, Millham ML, Reese MR, Schaefer JF, Abramov YA, Bordner J, Chantigny YA, Kleinman EF, Laird ER, Morgan BP, Murray JC, Salter ED, Wessel MD, Yocum SA.

J Med Chem. 2009 Mar 26;52(6):1731-43. doi: 10.1021/jm801512v.

PMID:
19239259
25.

The impact of resident teaching on total hip arthroplasty.

Robinson RP.

Clin Orthop Relat Res. 2007 Dec;465:196-201.

PMID:
18090473
26.
27.

Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.

Blagg JA, Noe MC, Wolf-Gouveia LA, Reiter LA, Laird ER, Chang SP, Danley DE, Downs JT, Elliott NC, Eskra JD, Griffiths RJ, Hardink JR, Haugeto AI, Jones CS, Liras JL, Lopresti-Morrow LL, Mitchell PG, Pandit J, Robinson RP, Subramanyam C, Vaughn-Bowser ML, Yocum SA.

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1807-10.

PMID:
15780611
28.

The early innovators of today's resurfacing condylar knees.

Robinson RP.

J Arthroplasty. 2005 Jan;20(1 Suppl 1):2-26.

PMID:
15647728
29.

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.

Reiter LA, Robinson RP, McClure KF, Jones CS, Reese MR, Mitchell PG, Otterness IG, Bliven ML, Liras J, Cortina SR, Donahue KM, Eskra JD, Griffiths RJ, Lame ME, Lopez-Anaya A, Martinelli GJ, McGahee SM, Yocum SA, Lopresti-Morrow LL, Tobiassen LM, Vaughn-Bowser ML.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3389-95.

PMID:
15177439
30.

The glucocorticoid receptor: molecular mechanism and new therapeutic opportunities.

Buckbinder L, Robinson RP.

Curr Drug Targets Inflamm Allergy. 2002 Jun;1(2):127-36. Review.

PMID:
14561195
31.

Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors.

Robinson RP, Laird ER, Donahue KM, Lopresti-Morrow LL, Mitchell PG, Reese MR, Reeves LM, Rouch AI, Stam EJ, Yocum SA.

Bioorg Med Chem Lett. 2001 May 7;11(9):1211-3.

PMID:
11354379
32.

Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.

Robinson RP, Laird ER, Blake JF, Bordner J, Donahue KM, Lopresti-Morrow LL, Mitchell PG, Reese MR, Reeves LM, Stam EJ, Yocum SA.

J Med Chem. 2000 Jun 15;43(12):2293-6. No abstract available.

PMID:
10882354
33.

Joint motion and surface contact area related to component position in total hip arthroplasty.

Robinson RP, Simonian PT, Gradisar IM, Ching RP.

J Bone Joint Surg Br. 1997 Jan;79(1):140-6.

PMID:
9020463
36.

Discovery of the hemifumarate and (alpha-L-alanyloxy)methyl ether as prodrugs of an antirheumatic oxindole: prodrugs for the enolic OH group.

Robinson RP, Reiter LA, Barth WE, Campeta AM, Cooper K, Cronin BJ, Destito R, Donahue KM, Falkner FC, Fiese EF, Johnson DL, Kuperman AV, Liston TE, Malloy D, Martin JJ, Mitchell DY, Rusek FW, Shamblin SL, Wright CF.

J Med Chem. 1996 Jan 5;39(1):10-8. Erratum in: J Med Chem. 2018 Apr 12;61(7):3237.

PMID:
8568796
37.

Reduction of intracellular pH by tenidap. Involvement of cellular anion transporters in the pH change.

McNiff P, Robinson RP, Gabel CA.

Biochem Pharmacol. 1995 Oct 26;50(9):1421-32.

PMID:
7503793
38.

Thermal expansion modular femoral head extractor for revision total hip arthroplasty.

Robinson RP, Simonian PT.

J Arthroplasty. 1995 Aug;10(4):476-9.

PMID:
8523007
39.

Titanium contamination of recycled Cell Saver blood in revision hip arthroplasty.

Simonian PT, Robinson RP.

J Arthroplasty. 1995 Feb;10(1):83-6.

PMID:
7730835
40.

Late infection of a bipolar prosthesis following endoscopy. A case report.

Vanderhooft JE, Robinson RP.

J Bone Joint Surg Am. 1994 May;76(5):744-6. No abstract available.

PMID:
8175823
41.

Hip arthroplasty using the cementless CLS stem. A 2--4-year experience.

Robinson RP, Lovell TP, Green TM.

J Arthroplasty. 1994 Apr;9(2):177-92.

PMID:
8014649
42.

Social catastrophe: orphaned by AIDS.

Robinson RP, Monk E, Coon L, Blanford C, Mason S.

JAMA. 1993 Apr 21;269(15):1942. No abstract available.

PMID:
8464122
43.

Technetium-99m-labeled platelets: comparison of labeling with a new lipid-soluble Sn(II)-mercaptopyridine-N-oxide and 99mTc-HMPAO.

Dewanjee MK, Robinson RP, Hellman RL, Ganz WI, Serafini AN, Sfakianakis GN.

Int J Rad Appl Instrum B. 1991;18(5):461-8.

PMID:
1917515
44.

Quantitation of platelet loss with indium-111 labeled platelets in a hollow-fiber membrane oxygenator and arterial filter during extracorporeal circulation in a pig model.

Palatianos GM, Dewanjee MK, Robinson RP, Novak S, Dewanjee PK, Kapadvanjwala M, Hsu LC, Sfakianakis GN, Kaiser GA.

ASAIO Trans. 1989 Jul-Sep;35(3):667-70.

PMID:
2597560
45.

Kinetics and quantitation of In-111 labeled platelet deposition on control and heparin-bonded polyurethane angio catheters in a dog model.

Dewanjee MK, Rowland SM, Robinson RP, Dewanjee PK, Halgovich JL, Kapadvanjwala M, MacGregor DC, Serafini AN, Palatianos GM, Sfakianakis GN.

ASAIO Trans. 1989 Jul-Sep;35(3):365-8.

PMID:
2597481
46.

Early femoral component loosening in DF-80 total hip arthroplasty.

Robinson RP, Lovell TP, Green TM, Bailey GA.

J Arthroplasty. 1989;4(1):55-64.

PMID:
2926409
47.

Failure of carbon fiber-reinforced polyethylene total knee-replacement components. A report of two cases.

Wright TM, Astion DJ, Bansal M, Rimnac CM, Green T, Insall JN, Robinson RP.

J Bone Joint Surg Am. 1988 Jul;70(6):926-32. No abstract available.

PMID:
3292535
48.

Pest control in hospitals.

Robinson RP.

J Hosp Infect. 1988 Feb;11 Suppl A:64-7. No abstract available.

PMID:
2896748
49.

Near normalization of metabolism of IDDM: comparison of continuous subcutaneous (CSII) versus intraperitoneal (CIPII) insulin delivery.

Gooch BR, Abumrad NN, Robinson RP, Crofford OB.

Horm Metab Res. 1984 Dec;16 Suppl 1:190-4.

PMID:
6398261
50.

The effect of thyroid hormones on gluconeogenesis and forearm metabolism in man.

Sandler MP, Robinson RP, Rabin D, Lacy WW, Abumrad NN.

J Clin Endocrinol Metab. 1983 Mar;56(3):479-85.

PMID:
6822648

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