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TRV0109101, a G Protein-Biased Agonist of the µ-Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration.

Koblish M, Carr R 3rd, Siuda ER, Rominger DH, Gowen-MacDonald W, Cowan CL, Crombie AL, Violin JD, Lark MW.

J Pharmacol Exp Ther. 2017 Aug;362(2):254-262. doi: 10.1124/jpet.117.241117. Epub 2017 May 22.


Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers.

Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR.

Pain. 2014 Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19.


Biased ligands at G-protein-coupled receptors: promise and progress.

Violin JD, Crombie AL, Soergel DG, Lark MW.

Trends Pharmacol Sci. 2014 Jul;35(7):308-16. doi: 10.1016/ Epub 2014 May 28. Review. Erratum in: Trends Pharmacol Sci. 2014 Sep;35(9):489.


First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers.

Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW.

J Clin Pharmacol. 2014 Mar;54(3):351-7. doi: 10.1002/jcph.207. Epub 2014 Jan 28.


First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers.

Soergel DG, Subach RA, Cowan CL, Violin JD, Lark MW.

J Clin Pharmacol. 2013 Sep;53(9):892-9. doi: 10.1002/jcph.111. Epub 2013 Jun 29.


GPCR biased ligands as novel heart failure therapeutics.

Violin JD, Soergel DG, Boerrigter G, Burnett JC Jr, Lark MW.

Trends Cardiovasc Med. 2013 Oct;23(7):242-9. doi: 10.1016/j.tcm.2013.01.002. Epub 2013 Mar 15. Review.


A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.

DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD.

J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8.


Cardiorenal actions of TRV120027, a novel ß-arrestin-biased ligand at the angiotensin II type I receptor, in healthy and heart failure canines: a novel therapeutic strategy for acute heart failure.

Boerrigter G, Lark MW, Whalen EJ, Soergel DG, Violin JD, Burnett JC Jr.

Circ Heart Fail. 2011 Nov;4(6):770-8. doi: 10.1161/CIRCHEARTFAILURE.111.962571. Epub 2011 Aug 11.


Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.

Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M, Lark MW.

J Pharmacol Exp Ther. 2010 Dec;335(3):572-9. doi: 10.1124/jpet.110.173005. Epub 2010 Aug 26.


Mechanical injury potentiates proteoglycan catabolism induced by interleukin-6 with soluble interleukin-6 receptor and tumor necrosis factor alpha in immature bovine and adult human articular cartilage.

Sui Y, Lee JH, DiMicco MA, Vanderploeg EJ, Blake SM, Hung HH, Plaas AH, James IE, Song XY, Lark MW, Grodzinsky AJ.

Arthritis Rheum. 2009 Oct;60(10):2985-96. doi: 10.1002/art.24857.


A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.

Kumar S, Dare L, Vasko-Moser JA, James IE, Blake SM, Rickard DJ, Hwang SM, Tomaszek T, Yamashita DS, Marquis RW, Oh H, Jeong JU, Veber DF, Gowen M, Lark MW, Stroup G.

Bone. 2007 Jan;40(1):122-31. Epub 2006 Sep 7.


Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.

Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF.

J Med Chem. 2006 Mar 9;49(5):1597-612.


Human osteoarthritis synovial fluid and joint cartilage contain both aggrecanase- and matrix metalloproteinase-generated aggrecan fragments.

Struglics A, Larsson S, Pratta MA, Kumar S, Lark MW, Lohmander LS.

Osteoarthritis Cartilage. 2006 Feb;14(2):101-13. Epub 2005 Sep 26.


Increased osteoblastogenesis and decreased bone resorption protect against ovariectomy-induced bone loss in thrombospondin-2-null mice.

Hankenson KD, James IE, Apone S, Stroup GB, Blake SM, Liang X, Lark MW, Bornstein P.

Matrix Biol. 2005 Aug;24(5):362-70.


An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkey.

Marquis RW, Ward KW, Roethke T, Smith BR, Ru Y, Yamashita DS, Tomaszek TA, Gorycki PD, Cheng HY, James IE, Stroup GB, Lark MW, Gowen M, Veber DF.

Mol Pharm. 2004 Jan 12;1(1):97-100. No abstract available.


Mechanisms and kinetics of glycosaminoglycan release following in vitro cartilage injury.

DiMicco MA, Patwari P, Siparsky PN, Kumar S, Pratta MA, Lark MW, Kim YJ, Grodzinsky AJ.

Arthritis Rheum. 2004 Mar;50(3):840-8.


Ultrastructural quantification of cell death after injurious compression of bovine calf articular cartilage.

Patwari P, Gaschen V, James IE, Berger E, Blake SM, Lark MW, Grodzinsky AJ, Hunziker EB.

Osteoarthritis Cartilage. 2004 Mar;12(3):245-52.


Proteoglycan degradation after injurious compression of bovine and human articular cartilage in vitro: interaction with exogenous cytokines.

Patwari P, Cook MN, DiMicco MA, Blake SM, James IE, Kumar S, Cole AA, Lark MW, Grodzinsky AJ.

Arthritis Rheum. 2003 May;48(5):1292-301.


Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.

Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CC, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1483-6.


Rapid inhibition of thyroxine-induced bone resorption in the rat by an orally active vitronectin receptor antagonist.

Hoffman SJ, Vasko-Moser J, Miller WH, Lark MW, Gowen M, Stroup G.

J Pharmacol Exp Ther. 2002 Jul;302(1):205-11.


Novel bone antiresorptive approaches.

Lark MW, James IE.

Curr Opin Pharmacol. 2002 Jun;2(3):330-7. Review.


A potent small molecule, nonpeptide inhibitor of cathepsin K (SB 331750) prevents bone matrix resorption in the ovariectomized rat.

Lark MW, Stroup GB, James IE, Dodds RA, Hwang SM, Blake SM, Lechowska BA, Hoffman SJ, Smith BR, Kapadia R, Liang X, Erhard K, Ru Y, Dong X, Marquis RW, Veber D, Gowen M.

Bone. 2002 May;30(5):746-53.


Clusterin expression in adult human normal and osteoarthritic articular cartilage.

Connor JR, Kumar S, Sathe G, Mooney J, O'Brien SP, Mui P, Murdock PR, Gowen M, Lark MW.

Osteoarthritis Cartilage. 2001 Nov;9(8):727-37.


Biosynthetic response and mechanical properties of articular cartilage after injurious compression.

Kurz B, Jin M, Patwari P, Cheng DM, Lark MW, Grodzinsky AJ.

J Orthop Res. 2001 Nov;19(6):1140-6.


In vitro models for investigation of the effects of acute mechanical injury on cartilage.

Patwari P, Fay J, Cook MN, Badger AM, Kerin AJ, Lark MW, Grodzinsky AJ.

Clin Orthop Relat Res. 2001 Oct;(391 Suppl):S61-71. Review.


Identification and initial characterization of 5000 expressed sequenced tags (ESTs) each from adult human normal and osteoarthritic cartilage cDNA libraries.

Kumar S, Connor JR, Dodds RA, Halsey W, Van Horn M, Mao J, Sathe G, Mui P, Agarwal P, Badger AM, Lee JC, Gowen M, Lark MW.

Osteoarthritis Cartilage. 2001 Oct;9(7):641-53.


Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.

Stroup GB, Lark MW, Veber DF, Bhattacharyya A, Blake S, Dare LC, Erhard KF, Hoffman SJ, James IE, Marquis RW, Ru Y, Vasko-Moser JA, Smith BR, Tomaszek T, Gowen M.

J Bone Miner Res. 2001 Oct;16(10):1739-46.


Azepanone-based inhibitors of human and rat cathepsin K.

Marquis RW, Ru Y, LoCastro SM, Zeng J, Yamashita DS, Oh HJ, Erhard KF, Davis LD, Tomaszek TA, Tew D, Salyers K, Proksch J, Ward K, Smith B, Levy M, Cummings MD, Haltiwanger RC, Trescher G, Wang B, Hemling ME, Quinn CJ, Cheng HY, Lin F, Smith WW, Janson CA, Zhao B, McQueney MS, D'Alessio K, Lee CP, Marzulli A, Dodds RA, Blake S, Hwang SM, James IE, Gress CJ, Bradley BR, Lark MW, Gowen M, Veber DF.

J Med Chem. 2001 Apr 26;44(9):1380-95.


Human osteoclast cathepsin K is processed intracellularly prior to attachment and bone resorption.

Dodds RA, James IE, Rieman D, Ahern R, Hwang SM, Connor JR, Thompson SD, Veber DF, Drake FH, Holmes S, Lark MW, Gowen M.

J Bone Miner Res. 2001 Mar;16(3):478-86.


Disease-modifying activity of SB 273005, an orally active, nonpeptide alphavbeta3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthritis.

Badger AM, Blake S, Kapadia R, Sarkar S, Levin J, Swift BA, Hoffman SJ, Stroup GB, Miller WH, Gowen M, Lark MW.

Arthritis Rheum. 2001 Jan;44(1):128-37.


Antagonism of the osteoclast vitronectin receptor with an orally active nonpeptide inhibitor prevents cancellous bone loss in the ovariectomized rat.

Lark MW, Stroup GB, Dodds RA, Kapadia R, Hoffman SJ, Hwang SM, James IE, Lechowska B, Liang X, Rieman DJ, Salyers KL, Ward K, Smith BR, Miller WH, Huffman WF, Gowen M.

J Bone Miner Res. 2001 Feb;16(2):319-27.


Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitro.

James IE, Marquis RW, Blake SM, Hwang SM, Gress CJ, Ru Y, Zembryki D, Yamashita DS, McQueney MS, Tomaszek TA, Oh HJ, Gowen M, Veber DF, Lark MW.

J Biol Chem. 2001 Apr 13;276(15):11507-11. Epub 2001 Jan 8. Erratum in: J Biol Chem. 2003 Aug 22;278(34):32484.


Markers of joint tissue turnover in joint fluids from hips with osteonecrosis of the femoral head.

Jingushi S, Lohmander LS, Shinmei M, Hoerrner LA, Lark MW, Sugioka Y, Iwamoto Y.

J Orthop Res. 2000 Sep;18(5):728-33.


FrzB-2: a human secreted frizzled-related protein with a potential role in chondrocyte apoptosis.

James IE, Kumar S, Barnes MR, Gress CJ, Hand AT, Dodds RA, Connor JR, Bradley BR, Campbell DA, Grabill SE, Williams K, Blake SM, Gowen M, Lark MW.

Osteoarthritis Cartilage. 2000 Nov;8(6):452-63.


Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures.

Badger AM, Roshak AK, Cook MN, Newman-Tarr TM, Swift BA, Carlson K, Connor JR, Lee JC, Gowen M, Lark MW, Kumar S.

Osteoarthritis Cartilage. 2000 Nov;8(6):434-43.


Injurious mechanical compression of bovine articular cartilage induces chondrocyte apoptosis.

Loening AM, James IE, Levenston ME, Badger AM, Frank EH, Kurz B, Nuttall ME, Hung HH, Blake SM, Grodzinsky AJ, Lark MW.

Arch Biochem Biophys. 2000 Sep 15;381(2):205-12.


Meniscal ossification in spontaneous osteoarthritis in the guinea-pig.

Kapadia RD, Badger AM, Levin JM, Swift B, Bhattacharyya A, Dodds RA, Coatney RW, Lark MW.

Osteoarthritis Cartilage. 2000 Sep;8(5):374-7.


Inhibition of caspase-3-like activity prevents apoptosis while retaining functionality of human chondrocytes in vitro.

Nuttall ME, Nadeau DP, Fisher PW, Wang F, Keller PM, DeWolf WE Jr, Goldring MB, Badger AM, Lee D, Levy MA, Gowen M, Lark MW.

J Orthop Res. 2000 May;18(3):356-63.


Identification and in vivo efficacy of small-molecule antagonists of integrin alphavbeta3 (the vitronectin receptor).

Miller WH, Keenan RM, Willette RN, Lark MW.

Drug Discov Today. 2000 Sep;5(9):397-408.


Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.

Lee D, Long SA, Adams JL, Chan G, Vaidya KS, Francis TA, Kikly K, Winkler JD, Sung CM, Debouck C, Richardson S, Levy MA, DeWolf WE Jr, Keller PM, Tomaszek T, Head MS, Ryan MD, Haltiwanger RC, Liang PH, Janson CA, McDevitt PJ, Johanson K, Concha NO, Chan W, Abdel-Meguid SS, Badger AM, Lark MW, Nadeau DP, Suva LJ, Gowen M, Nuttall ME.

J Biol Chem. 2000 May 26;275(21):16007-14.


Differential expression of egr-1 in osteoarthritic compared to normal adult human articular cartilage.

Wang FL, Connor JR, Dodds RA, James IE, Kumar S, Zou C, Lark MW, Gowen M, Nuttall ME.

Osteoarthritis Cartilage. 2000 May;8(3):161-9.


CKbeta-8 [CCL23], a novel CC chemokine, is chemotactic for human osteoclast precursors and is expressed in bone tissues.

Votta BJ, White JR, Dodds RA, James IE, Connor JR, Lee-Rykaczewski E, Eichman CF, Kumar S, Lark MW, Gowen M.

J Cell Physiol. 2000 May;183(2):196-207.


Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

J Med Chem. 2000 Jan 13;43(1):22-6. No abstract available.


Down-regulation of chondrocyte aggrecan and type-II collagen gene expression correlates with increases in static compression magnitude and duration.

Ragan PM, Badger AM, Cook M, Chin VI, Gowen M, Grodzinsky AJ, Lark MW.

J Orthop Res. 1999 Nov;17(6):836-42.


Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.

Lark MW, Stroup GB, Hwang SM, James IE, Rieman DJ, Drake FH, Bradbeer JN, Mathur A, Erhard KF, Newlander KA, Ross ST, Salyers KL, Smith BR, Miller WH, Huffman WF, Gowen M.

J Pharmacol Exp Ther. 1999 Nov;291(2):612-7.


Development and characterization of a human in vitro resorption assay: demonstration of utility using novel antiresorptive agents.

James IE, Lark MW, Zembryki D, Lee-Rykaczewski EV, Hwang SM, Tomaszek TA, Belfiore P, Gowen M.

J Bone Miner Res. 1999 Sep;14(9):1562-9.


Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Huffman WF, et al.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.


Applications of micro-CT and MR microscopy to study pre-clinical models of osteoporosis and osteoarthritis.

Kapadia RD, Stroup GB, Badger AM, Koller B, Levin JM, Coatney RW, Dodds RA, Liang X, Lark MW, Gowen M.

Technol Health Care. 1998 Dec;6(5-6):361-72.


Transport of tissue inhibitor of metalloproteinases-1 through cartilage: contributions of fluid flow and electrical migration.

Garcia AM, Lark MW, Trippel SB, Grodzinsky AJ.

J Orthop Res. 1998 Nov;16(6):734-42.


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