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Page 1
Highly selective inhibition of myosin motors provides the basis of potential therapeutic application.
Sirigu S, Hartman JJ, Planelles-Herrero VJ, Ropars V, Clancy S, Wang X, Chuang G, Qian X, Lu PP, Barrett E, Rudolph K, Royer C, Morgan BP, Stura EA, Malik FI, Houdusse AM. Sirigu S, et al. Among authors: lu pp. Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):E7448-E7455. doi: 10.1073/pnas.1609342113. Epub 2016 Nov 4. Proc Natl Acad Sci U S A. 2016. PMID: 27815532 Free PMC article.
Activation of fast skeletal muscle troponin as a potential therapeutic approach for treating neuromuscular diseases.
Russell AJ, Hartman JJ, Hinken AC, Muci AR, Kawas R, Driscoll L, Godinez G, Lee KH, Marquez D, Browne WF 4th, Chen MM, Clarke D, Collibee SE, Garard M, Hansen R, Jia Z, Lu PP, Rodriguez H, Saikali KG, Schaletzky J, Vijayakumar V, Albertus DL, Claflin DR, Morgans DJ, Morgan BP, Malik FI. Russell AJ, et al. Among authors: lu pp. Nat Med. 2012 Feb 19;18(3):452-5. doi: 10.1038/nm.2618. Nat Med. 2012. PMID: 22344294 Free PMC article.
Cardiac myosin activation: a potential therapeutic approach for systolic heart failure.
Malik FI, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M, Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W, Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Malik FI, et al. Among authors: lu pp. Science. 2011 Mar 18;331(6023):1439-43. doi: 10.1126/science.1200113. Science. 2011. PMID: 21415352 Free PMC article.
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
Morgan BP, Muci A, Lu PP, Qian X, Tochimoto T, Smith WW, Garard M, Kraynack E, Collibee S, Suehiro I, Tomasi A, Valdez SC, Wang W, Jiang H, Hartman J, Rodriguez HM, Kawas R, Sylvester S, Elias KA, Godinez G, Lee K, Anderson R, Sueoka S, Xu D, Wang Z, Djordjevic N, Malik FI, Morgans DJ Jr. Morgan BP, et al. Among authors: lu pp. ACS Med Chem Lett. 2010 Aug 20;1(9):472-7. doi: 10.1021/ml100138q. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900233 Free PMC article.
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function.
Collibee SE, Bergnes G, Chuang C, Ashcraft L, Gardina J, Garard M, Jamison CR, Lu K, Lu PP, Muci A, Romero A, Valkevich E, Wang W, Warrington J, Yao B, Durham N, Hartman J, Marquez A, Hinken A, Schaletzky J, Xu D, Hwee DT, Morgans D, Malik FI, Morgan BP. Collibee SE, et al. Among authors: lu pp, lu k. J Med Chem. 2021 Oct 28;64(20):14930-14941. doi: 10.1021/acs.jmedchem.1c01067. Epub 2021 Oct 12. J Med Chem. 2021. PMID: 34636234 Free article.
Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator.
Collibee SE, Bergnes G, Muci A, Browne WF 4th, Garard M, Hinken AC, Russell AJ, Suehiro I, Hartman J, Kawas R, Lu PP, Lee KH, Marquez D, Tomlinson M, Xu D, Kennedy A, Hwee D, Schaletzky J, Leung K, Malik FI, Morgans DJ Jr, Morgan BP. Collibee SE, et al. Among authors: lu pp. ACS Med Chem Lett. 2018 Feb 13;9(4):354-358. doi: 10.1021/acsmedchemlett.7b00546. eCollection 2018 Apr 12. ACS Med Chem Lett. 2018. PMID: 29670700 Free PMC article.
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF. Cushing TD, et al. Among authors: lu pp. Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074993
A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Jaen JC. Cushing TD, et al. Among authors: lu pp. Bioorg Med Chem Lett. 2011 Jan 1;21(1):423-6. doi: 10.1016/j.bmcl.2010.10.125. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074992
101 results