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Items: 27

1.

Optimized arylomycins are a new class of Gram-negative antibiotics.

Smith PA, Koehler MFT, Girgis HS, Yan D, Chen Y, Chen Y, Crawford JJ, Durk MR, Higuchi RI, Kang J, Murray J, Paraselli P, Park S, Phung W, Quinn JG, Roberts TC, Rougé L, Schwarz JB, Skippington E, Wai J, Xu M, Yu Z, Zhang H, Tan MW, Heise CE.

Nature. 2018 Sep;561(7722):189-194. doi: 10.1038/s41586-018-0483-6. Epub 2018 Sep 12.

PMID:
30209367
2.

Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA.

Alexander MK, Miu A, Oh A, Reichelt M, Ho H, Chalouni C, Labadie S, Wang L, Liang J, Nickerson NN, Hu H, Yu L, Du M, Yan D, Park S, Kim J, Xu M, Sellers BD, Purkey HE, Skelton NJ, Koehler MFT, Payandeh J, Verma V, Xu Y, Koth CM, Nishiyama M.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01142-18. doi: 10.1128/AAC.01142-18. Print 2018 Nov.

3.

Structural basis for dual-mode inhibition of the ABC transporter MsbA.

Ho H, Miu A, Alexander MK, Garcia NK, Oh A, Zilberleyb I, Reichelt M, Austin CD, Tam C, Shriver S, Hu H, Labadie SS, Liang J, Wang L, Wang J, Lu Y, Purkey HE, Quinn J, Franke Y, Clark K, Beresini MH, Tan MW, Sellers BD, Maurer T, Koehler MFT, Wecksler AT, Kiefer JR, Verma V, Xu Y, Nishiyama M, Payandeh J, Koth CM.

Nature. 2018 May;557(7704):196-201. doi: 10.1038/s41586-018-0083-5. Epub 2018 May 2.

PMID:
29720648
4.

A Putative Bacterial ABC Transporter Circumvents the Essentiality of Signal Peptidase.

Morisaki JH, Smith PA, Date SV, Kajihara KK, Truong CL, Modrusan Z, Yan D, Kang J, Xu M, Shah IM, Mintzer R, Kofoed EM, Cheung TK, Arnott D, Koehler MF, Heise CE, Brown EJ, Tan MW, Hazenbos WL.

MBio. 2016 Sep 6;7(5). pii: e00412-16. doi: 10.1128/mBio.00412-16.

5.

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Ramaswamy S, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini M.

ACS Med Chem Lett. 2016 Apr 5;7(6):595-600. doi: 10.1021/acsmedchemlett.6b00044. eCollection 2016 Jun 9.

6.

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Koehler MF, Bergeron P, Blackwood EM, Bowman K, Clark KR, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini MH.

ACS Med Chem Lett. 2016 Jan 6;7(3):223-8. doi: 10.1021/acsmedchemlett.5b00278. eCollection 2016 Mar 10.

7.

An integrated suite of modeling tools that empower scientists in structure- and property-based drug design.

Feng JA, Aliagas I, Bergeron P, Blaney JM, Bradley EK, Koehler MF, Lee ML, Ortwine DF, Tsui V, Wu J, Gobbi A.

J Comput Aided Mol Des. 2015 Jun;29(6):511-23. doi: 10.1007/s10822-015-9845-4. Epub 2015 Apr 29.

PMID:
25921252
8.

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.

ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9.

9.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G.

ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12.

10.

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ.

J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31.

PMID:
23659214
11.

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, Sideris S, St-Jean F, Trinh L, Truong T, Lyssikatos JP.

J Med Chem. 2013 Apr 11;56(7):3090-101. doi: 10.1021/jm400194n. Epub 2013 Mar 29.

PMID:
23473235
12.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP.

ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10.

13.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP.

J Med Chem. 2012 Dec 27;55(24):10958-71. doi: 10.1021/jm301389h. Epub 2012 Dec 12.

PMID:
23199076
14.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.

J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28.

PMID:
22698084
15.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP.

J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15.

PMID:
21495671
16.

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.

Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB.

J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2.

PMID:
21366295
17.

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. doi: 10.1016/j.bmcl.2010.02.021. Epub 2010 Feb 8. Erratum in: Bioorg Med Chem Lett. 2012 Jan 1;22(1):753-4.

PMID:
20189383
18.

GDC-0449-a potent inhibitor of the hedgehog pathway.

Robarge KD, Brunton SA, Castanedo GM, Cui Y, Dina MS, Goldsmith R, Gould SE, Guichert O, Gunzner JL, Halladay J, Jia W, Khojasteh C, Koehler MF, Kotkow K, La H, Lalonde RL, Lau K, Lee L, Marshall D, Marsters JC Jr, Murray LJ, Qian C, Rubin LL, Salphati L, Stanley MS, Stibbard JH, Sutherlin DP, Ubhayaker S, Wang S, Wong S, Xie M.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5576-81. doi: 10.1016/j.bmcl.2009.08.049. Epub 2009 Aug 15. Erratum in: Bioorg Med Chem Lett. 2010 Jan 15;20(2):771.

PMID:
19716296
19.

A new synthetic approach to the C ring of known as well as novel bryostatin analogues.

Wender PA, Koehler MF, Sendzik M.

Org Lett. 2003 Nov 27;5(24):4549-52.

PMID:
14627380
20.

Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.

Zobel K, Koehler MF, Beresini MH, Caris LD, Combs D.

Bioorg Med Chem Lett. 2003 May 5;13(9):1513-5.

PMID:
12699744
21.

Origins of PDZ domain ligand specificity. Structure determination and mutagenesis of the Erbin PDZ domain.

Skelton NJ, Koehler MF, Zobel K, Wong WL, Yeh S, Pisabarro MT, Yin JP, Lasky LA, Sidhu SS.

J Biol Chem. 2003 Feb 28;278(9):7645-54. Epub 2002 Nov 20.

22.

Albumin affinity tags increase peptide half-life in vivo.

Koehler MF, Zobel K, Beresini MH, Caris LD, Combs D, Paasch BD, Lazarus RA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2883-6.

PMID:
12270169
23.

The Erbin PDZ domain binds with high affinity and specificity to the carboxyl termini of delta-catenin and ARVCF.

Laura RP, Witt AS, Held HA, Gerstner R, Deshayes K, Koehler MF, Kosik KS, Sidhu SS, Lasky LA.

J Biol Chem. 2002 Apr 12;277(15):12906-14. Epub 2002 Jan 30.

24.

The rational design of potential chemotherapeutic agents: synthesis of bryostatin analogues.

Wender PA, Hinkle KW, Koehler MF, Lippa B.

Med Res Rev. 1999 Sep;19(5):388-407. Review.

PMID:
10502742
25.

The design, computer modeling, solution structure, and biological evaluation of synthetic analogs of bryostatin 1.

Wender PA, DeBrabander J, Harran PG, Jimenez JM, Koehler MF, Lippa B, Park CM, Siedenbiedel C, Pettit GR.

Proc Natl Acad Sci U S A. 1998 Jun 9;95(12):6624-9.

26.

Child psychiatric nursing option.

Koehler MF.

Nurs Outlook. 1981 Mar;29(3):174-7. No abstract available.

PMID:
6907850
27.

In vitro effects of desoxycorticosterone on vascular smooth muscle.

Koehler MF, Webb RC, Jones AW, Bohr DF.

Am J Physiol. 1979 Aug;237(2):H197-203.

PMID:
464113

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