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Items: 23


Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity.

Pillow TH, Adhikari P, Blake RA, Chen J, Del Rosario G, Deshmukh G, Figueroa I, Gascoigne KE, Kamath AV, Kaufman S, Kleinheinz T, Kozak KR, Latifi B, Leipold DD, Sing Li C, Li R, Mulvihill MM, O'Donohue A, Rowntree RK, Sadowsky JD, Wai J, Wang X, Wu C, Xu Z, Yao H, Yu SF, Zhang D, Zang R, Zhang H, Zhou H, Zhu X, Dragovich PS.

ChemMedChem. 2019 Oct 31. doi: 10.1002/cmdc.201900497. [Epub ahead of print]


Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues.

Zhang D, Dragovich PS, Yu SF, Ma Y, Pillow TH, Sadowsky JD, Su D, Wang W, Polson A, Khojasteh SC, Hop CECA.

Drug Metab Dispos. 2019 Oct;47(10):1146-1155. doi: 10.1124/dmd.119.087023. Epub 2019 Jul 29.


Catalytic Cleavage of Disulfide Bonds in Small Molecules and Linkers of Antibody-Drug Conjugates.

Zhang D, Fourie-O'Donohue A, Dragovich PS, Pillow TH, Sadowsky JD, Kozak KR, Cass RT, Liu L, Deng Y, Liu Y, Hop CECA, Khojasteh SC.

Drug Metab Dispos. 2019 Oct;47(10):1156-1163. doi: 10.1124/dmd.118.086132. Epub 2019 May 13.


Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody-Drug Conjugates with Phenol-Containing Payloads.

Zhang D, Le H, Cruz-Chuh JD, Bobba S, Guo J, Staben L, Zhang C, Ma Y, Kozak KR, Lewis Phillips GD, Vollmar BS, Sadowsky JD, Vandlen R, Wei B, Su D, Fan P, Dragovich PS, Khojasteh SC, Hop CECA, Pillow TH.

Bioconjug Chem. 2018 Feb 21;29(2):267-274. doi: 10.1021/acs.bioconjchem.7b00576. Epub 2018 Feb 7.


Intratumoral Payload Concentration Correlates with the Activity of Antibody-Drug Conjugates.

Zhang D, Yu SF, Khojasteh SC, Ma Y, Pillow TH, Sadowsky JD, Su D, Kozak KR, Xu K, Polson AG, Dragovich PS, Hop CECA.

Mol Cancer Ther. 2018 Mar;17(3):677-685. doi: 10.1158/1535-7163.MCT-17-0697. Epub 2018 Jan 18.


Development of Efficient Chemistry to Generate Site-Specific Disulfide-Linked Protein- and Peptide-Payload Conjugates: Application to THIOMAB Antibody-Drug Conjugates.

Sadowsky JD, Pillow TH, Chen J, Fan F, He C, Wang Y, Yan G, Yao H, Xu Z, Martin S, Zhang D, Chu P, Dela Cruz-Chuh J, O'Donohue A, Li G, Del Rosario G, He J, Liu L, Ng C, Su D, Lewis Phillips GD, Kozak KR, Yu SF, Xu K, Leipold D, Wai J.

Bioconjug Chem. 2017 Aug 16;28(8):2086-2098. doi: 10.1021/acs.bioconjchem.7b00258. Epub 2017 Jul 13.


Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates.

Pillow TH, Sadowsky JD, Zhang D, Yu SF, Del Rosario G, Xu K, He J, Bhakta S, Ohri R, Kozak KR, Ha E, Junutula JR, Flygare JA.

Chem Sci. 2017 Jan 1;8(1):366-370. doi: 10.1039/c6sc01831a. Epub 2016 Aug 22.


Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates.

Zhang D, Pillow TH, Ma Y, Cruz-Chuh JD, Kozak KR, Sadowsky JD, Lewis Phillips GD, Guo J, Darwish M, Fan P, Chen J, He C, Wang T, Yao H, Xu Z, Chen J, Wai J, Pei Z, Hop CE, Khojasteh SC, Dragovich PS.

ACS Med Chem Lett. 2016 Aug 26;7(11):988-993. eCollection 2016 Nov 10.


Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates.

Zhang D, Yu SF, Ma Y, Xu K, Dragovich PS, Pillow TH, Liu L, Del Rosario G, He J, Pei Z, Sadowsky JD, Erickson HK, Hop CE, Khojasteh SC.

Drug Metab Dispos. 2016 Sep;44(9):1517-23. doi: 10.1124/dmd.116.070631. Epub 2016 Jul 14.


A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1.

Rettenmaier TJ, Sadowsky JD, Thomsen ND, Chen SC, Doak AK, Arkin MR, Wells JA.

Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5. doi: 10.1073/pnas.1415365112. Epub 2014 Dec 17.


Ordering a dynamic protein via a small-molecule stabilizer.

Wang N, Majmudar CY, Pomerantz WC, Gagnon JK, Sadowsky JD, Meagher JL, Johnson TK, Stuckey JA, Brooks CL 3rd, Wells JA, Mapp AK.

J Am Chem Soc. 2013 Mar 6;135(9):3363-6. doi: 10.1021/ja3122334. Epub 2013 Feb 22.


Turning a protein kinase on or off from a single allosteric site via disulfide trapping.

Sadowsky JD, Burlingame MA, Wolan DW, McClendon CL, Jacobson MP, Wells JA.

Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):6056-61. doi: 10.1073/pnas.1102376108. Epub 2011 Mar 23.


High-resolution structural characterization of a helical alpha/beta-peptide foldamer bound to the anti-apoptotic protein Bcl-xL.

Lee EF, Sadowsky JD, Smith BJ, Czabotar PE, Peterson-Kaufman KJ, Colman PM, Gellman SH, Fairlie WD.

Angew Chem Int Ed Engl. 2009;48(24):4318-22. doi: 10.1002/anie.200805761.


Hydrophile scanning as a complement to alanine scanning for exploring and manipulating protein-protein recognition: application to the Bim BH3 domain.

Boersma MD, Sadowsky JD, Tomita YA, Gellman SH.

Protein Sci. 2008 Jul;17(7):1232-40. doi: 10.1110/ps.032896.107. Epub 2008 May 8.


A fluorescence polarization assay for identifying ligands that bind to vascular endothelial growth factor.

Peterson KJ, Sadowsky JD, Scheef EA, Pal S, Kourentzi KD, Willson RC, Bresnick EH, Sheibani N, Gellman SH.

Anal Biochem. 2008 Jul 1;378(1):8-14. doi: 10.1016/j.ab.2008.03.043. Epub 2008 Mar 28.


Exploration of structure--activity relationships among foldamer ligands for a specific protein binding site via parallel and split-and-mix library synthesis.

Murray JK, Sadowsky JD, Scalf M, Smith LM, Tomita Y, Gellman SH.

J Comb Chem. 2008 Mar-Apr;10(2):204-15. doi: 10.1021/cc700153z. Epub 2008 Feb 15.


H/D exchange- and mass spectrometry-based strategy for the thermodynamic analysis of protein-ligand binding.

Tang L, Hopper ED, Tong Y, Sadowsky JD, Peterson KJ, Gellman SH, Fitzgerald MC.

Anal Chem. 2007 Aug 1;79(15):5869-77. Epub 2007 Jun 21.


(alpha/beta+alpha)-peptide antagonists of BH3 domain/Bcl-x(L) recognition: toward general strategies for foldamer-based inhibition of protein-protein interactions.

Sadowsky JD, Fairlie WD, Hadley EB, Lee HS, Umezawa N, Nikolovska-Coleska Z, Wang S, Huang DC, Tomita Y, Gellman SH.

J Am Chem Soc. 2007 Jan 10;129(1):139-54.


Efficient synthesis of a beta-peptide combinatorial library with microwave irradiation.

Murray JK, Farooqi B, Sadowsky JD, Scalf M, Freund WA, Smith LM, Chen J, Gellman SH.

J Am Chem Soc. 2005 Sep 28;127(38):13271-80.


Chimeric (alpha/beta + alpha)-peptide ligands for the BH3-recognition cleft of Bcl-XL: critical role of the molecular scaffold in protein surface recognition.

Sadowsky JD, Schmitt MA, Lee HS, Umezawa N, Wang S, Tomita Y, Gellman SH.

J Am Chem Soc. 2005 Aug 31;127(34):11966-8.


NMR studies on the solution structure of a deletion mutant of the transcarboxylase biotin carrier subunit.

Jank MM, Sadowsky JD, Peikert C, Berger S.

Int J Biol Macromol. 2002 Oct 1;30(5):233-42.


Ring-closing metathesis of olefinic peptides: design, synthesis, and structural characterization of macrocyclic helical peptides.

Blackwell HE, Sadowsky JD, Howard RJ, Sampson JN, Chao JA, Steinmetz WE, O'Leary DJ, Grubbs RH.

J Org Chem. 2001 Aug 10;66(16):5291-302.


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