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Donald Karanewsky

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Guy Servant; Catherine Tachdjian; Xiaodong Li; Donald S Karanewsky
The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor.
Guy Servant; Catherine Tachdjian; Xiao-Qing Tang; Sara Werner; Feng Zhang; Xiaodong Li; Poonit Kamdar; Goran Petrovic; Tanya Ditschun; Antoniette Java; Paul Brust; Nicole Brune; Grant E DuBois; Mark Zoller; Donald S Karanewsky
Positive allosteric modulators of the human sweet taste receptor enhance sweet taste.
Robert Epple; Christopher Cow; Yongping Xie; Mihai Azimioara; Ross Russo; Xing Wang; John Wityak; Donald S Karanewsky; Tove tuntland; Vân T B Nguyêñ-Trân; Cara Cuc Ngo; David Huang; Enrique Saez; Tracy A Spalding; Andrea Gerken; Maya Iskandar; H Martin Seidel; Shin-Shay Tian
Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.

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All Publications

2011: Guy Servant; Catherine Tachdjian; Xiaodong Li; Donald S Karanewsky
The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor.
Trends in pharmacological sciences 2011;32(11):631-6.
2010: Guy Servant; Catherine Tachdjian; Xiao-Qing Tang; Sara Werner; Feng Zhang; Xiaodong Li; Poonit Kamdar; Goran Petrovic; Tanya Ditschun; Antoniette Java; Paul Brust; Nicole Brune; Grant E DuBois; Mark Zoller; Donald S Karanewsky
Positive allosteric modulators of the human sweet taste receptor enhance sweet taste.
Proceedings of the National Academy of Sciences of the United States of America 2010;107(10):4746-51.
2010: Robert Epple; Christopher Cow; Yongping Xie; Mihai Azimioara; Ross Russo; Xing Wang; John Wityak; Donald S Karanewsky; Tove tuntland; Vân T B Nguyêñ-Trân; Cara Cuc Ngo; David Huang; Enrique Saez; Tracy A Spalding; Andrea Gerken; Maya Iskandar; H Martin Seidel; Shin-Shay Tian
Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.
Journal of medicinal chemistry 2010;53(1):77-105.
2009: Guobao Zhang; Pingda Ren; Nathanael S Gray; Taebo Sim; Xia Wang; Yi Liu; Jianwei Che; Weitong Dong; Shin-Shay Tian; Mark L Sandberg; Tracy A Spalding; Russell Romeo; Maya Iskandar; Zhiliang Wang; H Martin Seidel; Donald S Karanewsky; Yun He
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
Bioorganic & medicinal chemistry letters 2009;19(23):6691-5.
2008: Guobao Zhang; Pingda Ren; Nathanael S Gray; Taebo Sim; Yi Liu; Xia Wang; Jianwei Che; Shin-Shay Tian; Mark L Sandberg; Tracy A Spalding; Russell Romeo; Maya Iskandar; Donald Chow; H Martin Seidel; Donald S Karanewsky; Yun He
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
Bioorganic & medicinal chemistry letters 2008;18(20):5618-21.
2008: Thomas H Marsilje; Phil B Alper; Wenshuo Lu; Daniel Mutnick; Pierre-Yves Michellys; Yun He; Donald S Karanewsky; Donald Chow; Andrea Gerken; Jianmin Lao; Min-Ju Kim; H Martin Seidel; Shin-Shay Tian
Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.
Bioorganic & medicinal chemistry letters 2008;18(19):5259-62.
2008: Phil B Alper; Thomas H Marsilje; Daniel Mutnick; Wenshuo Lu; Arnab Chatterjee; Michael J Roberts; Yun He; Donald S Karanewsky; Donald Chow; Jianmin Lao; Andrea Gerken; Tove tuntland; Bo Liu; Jonathan Chang; Perry Gordon; H Martin Seidel; Shin-Shay Tian
Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.
Bioorganic & medicinal chemistry letters 2008;18(19):5255-8.
2008: Steven L Roach; Robert I Higuchi; Mark E Adams; Yan Liu; Donald S Karanewsky; Keith B Marschke; Dale E Mais; Jeffrey N Miner; Lin Zhi
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Bioorganic & medicinal chemistry letters 2008;18(12):3504-8.
2008: Yun Oliver Long; Robert I Higuchi; Thomas R Caferro; Thomas L S Lau; Min Wu; Marquis L Cummings; Esther Martinborough; Keith B Marschke; William Y Chang; Francisco J López; Donald S Karanewsky; Lin Zhi
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Bioorganic & medicinal chemistry letters 2008;18(9):2967-71.
2007: Robert I Higuchi; Anthony W Thompson; Jyun-Hung Chen; Thomas R Caferro; Marquis L Cummings; Charlotte P Deckhut; Mark E Adams; Christopher M Tegley; James P Edwards; Francisco J López; E Adam Kallel; Donald S Karanewsky; William T Schrader; Keith B Marschke; Lin Zhi
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
Bioorganic & medicinal chemistry letters 2007;17(19):5442-6.
2007: Robert J Ardecky; Andrew R Hudson; Dean P Phillips; John S Tyhonas; Charlotte Deckhut; Thomas L Lau; Yongkai Li; Esther Martinborough; Steven L Roach; Robert I Higuchi; Francisco J Lopez; Keith B Marschke; Jeffrey N Miner; Donald S Karanewsky; Andrés Negro-Vilar; Lin Zhi
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Bioorganic & medicinal chemistry letters 2007;17(15):4158-62.
2006: Robert Epple; Mihai Azimioara; Ross Russo; Yongping Xie; Xing Wang; Christopher Cow; John Wityak; Donald S Karanewsky; Badry Bursulaya; Andreas Kreusch; Tove tuntland; Andrea Gerken; Maya Iskandar; Enrique Saez; H Martin Seidel; Shin-Shay Tian
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Bioorganic & medicinal chemistry letters 2006;16(21):5488-92.
2006: David C Tully; Hong Liu; Arnab K Chatterjee; Phil B Alper; Jennifer A Williams; Michael J Roberts; Daniel Mutnick; David Woodmansee; Thomas Hollenbeck; Perry Gordon; Jonathan Chang; Tove tuntland; Christine Tumanut; Jun Li; Jennifer L Harris; Donald S Karanewsky
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(19):5107-11.
2006: David C Tully; Hong Liu; Arnab K Chatterjee; Phil B Alper; Robert Epple; Jennifer A Williams; Michael J Roberts; David Woodmansee; Brian T Masick; Christine Tumanut; Jun Li; Glen Spraggon; Michael Hornsby; Jonathan Chang; Tove tuntland; Thomas Hollenbeck; Perry Gordon; Jennifer L Harris; Donald S Karanewsky
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Bioorganic & medicinal chemistry letters 2006;16(19):5112-7.
2006: David Ellis; Kelli L Kuhen; Beth Anaclerio; Baogen Wu; Karen Wolff; Hong Yin; Badry Bursulaya; Jeremy Caldwell; Donald S Karanewsky; Yun He
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(16):4246-51.
2006: Robert Epple; Ross Russo; Mihai Azimioara; Christopher Cow; Yongping Xie; Xing Wang; John Wityak; Donald S Karanewsky; Andrea Gerken; Maya Iskandar; Enrique Saez; H Martin Seidel; Shin-Shay Tian
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
Bioorganic & medicinal chemistry letters 2006;16(16):4376-80.
2006: Baogen Wu; Kelli L Kuhen; Truc Ngoc Nguyen; David Ellis; Beth Anaclerio; Xiaohui He; Kunyong Yang; Donald S Karanewsky; Hong Yin; Karen Wolff; Kimberly Bieza; Jeremy Caldwell; Yun He
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
Bioorganic & medicinal chemistry letters 2006;16(13):3430-3.
2006: Ha-Soon Choi; Zhicheng Wang; Wendy Richmond; Xiaohui He; Kunyong Yang; Tao Jiang; Donald S Karanewsky; Xiang-ju Gu; Vicki Zhou; Yi Liu; Jianwei Che; Christian C Lee; Jeremy Caldwell; Takanori Kanazawa; Ichiro Umemura; Naoko Matsuura; Osamu Ohmori; Toshiyuki Honda; Nathanael S Gray; Yun He
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Bioorganic & medicinal chemistry letters 2006;16(10):2689-92.
2006: Tao Jiang; Kelli L Kuhen; Karen Wolff; Hong Yin; Kimberly Bieza; Jeremy Caldwell; Badry Bursulaya; Tove tuntland; Kanyin Zhang; Donald S Karanewsky; Yun He
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
Bioorganic & medicinal chemistry letters 2006;16(8):2109-12.
2006: Ha-Soon Choi; Zhicheng Wang; Wendy Richmond; Xiaohui He; Kunyong Yang; Tao Jiang; Taebo Sim; Donald S Karanewsky; Xiang-ju Gu; Vicki Zhou; Yi Liu; Osamu Ohmori; Jeremy Caldwell; Nathanael S Gray; Yun He
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
Bioorganic & medicinal chemistry letters 2006;16(8):2173-6.
2006: David C Tully; Hong Liu; Phil B Alper; Arnab K Chatterjee; Robert Epple; Michael J Roberts; Jennifer A Williams; KhanhLinh T Nguyen; David Woodmansee; Christine Tumanut; Jun Li; Glen Spraggon; Jonathan Chang; Tove tuntland; Jennifer L Harris; Donald S Karanewsky
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Bioorganic & medicinal chemistry letters 2006;16(7):1975-80.
2006: Phil B Alper; Hong Liu; Arnab K Chatterjee; KhanhLinh T Nguyen; David C Tully; Christine Tumanut; Jun Li; Jennifer L Harris; Tove tuntland; Jonathan Chang; Perry Gordon; Thomas Hollenbeck; Donald S Karanewsky
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
Bioorganic & medicinal chemistry letters 2006;16(6):1486-90.
2005: Hong Liu; David C Tully; Robert Epple; Badry Bursulaya; Jun Li; Jennifer L Harris; Jennifer A Williams; Ross Russo; Christine Tumanut; Michael J Roberts; Phil B Alper; Yun He; Donald S Karanewsky
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.
Bioorganic & medicinal chemistry letters 2005;15(22):4979-84.
2005: Brett R Ullman; Teresa Aja; Ning Chen; Jose-Luis Diaz; Xin Gu; Julia Herrmann; Vincent J Kalish; Donald S Karanewsky; Lalitha Kodandapani; Joseph J Krebs; Steven D Linton; Steven P Meduna; Kip Nalley; Edward D Robinson; Silvio P Roggo; Robert O Sayers; Albert Schmitz; Robert J Ternansky; Kevin J Tomaselli; Joe C Wu
Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.
Bioorganic & medicinal chemistry letters 2005;15(15):3632-6.
2005: Lawrence G Hamann; J Hoyt Meyer; Daniel A Ruppar; Keith B Marschke; Francisco J Lopez; Elizabeth A Allegretto; Donald S Karanewsky
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.
Bioorganic & medicinal chemistry letters 2005;15(5):1463-6.
2004: Steven D Linton; Teresa Aja; Peter R Allegrini; Thomas L Deckwerth; Jose-Luis Diaz; Bastian Hengerer; Julia Herrmann; Kathy G Jahangiri; Joerg Kallen; Donald S Karanewsky; Steven P Meduna; Kip Nalley; Edward D Robinson; Silvio P Roggo; Giorgio Rovelli; Andre Sauter; Robert O Sayers; Albert Schmitz; Robert Smidt; Robert J Ternansky; Kevin J Tomaselli; Brett R Ullman; Christoph Wiessner; Joe C Wu
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Bioorganic & medicinal chemistry letters 2004;14(10):2685-91.
2004: Pierre-Yves Michellys; Jennifer D'Arrigo; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Dale A Mais; Christopher M Mapes; Anne Reifel-Miller; Deepa Rungta; Marcus F Boehm
Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Bioorganic & medicinal chemistry letters 2004;14(6):1593-8.
2003: Pierre-Yves Michellys; Marcus F Boehm; Jyun-Hung Chen; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Anne Reifel-Miller; Kathleen M Ogilvie; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Nathan Yumibe; Robert J Ardecky
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Bioorganic & medicinal chemistry letters 2003;13(22):4071-5.
2003: Brett R Ullman; Teresa Aja; Thomas L Deckwerth; Jose-Luis Diaz; Julia Herrmann; Vincent J Kalish; Donald S Karanewsky; Steven P Meduna; Kip Nalley; Edward D Robinson; Silvio P Roggo; Robert O Sayers; Albert Schmitz; Robert J Ternansky; Kevin J Tomaselli; Joe C Wu
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Bioorganic & medicinal chemistry letters 2003;13(20):3623-6.
2003: Pierre-Yves Michellys; Robert J Ardecky; Jyun-Hung Chen; Jennifer D'Arrigo; Timothy Grese; Donald S Karanewsky; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Chahrzad Montrose-Rafizadeh; Kathleen M Ogilvie; Anne Reifel-Miller; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Marcus F Boehm
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Journal of medicinal chemistry 2003;46(19):4087-103.
2003: Pierre-Yves Michellys; Robert J Ardecky; Jyun-Hung Chen; Diane L Crombie; Garret J Etgen; Margaret M Faul; A L Faulkner; Timothy Grese; Richard A Heyman; Donald S Karanewsky; Kay Klausing; Mark D Leibowitz; Sha Liu; Dale A Mais; Christopher M Mapes; Keith B Marschke; Anne Reifel-Miller; Kathleen M Ogilvie; Deepa Rungta; Anthony W Thompson; John S Tyhonas; Marcus F Boehm
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Journal of medicinal chemistry 2003;46(13):2683-96.
2002: Steven D Linton; Donald S Karanewsky; Robert J Ternansky; Ning Chen; Xian Guo; Kathy G Jahangiri; Vincent J Kalish; Steven P Meduna; Edward D Robinson; Brett R Ullman; Joe C Wu; Brian Pham; Lalitha Kodandapani; Robert Smidt; Jose-Luis Diaz; Lawrence C Fritz; U von Krosigk; Silvio P Roggo; Albert Schmitz; Kevin J Tomaselli
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.
Bioorganic & medicinal chemistry letters 2002;12(20):2973-5.
2002: Steven D Linton; Donald S Karanewsky; Robert J Ternansky; Joe C Wu; Brian Pham; Lalitha Kodandapani; Robert Smidt; Jose-Luis Diaz; Lawrence C Fritz; Kevin J Tomaselli
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.
Bioorganic & medicinal chemistry letters 2002;12(20):2969-71.
2001: Dawn A Brooks; Garret J Etgen; Christopher J Rito; Anthony J Shuker; Samuel J Dominianni; Alan M Warshawsky; Robert J Ardecky; James R Paterniti; John S Tyhonas; Donald S Karanewsky; Raymond F Kauffman; Carol L Broderick; Brian A Oldham; Chahrzad Montrose-Rafizadeh; Leonard L Winneroski; Margaret M Faul; James R McCarthy
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Journal of medicinal chemistry 2001;44(13):2061-4.
2001: Niel C Hoglen; B P Hirakawa; C D Fisher; S Weeks; A Srinivasan; AM Wong; K L Valentino; Kevin J Tomaselli; X Bai; Donald S Karanewsky; P C Contreras
Characterization of the caspase inhibitor IDN-1965 in a model of apoptosis-associated liver injury.
The Journal of pharmacology and experimental therapeutics 2001;297(2):811-8.
1999: JF Krebs; Robert C Armstrong; Abiraman Srinivasan; Teresa Aja; AM Wong; A Aboy; R Sayers; Brian Pham; T Vu; K Hoang; Donald S Karanewsky; C Leist; A Schmitz; Joe C Wu; Kevin J Tomaselli; Lawrence C Fritz
Activation of membrane-associated procaspase-3 is regulated by Bcl-2.
The Journal of cell biology 1999;144(5):915-26.
1998: Donald S Karanewsky; X Bai; Steven D Linton; JF Krebs; J Wu; Brian Pham; Kevin J Tomaselli
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).
Bioorganic & medicinal chemistry letters 1998;8(19):2757-62.
1997: Peer R E Mittl; S Di Marco; JF Krebs; X Bai; Donald S Karanewsky; JP Priestle; Kevin J Tomaselli; Markus G Grütter
Structure of recombinant human CPP32 in complex with the tetrapeptide acetyl-Asp-Val-Ala-Asp fluoromethyl ketone.
The Journal of biological chemistry 1997;272(10):6539-47.
1997: Robert C Armstrong; Teresa Aja; K D Hoang; S Gaur; X Bai; Emad S Alnemri; Gerald Litwack; Donald S Karanewsky; Lawrence C Fritz; Kevin J Tomaselli
Activation of the CED3/ICE-related protease CPP32 in cerebellar granule neurons undergoing apoptosis but not necrosis.
The Journal of neuroscience : the official journal of the Society for Neuroscience 1997;17(2):553-62.
1996: Robert C Armstrong; T Aja; J Xiang; S Gaur; JF Krebs; K Hoang; X Bai; S J Korsmeyer; Donald S Karanewsky; Lawrence C Fritz; Kevin J Tomaselli
Fas-induced activation of the cell death-related protease CPP32 Is inhibited by Bcl-2 and by ICE family protease inhibitors.
The Journal of biological chemistry 1996;271(28):16850-5.