Leyla Arik
Amgen
9 Papers
66 Citations
Leyla Arik is an academic researcher from Amgen. The author has contributed to research in topics: Receptor antagonist & Bradykinin. The author has an hindex of 7, co-authored 9 publications.
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Papers
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
Narender R. Gavva,Anthony W. Bannon,David N. Hovland,Sonya G. Lehto,Lana Klionsky,Sekhar Surapaneni,David C. Immke,Charles Henley,Leyla Arik,Annette Bak,James Davis,Nadia B. Ernst,Gal Hever,Rongzhen Kuang,Licheng Shi,Rami Tamir,Jue Wang,Weiya Wang,Gary Zajic,Dawn Zhu,Mark H. Norman,Jean-Claude Louis,Ella Magal,James J. S. Treanor +23 more
TL;DR: The in vitro and in vivo characterization of a novel and selective TRPV1 antagonist, AMG 517, and its pharmacology with that of a closely related analog, tert-butyl-2-(6-([2-(acetylamino)-1,3-benzothiazol-4-yl]oxy)pyrimidin- 4-yl)-5-(trifluoromethyl)phenylcarbamate (AMG8163) suggest that
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Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists.
Jian J. Chen,Wenyuan Qian,Kaustav Biswas,Vellarkad N. Viswanadhan,Benny C. Askew,Stephen Hitchcock,Randall W. Hungate,Leyla Arik,Eileen Johnson +8 more
TL;DR: A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.
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Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Kaustav Biswas,Aiwen Li,Jian J. Chen,Derin C. D'amico,Christopher H. Fotsch,Nianhe Han,Jason Brooks Human,Qingyian Liu,Mark H. Norman,Bobby Riahi,Chester Chenguang Yuan,Hideo Suzuki,David A. Mareska,James Zhan,David E. Clarke,Andras Toro,Robert D. Groneberg,Burgess Laurence E,Dianna Lester-Zeiner,Gloria Biddlecome,Barton H. Manning,Leyla Arik,Hong Dong,Ming Huang,Augustus Kamassah,Richard Loeloff,Hong Sun,Feng-Yin Hsieh,Gondi N. Kumar,Gordon Ng,Randall W. Hungate,Benny C. Askew,Eileen Johnson +32 more
TL;DR: The most potent analog at the human receptor, compound 38, was also active in a rabbit B1 receptor cellular assay and displayed in vivo activity in two rabbit models, a pharmacodynamic model with a blood pressure readout and an efficacy model of inflammatory pain.
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Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor Antagonist with Anti-Inflammatory Activity
Derin C. D'amico,Toshi Aya,Jason Brooks Human,Christopher H. Fotsch,Jian J. Chen,Kaustav Biswas,Bobby Riahi,Mark H. Norman,Christopher A. Willoughby,Randall W. Hungate,Paul J. Reider,Gloria Biddlecome,Dianna Lester-Zeiner,Carlo van Staden,Eileen Johnson,Augustus Kamassah,Leyla Arik,Judy Wang,Vellarkad N. Viswanadhan,Robert D. Groneberg,James Zhan,Hideo Suzuki,Andras Toro,David A. Mareska,David E. Clarke,Darren Martin Harvey,Burgess Laurence E,Laird Ellen,Benny C. Askew,Gordon Ng +29 more
TL;DR: The discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, and rabbit bradykinin B1 receptors, is reported and a novel method to calculate entropy is introduced and ascribed approximately 30% of the gained affinity to decreased conformational entropy.
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Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.
Kaustav Biswas,Tanya Peterkin,Marian C. Bryan,Leyla Arik,Sonya G. Lehto,Hong Sun,Feng-Yin Hsieh,Cen Xu,Robert T. Fremeau,Jennifer R. Allen +9 more
TL;DR: A novel series of potent phthalazinone B1 antagonists, where a sulfonamide acceptor is replaced with a cyclic carbonyl unit and compounds with subnanomolar B1 binding affinity are revealed.
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