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Page 1
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR. Gerstenberger BS, et al. Among authors: parikh m. J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3. J Med Chem. 2016. PMID: 27115555 Free PMC article.
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Taylor AP, Swewczyk M, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, Ferreira de Freitas R, Tatlock J, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown PJ, Arrowsmith CH, Owen DR. Taylor AP, et al. Among authors: parikh md. J Med Chem. 2019 Sep 12;62(17):7669-7683. doi: 10.1021/acs.jmedchem.9b00112. Epub 2019 Sep 3. J Med Chem. 2019. PMID: 31415173
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R. Vazquez ML, et al. Among authors: parikh md. J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29298069
Chemoselective Preparation of Clickable Aryl Sulfonyl Fluoride Monomers: A Toolbox of Highly Functionalized Intermediates for Chemical Biology Probe Synthesis.
Fadeyi O, Parikh MD, Chen MZ, Kyne RE Jr, Taylor AP, O'Doherty I, Kaiser SE, Barbas S, Niessen S, Shi M, Weinrich SL, Kath JC, Jones LH, Robinson RP. Fadeyi O, et al. Among authors: parikh md. Chembiochem. 2016 Oct 17;17(20):1925-1930. doi: 10.1002/cbic.201600427. Epub 2016 Aug 30. Chembiochem. 2016. PMID: 27504718
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
Gopalsamy A, Narayanan A, Liu S, Parikh MD, Kyne RE Jr, Fadeyi O, Tones MA, Cherry JJ, Nabhan JF, LaRosa G, Petersen DN, Menard C, Foley TL, Noell S, Ren Y, Loria PM, Maglich-Goodwin J, Rong H, Jones LH. Gopalsamy A, et al. Among authors: parikh md. J Med Chem. 2017 Apr 13;60(7):3094-3108. doi: 10.1021/acs.jmedchem.7b00124. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28257199
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.
Gopalsamy A, Aulabaugh AE, Barakat A, Beaumont KC, Cabral S, Canterbury DP, Casimiro-Garcia A, Chang JS, Chen MZ, Choi C, Dow RL, Fadeyi OO, Feng X, France SP, Howard RM, Janz JM, Jasti J, Jasuja R, Jones LH, King-Ahmad A, Knee KM, Kohrt JT, Limberakis C, Liras S, Martinez CA, McClure KF, Narayanan A, Narula J, Novak JJ, O'Connell TN, Parikh MD, Piotrowski DW, Plotnikova O, Robinson RP, Sahasrabudhe PV, Sharma R, Thuma BA, Vasa D, Wei L, Wenzel AZ, Withka JM, Xiao J, Yayla HG. Gopalsamy A, et al. Among authors: parikh md. J Med Chem. 2021 Jan 14;64(1):326-342. doi: 10.1021/acs.jmedchem.0c01518. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356244
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Meyers MJ, Pelc M, Kamtekar S, Day J, Poda GI, Hall MK, Michener ML, Reitz BA, Mathis KJ, Pierce BS, Parikh MD, Mischke DA, Long SA, Parlow JJ, Anderson DR, Thorarensen A. Meyers MJ, et al. Among authors: parikh md. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137931
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.
Nagarajan SR, Lu HF, Gasiecki AF, Khanna IK, Parikh MD, Desai BN, Rogers TE, Clare M, Chen BB, Russell MA, Keene JL, Duffin T, Engleman VW, Finn MB, Freeman SK, Klover JA, Nickols GA, Nickols MA, Shannon KE, Steininger CA, Westlin WF, Westlin MM, Williams ML. Nagarajan SR, et al. Among authors: parikh md. Bioorg Med Chem. 2007 May 15;15(10):3390-412. doi: 10.1016/j.bmc.2007.03.020. Epub 2007 Mar 13. Bioorg Med Chem. 2007. PMID: 17387018
635 results