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Items: 1 to 50 of 130

1.

Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Ryder TF, Calabrese MF, Walker GS, Cameron KO, Reyes AR, Borzilleri KA, Delmore J, Miller R, Kurumbail RG, Ward J, Kung DW, Brown JA, Edmonds DJ, Eng H, Wolford AC, Kalgutkar AS.

J Med Chem. 2018 Aug 2. doi: 10.1021/acs.jmedchem.8b00807. [Epub ahead of print]

PMID:
30036059
2.

Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models.

Esquejo RM, Salatto CT, Delmore J, Albuquerque B, Reyes A, Shi Y, Moccia R, Cokorinos E, Peloquin M, Monetti M, Barricklow J, Bollinger E, Smith BK, Day EA, Nguyen C, Geoghegan KF, Kreeger JM, Opsahl A, Ward J, Kalgutkar AS, Tess D, Butler L, Shirai N, Osborne TF, Steinberg GR, Birnbaum MJ, Cameron KO, Miller RA.

EBioMedicine. 2018 May;31:122-132. doi: 10.1016/j.ebiom.2018.04.009. Epub 2018 Apr 8.

3.

Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

Menhaji-Klotz E, Hesp KD, Londregan AT, Kalgutkar AS, Piotrowski DW, Boehm M, Song K, Ryder T, Beaumont K, Jones RM, Atkinson K, Brown JA, Litchfield J, Xiao J, Canterbury DP, Burford K, Thuma BA, Limberakis C, Jiao W, Bagley SW, Agarwal S, Crowell D, Pazdziorko S, Ward J, Price DA, Clerin V.

J Med Chem. 2018 Apr 26;61(8):3685-3696. doi: 10.1021/acs.jmedchem.8b00190. Epub 2018 Apr 17.

PMID:
29627981
4.

A sensitive method for the quantitation of the peptide-based glucagon-like peptide-1 receptor agonist liraglutide in plasma using microfluidics chromatography tandem MS.

King-Ahmad AJ, Kalgutkar AS, Niosi M, Eng H, Holliman C.

Bioanalysis. 2018 Mar 1;10(5):357-368. doi: 10.4155/bio-2017-0239. Epub 2018 Mar 8.

PMID:
29516741
5.

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO.

J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28.

PMID:
29466005
6.

Establishing Transcriptional Signatures to Differentiate PXR-, CAR-, and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes.

Moscovitz JE, Kalgutkar AS, Nulick K, Johnson N, Lin Z, Goosen TC, Weng Y.

J Pharmacol Exp Ther. 2018 May;365(2):262-271. doi: 10.1124/jpet.117.247296. Epub 2018 Feb 12.

PMID:
29440451
7.

Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.

Boehm M, Beaumont K, Jones R, Kalgutkar AS, Zhang L, Atkinson K, Bai G, Brown JA, Eng H, Goetz GH, Holder BR, Khunte B, Lazzaro S, Limberakis C, Ryu S, Shapiro MJ, Tylaska L, Yan J, Turner R, Leung SSF, Ramaseshan M, Price DA, Liras S, Jacobson MP, Earp DJ, Lokey RS, Mathiowetz AM, Menhaji-Klotz E.

J Med Chem. 2017 Dec 14;60(23):9653-9663. doi: 10.1021/acs.jmedchem.7b01028. Epub 2017 Oct 30.

8.

Induction of human cytochrome P450 3A4 by the irreversible myeloperoxidase inactivator PF-06282999 is mediated by the pregnane X receptor.

Moscovitz JE, Lin Z, Johnson N, Tu M, Goosen TC, Weng Y, Kalgutkar AS.

Xenobiotica. 2018 Jul;48(7):647-655. doi: 10.1080/00498254.2017.1353163. Epub 2017 Jul 24.

PMID:
28685622
9.

Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice.

Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO, Tran JL, Jatkar A, Cialdea K, Esquejo RM, Meissen J, Calabrese MF, Cordes J, Moccia R, Tess D, Salatto CT, Coskran TM, Opsahl AC, Flynn D, Blatnik M, Li W, Kindt E, Foretz M, Viollet B, Ward J, Kurumbail RG, Kalgutkar AS, Wojtaszewski JFP, Cameron KO, Miller RA.

Cell Metab. 2017 May 2;25(5):1147-1159.e10. doi: 10.1016/j.cmet.2017.04.010.

10.

Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy.

Salatto CT, Miller RA, Cameron KO, Cokorinos E, Reyes A, Ward J, Calabrese MF, Kurumbail RG, Rajamohan F, Kalgutkar AS, Tess DA, Shavnya A, Genung NE, Edmonds DJ, Jatkar A, Maciejewski BS, Amaro M, Gandhok H, Monetti M, Cialdea K, Bollinger E, Kreeger JM, Coskran TM, Opsahl AC, Boucher GG, Birnbaum MJ, DaSilva-Jardine P, Rolph T.

J Pharmacol Exp Ther. 2017 May;361(2):303-311. doi: 10.1124/jpet.116.237925. Epub 2017 Mar 13.

11.

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue.

Price DA, Eng H, Farley KA, Goetz GH, Huang Y, Jiao Z, Kalgutkar AS, Kablaoui NM, Khunte B, Liras S, Limberakis C, Mathiowetz AM, Ruggeri RB, Quan JM, Yang Z.

Org Biomol Chem. 2017 Mar 28;15(12):2501-2506. doi: 10.1039/c7ob00096k. Epub 2017 Mar 7.

PMID:
28266673
12.

Examination of the Human Cytochrome P4503A4 Induction Potential of PF-06282999, an Irreversible Myeloperoxidase Inactivator: Integration of Preclinical, In Silico, and Biomarker Methodologies in the Prediction of the Clinical Outcome.

Dong JQ, Gosset JR, Fahmi OA, Lin Z, Chabot JR, Terra SG, Le V, Chidsey K, Nouri P, Kim A, Buckbinder L, Kalgutkar AS.

Drug Metab Dispos. 2017 May;45(5):501-511. doi: 10.1124/dmd.116.074476. Epub 2017 Mar 2.

13.

Liabilities Associated with the Formation of "Hard" Electrophiles in Reactive Metabolite Trapping Screens.

Kalgutkar AS.

Chem Res Toxicol. 2017 Jan 17;30(1):220-238. doi: 10.1021/acs.chemrestox.6b00332. Epub 2016 Nov 10.

PMID:
27802597
14.

Inhibition of Hepatobiliary Transport Activity by the Antibacterial Agent Fusidic Acid: Insights into Factors Contributing to Conjugated Hyperbilirubinemia/Cholestasis.

Lapham K, Novak J, Marroquin LD, Swiss R, Qin S, Strock CJ, Scialis R, Aleo MD, Schroeter T, Eng H, Rodrigues AD, Kalgutkar AS.

Chem Res Toxicol. 2016 Oct 4. [Epub ahead of print]

PMID:
27676153
15.

Transporter-Mediated Hepatic Uptake Plays an Important Role in the Pharmacokinetics and Drug-Drug Interactions of Montelukast.

Varma MV, Kimoto E, Scialis R, Bi Y, Lin J, Eng H, Kalgutkar AS, El-Kattan AF, Rodrigues AD, Tremaine LM.

Clin Pharmacol Ther. 2017 Mar;101(3):406-415. doi: 10.1002/cpt.520. Epub 2016 Nov 18.

PMID:
27648490
16.

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.

Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J.

J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20.

PMID:
27490827
17.

Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.

Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J.

ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19.

PMID:
27391855
18.

Simulation of human plasma concentration-time profiles of the partial glucokinase activator PF-04937319 and its disproportionate N-demethylated metabolite using humanized chimeric mice and semi-physiological pharmacokinetic modeling.

Kamimura H, Ito S, Chijiwa H, Okuzono T, Ishiguro T, Yamamoto Y, Nishinoaki S, Ninomiya SI, Mitsui M, Kalgutkar AS, Yamazaki H, Suemizu H.

Xenobiotica. 2017 May;47(5):382-393. doi: 10.1080/00498254.2016.1199063. Epub 2016 Jul 7.

PMID:
27389028
19.

Tracking Where the O's Go.

Kalgutkar AS.

ACS Cent Sci. 2015 Jul 22;1(4):163-5. doi: 10.1021/acscentsci.5b00231. Epub 2015 Jun 22. No abstract available.

20.

Optimization of amide-based EP3 receptor antagonists.

Lee EC, Futatsugi K, Arcari JT, Bahnck K, Coffey SB, Derksen DR, Kalgutkar AS, Loria PM, Sharma R.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2670-5. doi: 10.1016/j.bmcl.2016.04.009. Epub 2016 Apr 9.

PMID:
27107947
21.

Species Differences in the Oxidative Desulfurization of a Thiouracil-Based Irreversible Myeloperoxidase Inactivator by Flavin-Containing Monooxygenase Enzymes.

Eng H, Sharma R, Wolford A, Di L, Ruggeri RB, Buckbinder L, Conn EL, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2016 Aug;44(8):1262-9. doi: 10.1124/dmd.116.070185. Epub 2016 Apr 14.

22.

The Antimicrobial Agent Fusidic Acid Inhibits Organic Anion Transporting Polypeptide-Mediated Hepatic Clearance and May Potentiate Statin-Induced Myopathy.

Eng H, Scialis RJ, Rotter CJ, Lin J, Lazzaro S, Varma MV, Di L, Feng B, West M, Kalgutkar AS.

Drug Metab Dispos. 2016 May;44(5):692-9. doi: 10.1124/dmd.115.067447. Epub 2016 Feb 17.

23.

Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans.

Dong JQ, Varma MV, Wolford A, Ryder T, Di L, Feng B, Terra SG, Sagawa K, Kalgutkar AS.

Drug Metab Dispos. 2016 Feb;44(2):209-19. doi: 10.1124/dmd.115.067868. Epub 2015 Nov 25.

24.

Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.

Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS.

J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28.

PMID:
26509551
25.

Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides.

Schwochert J, Turner R, Thang M, Berkeley RF, Ponkey AR, Rodriguez KM, Leung SS, Khunte B, Goetz G, Limberakis C, Kalgutkar AS, Eng H, Shapiro MJ, Mathiowetz AM, Price DA, Liras S, Jacobson MP, Lokey RS.

Org Lett. 2015 Jun 19;17(12):2928-31. doi: 10.1021/acs.orglett.5b01162. Epub 2015 Jun 5.

PMID:
26046483
26.

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products.

Bockus AT, Lexa KW, Pye CR, Kalgutkar AS, Gardner JW, Hund KC, Hewitt WM, Schwochert JA, Glassey E, Price DA, Mathiowetz AM, Liras S, Jacobson MP, Lokey RS.

J Med Chem. 2015 Jun 11;58(11):4581-9. doi: 10.1021/acs.jmedchem.5b00128. Epub 2015 May 20.

PMID:
25950816
27.

Revisiting N-to-O acyl shift for synthesis of natural product-like cyclic depsipeptides.

Schwochert J, Pye C, Ahlbach C, Abdollahian Y, Farley K, Khunte B, Limberakis C, Kalgutkar AS, Eng H, Shapiro MJ, Mathiowetz AM, Price DA, Liras S, Lokey RS.

Org Lett. 2014 Dec 5;16(23):6088-91. doi: 10.1021/ol503170b. Epub 2014 Nov 20.

PMID:
25412436
28.

Practical approaches to resolving reactive metabolite liabilities in early discovery.

Dalvie D, Kalgutkar AS, Chen W.

Drug Metab Rev. 2015 Feb;47(1):56-70. doi: 10.3109/03602532.2014.984813. Epub 2014 Nov 20. Review.

PMID:
25410913
30.

Comparison of the circulating metabolite profile of PF-04991532, a hepatoselective glucokinase activator, across preclinical species and humans: potential implications in metabolites in safety testing assessment.

Sharma R, Litchfield J, Bergman A, Atkinson K, Kazierad D, Gustavson SM, Di L, Pfefferkorn JA, Kalgutkar AS.

Drug Metab Dispos. 2015 Feb;43(2):190-8. doi: 10.1124/dmd.114.061218. Epub 2014 Nov 10.

31.

Predicting toxicities of reactive metabolite-positive drug candidates.

Kalgutkar AS, Dalvie D.

Annu Rev Pharmacol Toxicol. 2015;55:35-54. doi: 10.1146/annurev-pharmtox-010814-124720. Epub 2014 Oct 6. Review.

PMID:
25292426
32.

Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC, Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2014 Nov;42(11):1926-39. doi: 10.1124/dmd.114.060087. Epub 2014 Aug 20.

33.

Pharmacokinetics and metabolism studies on the glucagon-like peptide-1 (GLP-1)-derived metabolite GLP-1(9-36)amide in male Beagle dogs.

Eng H, Sharma R, McDonald TS, Landis MS, Stevens BD, Kalgutkar AS.

Xenobiotica. 2014 Sep;44(9):842-8. doi: 10.3109/00498254.2014.897011. Epub 2014 Mar 4.

PMID:
24588343
34.

Identification of a novel conformationally constrained glucagon receptor antagonist.

Lee EC, Tu M, Stevens BD, Bian J, Aspnes G, Perreault C, Sammons MF, Wright SW, Litchfield J, Kalgutkar AS, Sharma R, Didiuk MT, Ebner DC, Filipski KJ, Brown J, Atkinson K, Pfefferkorn JA, Guzman-Perez A.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. doi: 10.1016/j.bmcl.2013.12.090. Epub 2013 Dec 28.

PMID:
24418771
35.

Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.

Kalgutkar AS, Frederick KS, Hatch HL, Ambler CM, Perry DA, Garigipati RS, Chang GC, Lefker BA, Clark RW, Morehouse LA, Francone O, Hu X.

Xenobiotica. 2014 Jul;44(7):591-605. doi: 10.3109/00498254.2013.874611. Epub 2013 Dec 31.

PMID:
24380613
36.

In vitro metabolism of the glucagon-like peptide-1 (GLP-1)-derived metabolites GLP-1(9-36)amide and GLP-1(28-36)amide in mouse and human hepatocytes.

Sharma R, McDonald TS, Eng H, Limberakis C, Stevens BD, Patel S, Kalgutkar AS.

Drug Metab Dispos. 2013 Dec;41(12):2148-57. doi: 10.1124/dmd.113.054254. Epub 2013 Sep 20.

37.

Drug metabolites as cytochrome p450 inhibitors: a retrospective analysis and proposed algorithm for evaluation of the pharmacokinetic interaction potential of metabolites in drug discovery and development.

Callegari E, Kalgutkar AS, Leung L, Obach RS, Plowchalk DR, Tse S.

Drug Metab Dispos. 2013 Dec;41(12):2047-55. doi: 10.1124/dmd.113.052241. Epub 2013 Jun 21.

38.

Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor.

Eng H, Sharma R, McDonald TS, Edmonds DJ, Fortin JP, Li X, Stevens BD, Griffith DA, Limberakis C, Nolte WM, Price DA, Jackson M, Kalgutkar AS.

Drug Metab Dispos. 2013 Aug;41(8):1470-9. doi: 10.1124/dmd.113.052183. Epub 2013 May 7.

39.

Elucidation of the biochemical basis for a clinical drug-drug interaction between atorvastatin and 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha.

Kalgutkar AS, Chen D, Varma MV, Feng B, Terra SG, Scialis RJ, Rotter CJ, Frederick KS, West MA, Goosen TC, Gosset JR, Walsky RL, Francone OL.

Xenobiotica. 2013 Nov;43(11):963-72. doi: 10.3109/00498254.2013.791004. Epub 2013 Apr 30.

PMID:
23631744
40.

Reactive metabolite trapping studies on imidazo- and 2-methylimidazo[2,1-b]thiazole-based inverse agonists of the ghrelin receptor.

Kalgutkar AS, Ryder TF, Walker GS, Orr ST, Cabral S, Goosen TC, Lapham K, Eng H.

Drug Metab Dispos. 2013 Jul;41(7):1375-88. doi: 10.1124/dmd.113.051839. Epub 2013 Apr 22.

41.

Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

Piotrowski DW, Futatsugi K, Warmus JS, Orr ST, Freeman-Cook KD, Londregan AT, Wei L, Jennings SM, Herr M, Coffey SB, Jiao W, Storer G, Hepworth D, Wang J, Lavergne SY, Chin JE, Hadcock JR, Brenner MB, Wolford AC, Janssen AM, Roush NS, Buxton J, Hinchey T, Kalgutkar AS, Sharma R, Flynn DA.

ACS Med Chem Lett. 2012 Nov 9;4(1):63-8. doi: 10.1021/ml300277t. eCollection 2013 Jan 10.

42.

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y.

J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31.

PMID:
23234271
43.

From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.

Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5.

PMID:
23177788
44.

Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.

Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E, Kalgutkar AS.

Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20.

45.

Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.

Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16.

PMID:
23153798
46.

Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().

Rand AC, Leung SS, Eng H, Rotter CJ, Sharma R, Kalgutkar AS, Zhang Y, Varma MV, Farley KA, Khunte B, Limberakis C, Price DA, Liras S, Mathiowetz AM, Jacobson MP, Lokey RS.

Medchemcomm. 2012 Oct;3(10):1282-1289.

47.

Insights into the novel hydrolytic mechanism of a diethyl 2-phenyl-2-(2-arylacetoxy)methyl malonate ester-based microsomal triglyceride transfer protein (MTP) inhibitor.

Ryder T, Walker GS, Goosen TC, Ruggeri RB, Conn EL, Rocke BN, Lapham K, Steppan CM, Hepworth D, Kalgutkar AS.

Chem Res Toxicol. 2012 Oct 15;25(10):2138-52. doi: 10.1021/tx300243v. Epub 2012 Sep 27.

PMID:
22989032
48.

Drug discovery for a new generation of covalent drugs.

Kalgutkar AS, Dalvie DK.

Expert Opin Drug Discov. 2012 Jul;7(7):561-81. doi: 10.1517/17460441.2012.688744. Epub 2012 May 19. Review. Erratum in: Expert Opin Drug Discov. 2012 Sep;7(9):861.

PMID:
22607458
49.

Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.

Orr ST, Ripp SL, Ballard TE, Henderson JL, Scott DO, Obach RS, Sun H, Kalgutkar AS.

J Med Chem. 2012 Jun 14;55(11):4896-933. doi: 10.1021/jm300065h. Epub 2012 Mar 27. Review. No abstract available.

PMID:
22409598
50.

Immune-mediated agranulocytosis caused by the cocaine adulterant levamisole: a case for reactive metabolite(s) involvement.

Wolford A, McDonald TS, Eng H, Hansel S, Chen Y, Bauman J, Sharma R, Kalgutkar AS.

Drug Metab Dispos. 2012 Jun;40(6):1067-75. doi: 10.1124/dmd.112.045021. Epub 2012 Mar 5. Review.

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