B. Metcalf

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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

M. Bower, R. Wynn, Q. Wang, 2017, ACS medicinal chemistry letters.

Regiospecific 1,4 addition of a propargylic anion. A general synthon for 2-substituted propargylamines as potential catalytic irreversible enzyme inhibitors.

B. Metcalf, P. Casara, 1975 .

Catalytic inhibition of γ-aminobutyric acid-α-ketoglutarate transaminase of bacterial origin by 4-aminohex-5-ynoic acid, a substrate analog

B. Metcalf, M. Jung, 1975 .

THE EFFECT OF 4‐AMINO HEX‐5‐YNOIC ACID (γ‐ACETYLENIC GABA, γ‐ETHYNYL GABA) A CATALYTIC INHIBITOR OF GABA TRANSAMINASE, ON BRAIN GABA METABOLISM IN VIVO

A. Sjoerdsma, P. Schechter, B. Metcalf, 1977 .

γ‐VINYL GABA (4‐amino‐hex‐5‐enoic acid), A NEW SELECTIVE IRREVERSIBLE INHIBITOR OF GABA‐T: EFFECTS ON BRAIN GABA METABOLISM IN MICE 1

P. Schechter, B. Metcalf, P. Böhlen, 1977, Journal of neurochemistry.

Identification and Characterization of INCB 9471 , an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011 .

Identification and Characterization of INCB9471, an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011, Journal of Pharmacology and Experimental Therapeutics.

Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy

H. Koblish, M. Stubbs, Q. Wang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

P. Scherle, K. Vaddi, M. Covington, 2011, ACS medicinal chemistry letters.

GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half‐life in a murine model of sickle cell disease

S. Almo, Y. Patskovsky, K. Dufu, 2016, British journal of haematology.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin

C. Johnson, S. Almo, Lan Hua, 2017, ACS medicinal chemistry letters.

4-Amino-4,5-dihydrothiophene-2-carboxylic Acid.

J. Adams, B. Metcalf, Teng-Man Chen, 1986 .

4-Amino-4,5-dihydrothiophene-2-carboxylic acid

J. Adams, B. Metcalf, Teng-Man Chen, 1985 .

Phosphinic acid inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme a reductase

R. Mayer, T. Meek, G. Dreyer, 1991 .

Inhibition of rat liver steroid 5 alpha-reductase by 3-androstene-3-carboxylic acids: mechanism of enzyme-inhibitor interaction.

D. Holt, B. Metcalf, J. R. Heys, 1990, Biochemistry.

Parsaclisib Is a Next-Generation PI3Kδ Inhibitor With Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy a

Kathy, Qianqian Wang, H. Koblish, 2020 .

Purification and properties of the catalytic domain of human 3-hydroxy-3-methylglutaryl-CoA reductase expressed in Escherichia coli.

C. Debouck, R. Mayer, B. Metcalf, 1988, Archives of biochemistry and biophysics.

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

J. Fridman, Jun Li, X. Wen, 2010, The Journal of Immunology.

Selective Inhibition of JAK 1 and JAK 2 Is Efficacious in Rodent Models of Arthritis : Preclinical Characterization of INCB 028050

J. Fridman, Jun Li, X. Wen, 2010 .

Preclinical Characterization of INCB 028050 Efficacious in Rodent Models of Arthritis : Selective Inhibition of JAK 1 and JAK 2 Is

J. Fridman, Jun Li, X. Wen, 2010 .

Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.

J. Fridman, P. Scherle, C. Neilan, 2011, The Journal of investigative dermatology.

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

H. Koblish, P. Scherle, T. Maduskuie, 2019, ACS medicinal chemistry letters.

Discovery of a novel 2-spiro-proline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

R. Wynn, P. Scherle, Yanlong Li, 2022, Bioorganic & medicinal chemistry letters.

The synthesis of α,α-difluoroaldehydes and ketones via claisen rearrangements

B. Metcalf, E. Jarvi, J. P. Burkhart, 1985 .

The synthesis of a 3-diazobicyclo[2.2.1]Heptan-2-one inhibitor of thromboxane a2 synthetase

J. Adams, B. Metcalf, 1984 .

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

P. Scherle, K. Vaddi, Joseph Glenn, 2010, ACS medicinal chemistry letters.

3-Phosphinic acid and 3-phosphonic acid steroids as inhibitors of steroid 5α-reductase: Species comparison and mechanistic studies

L. Rozamus, D. Holt, B. Metcalf, 1991 .

Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction.

S. Shepard, J. Rodgers, B. Metcalf, 2009, Organic Letters.

Steroidal acetylenes: Mechanism-based inactivators of lanosterol 14α-demethylase

J. Adams, T. Gallagher, T. Tomaszek, 1991 .

A novel, convenient assay of lanosterol 14α-demethylase

J. Adams, T. Tomaszek, B. Metcalf, 1989 .

Inhibitors of steroid 5 alpha-reductase in benign prostatic hyperplasia, male pattern baldness and acne.

D. Holt, B. Metcalf, M. Levy, 1989, Trends in pharmacological sciences.

Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.

D. J. Rogier, Wei Huang, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

4-amino-hex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyric-acid aminotransferase in mammalian brain.

B. Metcalf, P. Casara, M. Jung, 1977, European journal of biochemistry.

Inhibitors of GABA metabolism.

B. Metcalf, 1979, Biochemical Pharmacology.

The search for antimicrobial agents effective against bacteria resistant to multiple antibiotics

G Poste, G. Poste, I. Chopra, 1997, Antimicrobial agents and chemotherapy.

Inhibition of HIV-1 protease in infected T-lymphocytes by synthetic peptide analogues

Brian W. Metcalf, Michael L. Moore, C. Debouck, 1990, Nature.

Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1′-P2′ amide bond isostere

R. Lum, M. Darcy, D. Lambert, 1994 .

Cellular adhesion : molecular definition to therapeutic potential

G. Poste, B. Metcalf, B. Dalton, 1994 .

Stereospecific synthesis of (2R,5R)-hept-6-yne-2,5-diamine: a potent and selective enzyme-activated irreversible inhibitor of ornithine decarboxylase (ODC)

C. Darwin, B. Metcalf, P. Casara, 1985 .

Letter: A stereospecific total synthesis of racemic 11alpha-hydroxyprogesterone via a biomimetic polyene cyclization.

B. Metcalf, S. Escher, W. S. Johnson, 1976, Journal of the American Chemical Society.

Cleavage of tert-butyldimethylsilyl ethers by tetrafluoroborate salts

B. Metcalf, K. Jund, J. P. Burkhart, 1980 .

The synthesis of α,α-difluoroaldehydes and ketones via claisen rearrangements

B. Metcalf, E. Jarvi, J. P. Burkhart, 1985 .

Asymmetric Synthesis of Conformationally Constrained trans-2,3-Piperidinedicarboxylic Acid Derivatives

B. Metcalf, W. Yao, Meizhong Xu, 2007 .

Synthesis of 11β-hydroxy-18-ethynylprogesterone: an inhibitor of aldosterone biosynthesis

B. Metcalf, J. O. Johnston, G. W. Holbert, 1985 .

The time-dependent inactivation of aromatase by 17beta-hydroxy-10-methylthioestra-1,4-dien-3-one.

B. Metcalf, J. O. Johnston, G. Flynn, 1981, Biochemical and biophysical research communications.

Synthesis of α-ethynylhistamine, an inactivator of histidine decarboxylase

B. Metcalf, G. W. Holbert, 1984 .

Synthetic access to α-substituted prop-2-ynylamines and α-acetylenic amino acids via the t-butyl N-trimethylsilylprop-2-ynylcarbamate dianion

B. Metcalf, P. Casara, 1979 .

Trimethylsilylacetylene-N-carboethoxy glycinate dianion - a general synthon for α-acetylenic α-amino acids.

B. Metcalf, P. Casara, 1978 .

The synthesis of fluorinated aminophosphonic acid inhibitors of alanine racemase

D. Beight, B. Metcalf, E. Bohme, 1985 .

Inhibition of human immunodeficiency virus 1 protease in vitro: rational design of substrate analogue inhibitors.

C. Debouck, J. Strickler, T. Meek, 1989, Proceedings of the National Academy of Sciences of the United States of America.

Catalytic irreversible inhibition of mammalian ornithine decarboxylase (E.C.4.1.1.17) by substrate and product analogs

B. Metcalf, C. Danzin, P. Casara, 1978 .

Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.

Karl Blom, Michael Bower, James Pruitt, 2005, Journal of medicinal chemistry.

Stereospecific irreversible inhibition of mammalian (S)-ornithine decarboxylase by (R)-(–)-hex-5-yne-1,4-diamine

B. Metcalf, C. Danzin, P. Casara, 1982 .

Inhibition of 3(17)beta-hydroxysteroid dehydrogenase from Pseudomonas testosteroni by steroidal A ring fused pyrazoles.

D. Holt, B. Metcalf, M. Brandt, 1987, Biochemistry.

8 – COFACTOR DEPENDENCY IN THE INHIBITION OF STEROID 5 ALPHA-REDUCTASE

D. Holt, B. Metcalf, M. Levy, 1989 .

Substrate-induced inactivation of aromatase by allenic and acetylenic steroids

B. Metcalf, J. O. Johnston, J. P. Burkhart, 1981 .

Cleavage of tert-butyldimethylsilyl ethers by tetrafluoroborate salts

B. Metcalf, K. Jund, J. P. Burkhart, 1980 .

Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.

M. Bower, R. Wynn, Wenyu Zhu, 2006, Journal of medicinal chemistry.

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.

Qian Wang, Michael Bower, Richard Wynn, 2009, Journal of medicinal chemistry.

Chapter 26. Recent Progress in the Design of Suicide Enzyme Inhibitors

B. Metcalf, 1981 .

Inhibition of testosterone 5 alpha-reductase by a proposed enzyme-activated, active site-directed inhibitor.

A. Sjoerdsma, B. Metcalf, T. R. Blohm, 1980, Biochemical and biophysical research communications.

Correction: Slow binding inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A reductase [Erratum to document cited in CA112(23):212921g]

J. D. Elliott, C. E. Peishoff, R. Mayer, 1990 .

Target Enzyme-Activated Irreversible Enzyme Inhibitors

B. Metcalf, 1981 .

Biochemical consequences of reactions catalyzed by GAD and GABA-T

B. Metcalf, M. Jung, B. Lippert, 1980, Brain Research Bulletin.

Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

P. Scherle, Yanlong Li, M. Covington, 2009, Bioorganic & medicinal chemistry letters.

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

D. J. Rogier, P. Scherle, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Peptide substrates and inhibitors of the HIV-1 protease.

C. Debouck, J. Strickler, T. Meek, 1989, Biochemical and biophysical research communications.

Time-dependent inhibition of aromatase in trophoblastic tumor cells in tissue culture.

B. Metcalf, J. O. Johnston, C. Wright, 1984, Journal of steroid biochemistry.

[31] Synthesis of irreversible inhibitors of polyamine biosynthesis

B. Metcalf, P. Casara, P. Bey, 1983 .

α,α-Difluoroketone inhibitors of HMG CoA reductase

G. Dreyer, B. Metcalf, 1988 .

Substrate-induced inactivation of aromatase by allenic and acetylenic steroids

B. Metcalf, J. O. Johnston, J. P. Burkhart, 1981 .

(2R,5R)-6-heptyne-2,5-diamine, an extremely potent inhibitor of mammalian ornithine decarboxylase.

B. Metcalf, C. Danzin, P. Casara, 1983, Biochemical and biophysical research communications.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Lixin Shao, Michael Xia, D. J. Rogier, 2011, ACS medicinal chemistry letters.

Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells

R. Wynn, P. Scherle, Phillip C. C. Liu, 2006, Cancer biology & therapy.

Synergistic drug interactions of an HIV-1 protease inhibitor with AZT in different in vitro models of HIV-1 infection.

D. Lambert, G. Dreyer, B. Metcalf, 1993, Antiviral research.

Human immunodeficiency virus type 1 protease inhibitors irreversibly block infectivity of purified virions from chronically infected cells

D. Lambert, D. Bolognesi, T. Meek, 1992, Antimicrobial Agents and Chemotherapy.

Studies on the mechanism of steroid 5α-reductase inhibition by 3-carboxy A-ring aryl steroids

D. Holt, B. Metcalf, M. Brandt, 1990, The Journal of Steroid Biochemistry and Molecular Biology.

Interaction between rat prostatic steroid 5α-reductase and 3-carboxy-17β-substituted steroids : novel mechanism of enzyme inhibition

D. Holt, B. Metcalf, M. Brandt, 1989 .

Potent inhibition of human steroid 5α-reductase (EC 1.3.1.30) by 3-androstene-3-carboxylic acids

D. Holt, B. Metcalf, H. Oh, 1989 .

Steroidal A ring aryl carboxylic acids: a new class of steroid 5 alpha-reductase inhibitors.

D. Holt, B. Metcalf, H. Oh, 1990, Journal of medicinal chemistry.

Steroidal A Ring Aryl Carboxylic Acids: A New Class of Steroid 5α-Reductase Inhibitors.

D. Holt, B. Metcalf, H. Oh, 1990 .

The synthesis of novel bridged A ring steroids

J. D. Elliott, D. Holt, H. Lan-Hargest, 1987 .

Structures of full-length plasma kallikrein bound to highly specific inhibitors describe a new mode of targeted inhibition.

H. Sham, J. Partridge, B. Metcalf, 2019, Journal of structural biology.

Human immunodeficiency virus protease: A target for aids therapy

Brian W. Metcalf, C. Debouck, B. Metcalf, 1990 .

Molecular basis for the irreversible inhibition of 4-aminobutyric acid:2-oxoglutarate and L-ornithine:2-oxoacid aminotransferases by 3-amino-1,5-cyclohexadienyl carboxylic acid (isogabaculline).

B. Metcalf, M. Jung, 1979, Molecular pharmacology.

Enzyme-activated irreversible inhibition of rat and mouse brain 4-aminobutyric acid-alpha-ketoglutarate transaminase by 5-fluoro-4-oxo-pentanoic acid.

B. Metcalf, B. Lippert, R. Resvick, 1982, Biochemical and biophysical research communications.

The impact of genomics on drug discovery.

C. Debouck, B. Metcalf, C Debouck, 2000, Annual review of pharmacology and toxicology.

The effect of 4-amino hex-5-ynoic acid (gamma-acetylenic GABA, gammma-ethynyl GABA) a catalytic inhibitor of GABA transaminase, on brain GABA metabolism in vivo.

A. Sjoerdsma, P. Schechter, B. Metcalf, 1977, Journal of neurochemistry.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

R. Wynn, J. Fridman, P. Scherle, 2009, Bioorganic & Medicinal Chemistry Letters.

Human immunodeficiency virus 1 protease expressed in Escherichia coli behaves as a dimeric aspartic protease.

C. Debouck, J. Strickler, M. Rosenberg, 1989, Proceedings of the National Academy of Sciences of the United States of America.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5α-reductase isoform 2

D. Holt, D. Bergsma, B. Metcalf, 1994, The Journal of Steroid Biochemistry and Molecular Biology.

Human immunodeficiency virus protease expressed in Escherichia coli exhibits autoprocessing and specific maturation of the gag precursor.

C. Debouck, J. Strickler, M. Rosenberg, 1987, Proceedings of the National Academy of Sciences of the United States of America.

New approaches to the control of infections caused by antibiotic-resistant bacteria. An industry perspective.

G. Poste, I. Chopra, B. Metcalf, 1996, JAMA.

Proteolysis of an active site peptide of lactate dehydrogenase by human immunodeficiency virus type 1 protease.

C. Debouck, I. Brooks, J. Strickler, 1992, Biochemistry.

Biochemical and endocrine properties of a mechanism-based inhibitor of aromatase.

B. Metcalf, J. O. Johnston, C. Wright, 1984, Endocrinology.

Decrease of polyamine levels in rat tissues by 5-hexyne-1,4-diamine, an enzyme-activated irreversible inhibitor of ornithine decarboxylase.

B. Metcalf, C. Danzin, P. Casara, 1979, Biochemical pharmacology.

Inhibition of steroid 5 alpha-reductase by unsaturated 3-carboxysteroids.

D. Holt, H. Lan-Hargest, B. Metcalf, 1990, Journal of medicinal chemistry.

The photochemical rearrangement of a steroidal dienol triflate

J. D. Elliott, H. Lan-Hargest, B. Metcalf, 1987 .

Slow binding inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

J. D. Elliott, C. E. Peishoff, R. Mayer, 1990, Biochemistry.

GBT440 Demonstrates High Specificity for Red Blood Cells in Nonclinical Species

B. Metcalf, A. Hutchaleelaha, D. Oksenberg, 2015 .

Synthesis of 3-keto-4-diazo-5-α-dihydrosteroids as potential irreversible inhibitors of steroid 5-α-reductase

B. Metcalf, K. Jund, J. P. Burkhart, 1980 .

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

M. Bower, R. Wynn, J. Fridman, 2007, Journal of medicinal chemistry.

9 – Aromatase: A Target Enzyme in Breast Cancer

B. Metcalf, J. O. Johnston, W. MetcalfBrian, 1984 .

Synthesis of β,γ-unsaturated amino acids as potential catalytic irreversible enzyme inhibitors

B. Metcalf, K. Jund, 1977 .

alpha-Ethynyl and alpha-vinyl analogues of ornithine as enzyme-activated inhibitors of mammalian ornithine decarboxylase.

B. Metcalf, C. Danzin, P. Casara, 1981, Journal of medicinal chemistry.

Hydroxyethylene isostere inhibitors of human immunodeficiency virus-1 protease: structure-activity analysis using enzyme kinetics, X-ray crystallography, and infected T-cell assays.

A M Hassell, M. Minnich, D. Lambert, 1992, Biochemistry.

The chronically infected cell as a target for the treatment of HIV infection and AIDS.

D. Lambert, B. Metcalf, S. Petteway, 1991, Trends in pharmacological sciences.

Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.

D. J. Rogier, A. Bahinski, P. Scherle, 2011, Bioorganic & medicinal chemistry letters.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

An orally bioavailable HIV-1 protease inhibitor containing an imidazole-derived peptide bond replacement: crystallographic and pharmacokinetic analysis.

R. DesJarlais, Baoguang Zhao, K. Murthy, 1994, Biochemistry.

Mechanism of the stereospectific irreversible inhibition of bacterial glutamic acid decarboxylase by (R)-(--)-4-aminohex-5-ynoic acid, an analogue of 4-aminobutyric acid.

B. Metcalf, P. Casara, M. Jung, 1978, Biochemistry.

Effect of 5-hexyne-1,4-diamine on brain 4-aminobutyric acid metabolism in rats and mice.

N. Seiler, B. Metcalf, C. Danzin, 1979, Biochemical Pharmacology.

Cellular adhesion : molecular definition to therapeutic potential

G. Poste, B. Metcalf, B. Dalton, 1994 .

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.