Martin H. Johansson

Tu1741 PRECLINICAL DEVELOPMENT OF AQ312, A POTENT AND SELECTIVE SMALL MOLECULE ARYL HYDROCARBON AGONIST, FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE.

Martin H. Johansson, Wayne L. Russell, Malin Hultqvist, Johan Lund

Su1280 CLINICAL DEVELOPMENT OF AQ280, A POTENT AND HIGHLY SELECTIVE JAK1 INHIBITOR, FOR THE TREATMENT OF EOSINOPHILIC ESOPHAGITIS

Anneli Tinnerholm, Martin H. Johansson, Malin Hultqvist, Fredrik Lindgren et autres

Preclinical Characterization of 3β-(N-Acetyl l -cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer

Zilma Escobar, Anders Bjartell, Giacomo Canesin, Susan Evans‐Axelsson et autres

The transcription factor STAT3 is a potential target for the treatment of castration-resistant prostate cancer. Galiellalactone (1), a direct inhibitor of STAT3, prevents the transcription of STAT3 regulated genes. In this study we characterized 6 (GPA512, Johansson , M. ; Sterner , …

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Reduction in PD-L1 expression by STAT3 inhibition with GPA500 in enzalutamide-resistant prosate cancer.

Jennifer L. Bishop, Daksh Thaper, Sepideh Vaheid, Martin H. Johansson et autres

e16075 Background: Treatment benefits of the anti-androgen Enzalutamide (ENZ) in patients with castration-resistant prostate cancer (CRPC) are limited, underscoring the need for alternative therapies. Mechanisms of resistance to androgen targeted therapies like ENZ are varied, but include hyperactivation of oncogenic signaling pathways, …

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Targeting STAT3 in castration-resistant prostate cancer: Galiellalactone as a direct inhibitor of STAT3 in prostate cancer cells.

Rebecka Hellsten, Nicholas Don‐Doncow, Zilma Escobar, Martin H. Johansson et autres

e16065 Background: The transcription factor STAT3 is constitutively active in castration-resistant prostate cancer (CRPC) and constitutes a promising therapeutic target. The reactive fungal metabolite galiellalactone (GL), a STAT3-signaling inhibitor, inhibits the growth, both in vitro and in vivo, of prostate cancer cells …

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Preclinical characterization of GPA512: A prodrug of a direct STAT3 inhibitor for the treatment of prostate cancer.

Martin H. Johansson, Rebecka Hellsten, Giacomo Canesin, Susan Evans‐Axelsson et autres

e22186 Background: The transcription factor STAT3 is a promising target for the treatment of castration-resistant prostate cancer (CRPC) as STAT3 is implicated in drug resistance, the progression of androgen independent growth, metastatic spread, immune-avoidance and tumor growth. Galiellalactone (GL) is a direct …

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Reversible Michael Additions: Covalent Inhibitors and Prodrugs

Martin H. Johansson

Reversible Michael Additions: Covalent Inhibitors and Prodrugs

Martin H. Johansson

Covalent inhibition is an efficient molecular mechanism for inhibiting enzymes or modulating the function of proteins and is found in the action of many drugs and biologically active natural products. However, it is has been less appreciated that the formation of covalent …

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Synthesis of novel tetrahydroisoquinoline bronchodilators

María F. Dalence-Guzmán, Jörgen Toftered, Viveca T. Oltner, David Wensbo et autres

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The Tensin Family Of Putative Metastasis Suppressor Proteins Are Down-Regulated In Human Kidney Cancer

Danuta Martuszewska, Börje Ljungberg, Martin H. Johansson, Cecilia Oslakovic et autres

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Synthesis of 3‐Aryl‐5‐methyl 4‐Substituted [1,2,4]Triazoles.

Johan Lindstroem, Martin H. Johansson

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

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Synthesis of 3‐Aryl‐5‐methyl 4‐Substituted [1,2,4]Triazoles

Johan Lindström, Martin H. Johansson

Treatment of N‐substituted acetamides with oxalyl chloride generates imidoyl chlorides, which react readily with aryl hydrazides. Following cyclization, triazoles can easily be obtained in moderate to good yields. 5‐Methyl triazoles can be further functionalized through α‐lithiation and subsequent reaction with an electrophile.

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