Publications & Patents

PUBLICATIONS

 

Alchanaty, I. Teicher, C., Cohen, G., Shemesh, V., Barr, H., Nakache, P., Ben-Avraham, D., Idelevich, A.,Angel, I., Livnah, N.,Tuvia, S.,Reiss, Y., Teiglicht, D and Erez, O.“The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex – a potentially new drug target”

PLoS One, 2009; 4(12), e8104.

Dvir, E, Friedman, J.E., Lee, J-Y., Koh, J-H., Younis, F., Raz, S., Shapiro, I, Hoffman, A., Dahan, A., Rosenberg, G.., Angel, I., Kozak, A.,  Duvdevani, R.

“A novel phospholipid derivative of indomethacin, DP-155, shows superior safety and similar efficacy in reducing brain amyloid β in an Alzheimer’s disease model”

J. Pharmacol. Exper. Therapeu., 2006, 318: 1248-1256.

Lee, J-Y., Kim, J-H.,  Friedman, J.E.,  Angel, I., Kozak, A., Koh, J-Y.

“The lipophilic metal chelator DP-109 reduces amyloid pathology in the brains of human b-amyloid precursor protein transgenic mice”.

Neurobiology of Aging. 2004, 25(10):1315-21.

Kolusheva, S., Friedman, J., Angel, I. And Jelinek, R.

“Membrane interactions and metal-ion effects on bilayar permeation of the lipophilic ion modulator DP-109”

Biochemistry, 2005, 44(36):12077-85

Rosenberg, G, Angel, I., Kozak, A,

“Clinical pharmacology of DP-b99 in healthy volunteers: First administration to humans”

Br. J. Pharmacol. 2005, 60 (1), 7-16.

Angel, I., “Loosing Our Minds: What the future holds for the treatment of Neurodegenerative Disorders”.

European Biopharmaceutical Review. June, 2003

Angel, I, Bar A and Haring, R.

“Bioactive lipids and their receptors”.

Curr Opin Drug Discov Devel. 2002, 5:728-740.

Angel, I., Bar, A., Horowitz T., Taler, G., Krakovsky M., Resnitsky D.,Rosenberg, G.,Striam, S., Friedman, J.E. and Kozak, A.

“Metal ion chelation in Neurodegenerative disorders”.

Drug Devel. Res. 2002:56:300-309.

Polyak, M., Ayalon, O., Vinnikova, M., Angel, I and Kozak, A

 “Controlled modulation of the blood-brain barrier and blood–tumor barrier using novel lipid mimetic compounds”.

 In: Blood-Brain Barrier. Edited by Kobiler et al., Kluwer Academic/Plenum Publishers,New York, 2001

Krakovsky, M., Polyak, M., Angel,I. and Kozak, A.

“DP-b99, A Novel Membrane Targeted Compound Active against Global and Focal Cerebral Ischemia”

In: Gjedde SH, Kundsen GM, Paulson OB, editors. Physiological Imaging of the Brain with PET.New York: Academic Press, p347-352, 2001.

Angel, I.,  Krakovsky, M.,  Shemesh, T.,  Beit-Yannai, E., Friedman, J. and Kozak, A.

“DP-b99 A Neuroprotective Agent for Cerebral Ischemia”.

Bio Tech International. 2001:Vol 12, no.6 p20-22.

 

Angel, I.

“Ischemic Injury: Novel Targets and Therapeutics”

Idrugs. 2001: 4(4):380-382, Pharma Press Ltd.

Angel, I., Krakovsky, M., Shemesh, T. Beit-Yanai, E., Friedman, J.E., Kozak, A.

“DP-b99 A neuroprotective agent for cerebral ischemia.”

Bio Tech International. 2000;12(6):20-22

Angel, I. and Horowitz T.

“Bipolar disorders and valproic acid”.

Curr Opin CPNS Investigational Drugs. 1999:1(4)466-469.

Goldhill, J. and Angel, I.

“Mechanism of tachykinin NK3 receptor-mediated colonic ion transport in the guinea pig.”
Eur J Pharmacol. 1998 Dec 18;363(2-3):161-8

Martin, D., Lluel, P. Guillot, E., Coste, A Jammes, D and Angel, I.

“Comparative alpha1-aderenoceptor subtype selectivity and functional uroselectivity alpha1-aderenoceptor antagonists”

J. Pharmacol. And Exp. Ther., 1998:63 (3): 169-76.

 

Martin, DJ., Lluel, P., Pouyet, T., Rauch-Desanti, C. and Angel, I.

“Relationship between the effects of alfuzosin on rat urethral and blood pressures and its tissue concentrations”.
Life Sci. 1998;63(3):169-76.

Martin, DJ., Angel, I. and Arbilla, S.

“Functional uroselectivity”.

Eur Urol. 1998;33 Suppl 2:12-8.

Goldhill, J., Porquet, MF. and Angel, I.

“The response of rat colonic mucosa to 5-hydroxytryptamine in health and following restraint stress”.

Eur J Pharmacol. 1998 Jul 24;353(2-3):289-96.

Guillot, E., Coste, A., Eon, MT. and Angel, I.

“Mechanisms of the hypoglycemic effects of the alpha2-adrenoceptor antagonists SL84.0418 and deriglidole”.

Life Sci. 1998;62(9):839-52.

Goldhill, J, Pichat, P, Roome, N, Angel, I and Arbilla, S.

“Effect of mizolastine on visceral sensory afferent sensitivity and inflammation during experimental colitis”.

Arzneimittelforschung. 1998: Feb;48(2):179-84.

Deplanne, V., Palea, S. and Angel, I.

“The adrenergic, cholinergic and NANC nerve-mediated contractions of the female rabbit bladder neck and proximal, medial and distal urethra”.

Br J Pharmacol. 1998: Apr;123(8):1517-24

Buzelin, JM., Delauche Cavallier, MC., Martin, D. and Angel, I.

“Clinical uroselectivity: evidence from patients treated with slow release alfuzosin for symptomatic benign prostatic obstruction”.

Br J Urol. 1998 Apr;81(4):655-6.

Pichat, P., Angel, .I. and Arbilla, S.

“Anti-inflammatory properties of mizolastine after oral administration on arachidonic acid-induced cutaneous reaction in the rat”.

Arzneimittelforschung. 1998 Feb;48(2):173-8.

Martin, DJ., Lluel, P., Guillot, E., Coste, A., Jammes, D. and Angel, I.

“Comparative alpha-1 adrenoceptor subtype selectivity and functional uroselectivity of alpha-1 adrenoceptor antagonists”.

J Pharmacol Exp Ther. 1997 Jul;282(1):228-35.

Goldhill, J., Porquet, MF. and Angel, I.

“Post-synaptic 5-HT4 receptor modulation of tachykinergic excitation of rat oesophageal tunica muscularis mucosae”.

Eur J Pharmacol. 1997 Apr 4;323(2-3):229-33.

Van Der Graaf, P., Deplanne, V., Duquenne, C. and Angel I.

“Analysis of alpha1-aderenoceptors in rabbit lower urinary tract and mesenteric artery”

Eur. J. Pharmacol.,1997:327 (1): 25-32.

Palea,. S. and Angel, I

“The effect of in vivo oestrogen pretreatment on the contractile response of the rat isolate detrusor muscle and urethra”

Life Sci., 1997:61 (1): PL21-26.

Barras, M., Van Der Graaf P. and Angel, I.

“Characterization of the 5-hydroxytryptamine receptor potentiating neurotransmission in rabbit bladder”

Eur. J. Pharamacol., 1996:318/3-3: 425-428.

Angel, I., Burcelin, R., Proteau, M., Girard, J. and  Langer, SZ.

“Normalization of insulin secretion by a selective alpha-2 adrenoceptor antagonist restores GLUT-4 glucose transporter expression in adipose tissue of type-II diabetic rats.”

Endocrinology 1996:137:2022-2027.

Guillot, E., Coste, A. and Angel, I.

“Involvement of capsaicin-sensitive nerves in the regulation of glucose tolerance in diabetic rats”

Life Sci.,1996:59:969-977,

Martin, D., Jammes, D. and Angel, I.

“Effects of Alfuzosin on urethral and blood pressures in conscious male rats”.

Life Sci. 1995:57: PL 387-391.

Guillot, E., Morand, R., Boulcy, C., Eon, MT. and Angel, I.

“Involvement of  a2-adrennoceptors in metabolic and hormonal responses to a mixed mea in beagle dogs”

Am. J. Physiol. , 1995: 269:E991-E995.

Angel, I, Le Rouzi, M., Pimoule, C., Graham, D. and Arbilla, S.

“[3H]cirazoline as a tool for the characterization of imidazoline sites”.
Acad Sci. 1995 Jul 12;763:112-24.

Le Rouzi, M., Angel, I., Schoemaker H., Allen, J., Arbilla, S. and  Langer, SZ.

“Binding of [3H]cirazoline to an imidazoline site in rat brain and kidney membranes”.
Eur J Pharmacol. 1995 May 24;278(3):261-4.

Martin, D., Jammes, D. and Angel, I.

“Effects of alfuzosin on urethral and blood pressures in conscious male rats”.
Life Sci. 1995;57(25):PL387-91.

Guillot, E., Coste, A. and Angel, I.
”Alpha 2-adrenoceptors and the regulation of glucose, insulin and amylin levels in diabetic rats”.

Life Sci. 1995;57(23):2081-90.

Jonas, JC., Garcia-Barrado, M.J, Angel, I. andHenquin, JC.

“The imidazoline SL 84.0418 shows stereoselectivity in blocking alpha 2-adrenoceptors but not ATP-sensitive K+ channels in pancreatic B-cells”.
Eur J Pharmacol. 1994 Oct 13; 264(1):81-4.

Jonas, JC., Plant, TD., Angel, I, Langer, SZ and Henquin, JC.

“In vitro stimulation of insulin release by SL 84.0418, a new alpha 2-adrenoceptor antagonist”.
Eur J Pharmacol. 1994 Mar 11;254(1-2):27-33.

Angel I., Schoemaker, H., Prouteau, M., Garreau, M. and Langer, SZ.

“Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties”.
Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.

Angel, I., Grosset, A., Perrault, G., Schoemaker, H. and Langer, S.Z.

“In vivo pharmacological profile of SL 84.0418, a new selective, peripherally active alpha 2-adrenoceptor antagonist”.
Eur J Pharmacol. 1993 Apr 6;234(2-3):137-45.

Lorrain, J., Angel, I., Eon, MT., Oblin, A. and Langer, SZ.

“Inhibition of insulin release induced by galanin in the dog is not exclusively mediated by activation of ATP-sensitive K+ channels”.
Pharmacology. 1993;46(2):109-14.

Angel, I., Schoemaker, H., Arbilla, S., Galzin, AM., Berry, C., Niddam, R., Pimoule, C., Sevrin, M., Wick, A. and Langer, SZ.

“SL 84.0418: a novel, potent and selective alpha-2 adrenoceptor antagonist: in vitro pharmacological profile”.

J Pharmacol Exp Ther. 1992 Dec;263(3):1327-33.

Langer, SZ., Graham, D., Arbilla, S., Schoemaker, H. and Angel, I.

“The serotonin re-uptake transporter as a target for antidepressant action”.
Clin Neuropharmacol. 1992;15 Suppl 1 Pt A:436A-437A.

Lorrain, J. Angel I.,  Duval, N., Eon, M.T., Oblin, A. and Langer, S.Z.

“Adrenergic and nonadrenergic cotransmitters inhibit insulin secretion during sympathetic stimulation in dogs”.
Am J Physiol. 1992 Jul;263(1 Pt 1):E72-8.

Angel, I., Hauger, RL., Giblin, BA. and Paul, SM.

“Regulation of the anorectic drug recognition site during glucoprivic feeding”.
Brain Res Bull. 1992 Feb;28(2):201-7.

Langer, SZ., Angel,  I., and Schoemaker, H.

“Physiological and Pharmalogical relevance of presynaptic receptors in neurotransmission”.
in “Advances in the Biosciences”  Vol 82, pp 1-5, 1991

Schoemaker, H., Grosset, A., Angel., and Langer, SZ.

“Antagonist activity of SL 84.0418 and idazoxan at pre and postsynaptic alpha-adrenoceptors”

in “Advances in the BiosciencesVol. 82, pp. 27-28, 1991

Duval, N., Angel, I., Oblin, A., Eon, MT. and Langer SZ.

“Effect of alpha-2 adrenoceptor antagonists on norepinephrine release and inhibition of insulin secretion during pancreatic nerve stimulation.  Interaction at pre-anpostnyaptic sites”.

In “Advances in the Biosciences” Vol. 82, pp. 25-26, 1991

Langer, SZ. and Angel, I.

“Pre- and postsynaptic alpha-2 adrenoceptors as target for drug discovery” .J Neural Transm Suppl. 1991;34:171-7.

Angel, I. and Bidet, S.

“The binding site for [3H]glibenclamide in the rat cerebral cortex does not recognize K-channel agonists or antagonists other than sulphonylureas” .

Fundam Clin Pharmacol. 1991;5(2):107-15.

Angel, I.

“Central receptors and recognition sites mediating the effects of monoamines and anorectic drugs on feeding behavior” .

Clin Neuropharmacol. 1990 Oct;13(5):361-91.

Niddam, R., Angel, I., Bidet, S. and Langer, SZ.

”Pharmacological characterization of alpha-2 adrenergic receptor subtype involved in the release of insulin from isolated rat pancreatic islets” .

J Pharmacol Exp Ther. 1990 Sep;254(3):883-7

Angel, I., Niddam, R. and Langer, SZ.

“Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia” .

J Pharmacol Exp Ther. 1990 Sep;254(3):877-82.

 

 

Angel, I., Janowsky,A. and Paul, SM.

“The effects of serotonergic and dopaminergic lesions on sodium-sensitive [3H]mazindol binding in rat hypothalamus and corpus striatum” .

Brain Res. 1989 Dec 4;503(2):339-41.

 

 

Angel, I. and Taranger, MA.

”Coupling between hypothalamic alpha 2-adrenoceptors and [3H]mazindol binding site in response to several hyperglycaemic stimuli in mice”.

Brain Res. 1989 Jun 26;490(2):367-72.

Angel, I.

“The use of microtiter plates for the simple and sensitive determination of insulin by an ELISA method”.

Experientia. 1988 Oct 15;44(10):877-9.

Angel, I. and Langer, SZ.

 “Adrenergic-induced hyperglycemia in anaesthetized rats: involvement of peripheral alpha 2-adrenoceptors”.

Eur J Pharmacol. 1988 Sep 13;154(2):191-6.

Angel, I., Bidet, S. and Langer, SZ.

 “Pharmacological characterization of the hyperglycemia induced by alpha-2 adrenoceptor agonists” .

J Pharmacol Exp Ther. 1988 Sep;246(3):1098-103. PMID: 2901484

 

Angel, I., Taranger, MA., Claustre, Y., Scatton, B. and Langer, SZ.

“Anorectic activities of serotonin uptake inhibitors: correlation with their potencies at inhibiting serotonin uptake in vivo and 3H-mazindol binding in vitro”.

Life Sci. 1988;43(8):651-8.

Janowsky A, Vocci, F., Berger, P., Angel, I., Zelnik, N., Kleinman, JE., Skolnick P. and Paul, SM.

 “[3H]GBR-12935 binding to the dopamine transporter is decreased in the caudate nucleus in Parkinson’s disease” .

J Neurochem. 1987 Aug;49(2):617-21.

Angel, I., Stivers, JA., Paul, SM. andCrawley, JN.

 “Site of action of anorectic drugs: glucoprivic- versus food deprivation-induced feeding “.

Pharmacol Biochem Behav. 1987 Jun;27(2):291-7.

Angel, I.,Luu.,MD and Paul, SM.

 “Characterization of [3H]mazindol binding in rat brain: sodium-sensitive binding correlates with the anorectic potencies of phenylethylamines” .

J Neurochem. 1987 Feb;48(2):491-7.

Hauger, R., Hulihan-Giblin, B ,Janowsky A, Angel, I,. Berger, P., Luu, M.D., Schweri, M.M., Skolnick P., Paul, SM.and Vocci, F.

“Central recognition site for psychomotor stimulants: Methylphenidate and amphetamine.”

In: Receptor binding in drug research. Robert A. O’Brian, Ed., 1986, CRC Press.

Angel, I., Kiss, A., Stivers, JA., Skirboll, L.,Crawley, JN. and Paul, SM.

”Regulation of [3H]mazindol binding to subhypothalamic areas: involvement in glucoprivic feeding” .

Brain Res Bull. 1986 Dec;17(6):873-7.

Zelnik, N., Angel, I., Paul, SM. and Kleinman, JE.

“Decreased density of human striatal dopamine uptake sites with age”.

Eur J Pharmacol. 1986 Jul 15;126(1-2):175-6.

Hauger, R., Hulihan-Giblin, B., Angel, I.,Luu,MD., Janowsky, A., Skolnick, P. and Paul, SM.

“Glucose regulates [3H](+)-amphetamine binding and Na+K+ ATPase activity in the hypothalamus: a proposed mechanism for the glucostatic control of feeding and satiety”.

Brain Res Bull. 1986 Feb;16(2):281-8.

Angel, I., Hauger, RL.,Luu,MD., Giblin, B., Skolnick, P. and Paul, SM.

“Glucostatic regulation of (+)-[3H]amphetamine binding in the hypothalamus: correlation with Na+,K+-ATPase activit”.

Proc Natl Acad Sci U S A. 1985 Sep;82(18):6320-4

Angel, I. and Paul, SM.

 “Demonstration of specific binding sites for [3H]mazindol in rat hypothalamus: correlation with the anorectic properties of phenylethylamines”.

Eur J Pharmacol. 1985 Jul 11;113(1):133-4.

Angel, I.,Goldman,ME., Skolnick, P., Pisano, JJ. and Paul, SM.

“Characterization of endogenous inhibitors of [3H]-imipramine binding and [3H]-serotonin uptake from rat serum” .

Prog Clin Biol Res. 1985;192:457-64.

Angel, I. and Paul, SM.

 “Inhibition of synaptosomal 5-[3H]hydroxytryptamine uptake by endogenous factor(s) in human blood” .

FEBS Lett. 1984 Jun 11;171(2):280-4.

Angel, I., Fleissner A. and Seifert, R.

“Synaptic vesicles from hog brain: their isolation and the coupling between synthesis and uptake of gamma-aminobutyrate by glutamate decarboxylase”.

Neurochem Int 1983 5:697-712

Angel, I. and Michaelson, DM.

“Determination of Δψ, ΔpH and the proton electrochemical gradient in isolated cholinergic synaptic vesicles” .

Life Sci. 1981 Jul 27;29(4):411-6

Michaelson, DM. and Angel, I.

“Saturable acetylcholine transport into purified cholinergic synaptic vesicles”.

Proc Natl Acad Sci U S A. 1981 Apr;78(4):2048-52

Michaelson, DM., Avissar, S., Ophir, I., Pinchasi, I., Angel, I., Kloog, Y. and Sokolovsky, M.

”On the regulation of acetylcholine release: a study utilizing Torpedo synaptosomes and synaptic vesicles”.

J Physiol (Paris). 1980 Sep;76(5):505-14.

Michaelson, DM. and Angel, I.

“Determination of Δ pH in cholinergic synaptic vesicles: its effect on storage and release of acetylcholine”.

Life Sci. 1980 Jul 7;27(1):39-44

Michaelson, DM., Ophir, I.and Angel, I.

“ATP-stimulated Ca2+ transport into cholinergic Torpedo synaptic vesicles” .

J Neurochem. 1980 Jul;35(1):116-24.

Patents:

 

Angel, I., Arbilla, S., Even, L., Goldhill, J., Pichat, Ph. And Roome, N.

“Use of Mizolastine for preparing a medicine for treating inflammation”

WO 98/47511 (PCT/FR98/00765)

 

Angel, I., Arbilla, S., Even, L., Goldhill, J., Pichat, Ph. And Roome, N.

“Use of Mizolastine for treating inflammatory diseases associated with 5-lipoxygenase”

US 6140335 (371 PCT/FR98/00765)

Jegham, S., Angel, I., Purcell, T. and Schoemaker, J.

“PIPERIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY”

CA2107061 (FR92/9211551)

 

Angel, I., Martin, D. and Arbilla, S.

“Use of sulphonanilide derivatives to obtain medicine for treating retrograde ejaculation or aspermia”

WO 99/12536 (PCT/FR98/01928)

Angel, I., Martin, D. Body, Ph. and Arbilla, S.

“Use of sulphonamide benzene derivatives to obtain medicine for treating retrograde ejaculation or aspermia”

WO 99/12535 (PCT/FR98/01927)

Fraser, R., Angel, I. and Guillot, E.

“Adipose specific protein”

WO 00/26374 (PCT/FR99/08351)

Nackache, P., Angel,I., Livnah, N. And Borovitov, M.

Pyrimidine Derivatives as POSH and POSH-AP Inhibitors”

 PCT/IL2007/001356

Gilat, T. and Angel, I.

METHODS AND COMPOSITIONS FOR TREATING ALZHEIMER’S DISEASE

(WO/2010/086864)

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