Search results
- 1.0587259 - ÚOCHB 2025 RIV NL eng J - Journal Article
Bach, Kathrin - Dohnálek, Jan - Škerlová, Jana - Kumzík, Ján - Poláchová, Edita - Stanchev, Stancho - Majer, Pavel - Fanfrlík, Jindřich - Pecina, Adam - Řezáč, Jan - Lepšík, Martin - Borshchevskiy, V. - Polovinkin, V. - Stříšovský, Kvido
Extensive targeting of chemical space at the prime side of ketoamide inhibitors of rhomboid proteases by branched substituents empowers their selectivity and potency.
European Journal of Medicinal Chemistry. (2024), č. článku 116606. ISSN 0223-5234. E-ISSN 1768-3254
R&D Projects: GA ČR(CZ) GA21-24456S; GA MŠMT(CZ) LUC23180; GA MŠMT(CZ) EF16_019/0000729; GA MŠMT LX22NPO5102
Research Infrastructure: e-INFRA CZ II - 90254
Institutional support: RVO:61388963
Impact factor: 6.7, year: 2022
Method of publishing: Open access
https://doi.org/10.1016/j.ejmech.2024.116606
Permanent Link: https://hdl.handle.net/11104/0354501File Download Size Commentary Version Access 10.1016j.ejmech.2024.116606.pdf 0 6.6 MB Publisher’s postprint open-access - 2.0578510 - ÚOCHB 2024 RIV US eng J - Journal Article
Novotná, Kateřina - Tenora, Lukáš - Prchalová, E. - Paule, J. - Alt, J. - Veeravalli, V. - Lam, J. - Wu, Y. - Šnajdr, Ivan - Gori, S. - Mettu, V. S. - Tsukamoto, T. - Majer, Pavel - Slusher, B. S. - Rais, R.
Discovery of tert-Butyl Ester Based 6-Diazo-5-oxo-L-norleucine Prodrugs for Enhanced Metabolic Stability and Tumor Delivery.
Journal of Medicinal Chemistry. Roč. 66, č. 22 (2023), s. 15493-15510. ISSN 0022-2623. E-ISSN 1520-4804
R&D Projects: GA MŠMT LTAUSA18166; GA MŠMT LX22NPO5102
Institutional support: RVO:61388963
Keywords : phase-I * 6-diazo-5-oxo-l-norleucine DON * clinical pharmacology
OECD category: Organic chemistry
Impact factor: 7.3, year: 2022
Method of publishing: Open access
https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c01681
Permanent Link: https://hdl.handle.net/11104/0347498File Download Size Commentary Version Access 10.1021acs.jmedchem.3c01681.pdf 0 2.8 MB Publisher’s postprint open-access - 3.0576214 - ÚOCHB 2024 RIV US eng J - Journal Article
Lemberg, K. M. - Ali, E. S. - Krečmerová, Marcela - Aguilar, J. M. H. - Alt, J. - Peters, D. E. - Zhao, L. - Wu, Y. - Nuha, N. - Asara, J. M. - Staedtke, V. - Pratilas, C. A. - Majer, Pavel - Rais, R. - Ben-Sahra, I. - Slusher, B. S.
Pro-905, a Novel Purine Antimetabolite, Combines with Glutamine Amidotransferase Inhibition to Suppress Growth of Malignant Peripheral Nerve Sheath Tumor.
Molecular Cancer Therapeutics. Roč. 22, č. 12 (2023), s. 1390-1403. ISSN 1535-7163. E-ISSN 1538-8514
R&D Projects: GA MŠMT(CZ) LM2023053
Institutional support: RVO:61388963
Keywords : loading 6-mercaptopurine therapies * standard dose 6-mercaptopurine * combination 6-mercaptopurine
OECD category: Medicinal chemistry
Impact factor: 5.7, year: 2022
Method of publishing: Open access
https://doi.org/10.1158/1535-7163.MCT-23-0258
Permanent Link: https://hdl.handle.net/11104/0345801 - 4.0574532 - BTÚ 2024 RIV US eng J - Journal Article
Motlová, Lucia - Šnajdr, Ivan - Kutil, Zsofia - Andris, Erik - Ptáček, Jakub - Novotná, Adéla - Nováková, Zora - Havlínová, Barbora - Tueckmantel, W. - Dráberová, Helena - Majer, Pavel - Schutkowski, M. - Kozikowski, A. - Rulíšek, Lubomír - Bařinka, Cyril
Comprehensive Mechanistic View of the Hydrolysis of Oxadiazole-Based Inhibitors by Histone Deacetylase 6 (HDAC6).
ACS Chemical Biology. Roč. 18, č. 7 (2023), s. 1594-1610. ISSN 1554-8929. E-ISSN 1554-8937
R&D Projects: GA ČR(CZ) GA21-31806S; GA ČR(CZ) GA23-05940S; GA MŠMT(CZ) LUAUS23247
Research Infrastructure: CIISB III - 90242; EATRIS-CZ IV - 90253
Institutional support: RVO:86652036 ; RVO:61388963
Keywords : BASIS-SETS * COSMO * ENERGY * REFINEMENT
OECD category: Biochemistry and molecular biology
Impact factor: 4, year: 2022
Method of publishing: Open access
https://pubs.acs.org/doi/10.1021/acschembio.3c00212
Permanent Link: https://hdl.handle.net/11104/0347139 - 5.0574388 - ÚOCHB 2024 RIV US eng J - Journal Article
Peters, D. E. - Norris, L. D. - Tenora, Lukáš - Šnajdr, Ivan - Ponti, A. K. - Zhu, X. - Sakamoto, S. - Veeravalli, V. - Pradhan, M. - Alt, J. - Thomas, A. G. - Majer, Pavel - Rais, R. - McDonald, C. - Slusher, B. S.
A gut-restricted glutamate carboxypeptidase II inhibitor reduces monocytic inflammation and improves preclinical colitis.
Science Translational Medicine. Roč. 15, č. 708 (2023), č. článku eabn7491. ISSN 1946-6234. E-ISSN 1946-6242
R&D Projects: GA MŠMT(CZ) LM2018133
Institutional support: RVO:61388963
Keywords : gene expression profiles * dextran sulfate sodium * membrane antigen PSMA
OECD category: Medicinal chemistry
Impact factor: 17.1, year: 2022
Method of publishing: Limited access
https://doi.org/10.1126/scitranslmed.abn7491
Permanent Link: https://hdl.handle.net/11104/0344718 - 6.0571548 - BTÚ 2024 RIV CH eng J - Journal Article
Ptáček, Jakub - Šnajdr, Ivan - Schimer, Jiří - Kutil, Zsofia - Mikesova, Jana - Baranová, Petra - Havlínová, Barbora - Tueckmantel, W. - Majer, Pavel - Kozikowski, A. - Bařinka, Cyril
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells.
International Journal of Molecular Sciences. Roč. 24, č. 5 (2023), č. článku 4720. E-ISSN 1422-0067
R&D Projects: GA ČR(CZ) GA21-31806S; GA MŠMT LX22NPO5102
Institutional support: RVO:86652036 ; RVO:61388963
Keywords : metallohydrolase * histone deacetylase * inhibitor profiling * tubulin * histone acetylation * nanoBRET
OECD category: Biochemistry and molecular biology
Impact factor: 5.6, year: 2022
Method of publishing: Open access
https://www.mdpi.com/1422-0067/24/5/4720
Permanent Link: https://hdl.handle.net/11104/0342903 - 7.0570994 - ÚOCHB 2024 RIV NL eng J - Journal Article
Frejlachová, A. - Lencová, R. - Venhauerová, A. - Skaličková, M. - Uher, O. - Caisova, V. - Majer, Pavel - Tenora, Lukáš - Hansen, P. - Chmelař, J. - Kopecký, J. - Zhuang, Z. - Pacak, K. - Ženka, J.
The combination of immunotherapy and a glutamine metabolism inhibitor represents an effective therapeutic strategy for advanced and metastatic murine pancreatic adenocarcinoma.
International Immunopharmacology. Roč. 118, May (2023), č. článku 110150. ISSN 1567-5769. E-ISSN 1878-1705
Institutional support: RVO:61388963
Keywords : cancer * pancreatic adenocarcinoma * intratumoral * immunotherapy * glutamine antagonist
OECD category: Medicinal chemistry
Impact factor: 5.6, year: 2022
Method of publishing: Limited access
https://doi.org/10.1016/j.intimp.2023.110150
Permanent Link: https://hdl.handle.net/11104/0342323 - 8.0568134 - ÚOCHB 2024 RIV GB eng J - Journal Article
Tsai, J. - Gori, S. - Alt, J. - Tiwari, S. - Iyer, J. - Talwar, R. - Hinsu, D. - Ahirwar, K. - Mohanty, S. - Khunt, C. - Sutariya, B. - Jani, K. - Venkatasubbaiah, V. - Patel, A. - Meghapara, J. - Joshi, K. - Sahu, R. - Rana, V. - Nigade, P. - Talluri, R. S. - Murty, K. V. S. N. - Joshi, K. - Ramanathan, V. - Li, A. - Islam, N. - Šnajdr, Ivan - Majer, Pavel - Rais, R. - Slusher, B. S. - Garza, L. A.
Topical SCD-153, a 4-methyl itaconate prodrug, for the treatment of alopecia areata.
PNAS Nexus. Roč. 2, č. 1 (2023), č. článku pgac297. E-ISSN 2752-6542
Institutional support: RVO:61388963
Keywords : alopecia areata * hair growth * topical * itaconate * prodrug * inflammation * immunosuppression * cytokine * interleukin * interferon * double-stranded RNA * polyinosinic–polycytidylic acid * hair cycle * anagen * telogen * keratinocyte * stability * pharmacokinetics * cytotoxicity
OECD category: Medicinal chemistry
Impact factor: 2.2, year: 2023
Method of publishing: Open access
https://doi.org/10.1093/pnasnexus/pgac297
Permanent Link: https://hdl.handle.net/11104/0339488
Research data: Mendeley Data - 9.0566618 - ÚOCHB 2024 RIV US eng J - Journal Article
Poláchová, Edita - Bach, Kathrin - Heuten, E. - Stanchev, Stancho - Tichá, Anežka - Lampe, P. - Majer, Pavel - Langer, T. - Lemberg, M. K. - Stříšovský, Kvido
Chemical Blockage of the Mitochondrial Rhomboid Protease PARL by Novel Ketoamide Inhibitors Reveals Its Role in PINK1/Parkin-Dependent Mitophagy.
Journal of Medicinal Chemistry. Roč. 66, č. 1 (2023), s. 251-265. ISSN 0022-2623. E-ISSN 1520-4804
R&D Projects: GA MŠMT LO1302; GA MŠMT(CZ) EF16_019/0000729
Institutional support: RVO:61388963
Keywords : lipid bilayer nanodiscs * membrane proteins * PINK1
OECD category: Biochemistry and molecular biology
Impact factor: 7.3, year: 2022
Method of publishing: Open access
https://doi.org/10.1021/acs.jmedchem.2c01092
Permanent Link: https://hdl.handle.net/11104/0338165 - 10.0565749 - ÚOCHB 2024 RIV GB eng J - Journal Article
Kugler, Michael - Hadzima, Martin - Dzijak, Rastislav - Rampmaier, Robert - Srb, Pavel - Vrzal, Lukáš - Voburka, Zdeněk - Majer, Pavel - Řezáčová, Pavlína - Vrábel, Milan
Identification of specific carbonic anhydrase inhibitors via in situ click chemistry, phage-display and synthetic peptide libraries: comparison of the methods and structural study.
RSC MEDICINAL CHEMISTRY. Roč. 14, č. 1 (2023), s. 144-153. E-ISSN 2632-8682
R&D Projects: GA MŠMT(CZ) EF16_019/0000729
EU Projects: European Commission(XE) 677465 - SWEETOOLS
Institutional support: RVO:61388963
Keywords : fragment-based discovery * combinatorial libraries * generation
OECD category: Biochemical research methods
Impact factor: 4.1, year: 2022
Method of publishing: Limited access
https://doi.org/10.1039/D2MD00330A
Permanent Link: https://hdl.handle.net/11104/0337258File Download Size Commentary Version Access 10.1039D2MD00330A.pdf 0 6.5 MB Publisher’s postprint require
Research data: Worldwide PBD, Worldwide PBD, Worldwide PBD, Worldwide PBD, Worldwide PBD, Worldwide PBD