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Showing 1 to 12 of 19 entries
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Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene.

Letters in drug design & discovery

Gramling S, Reisman D.
PMID: 23565070
Lett Drug Des Discov. 2011 Jan 01;8(1):93-99. doi: 10.2174/157018011793663840.

Drug discovery in the field of oncology has been advanced mainly through the targeting of receptor tyrosine kinases. Both antibodies and small molecule inhibitors have been found to have successful applications in blocking the proliferative functions of these cell...

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Gramling S, Reisman D. Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene. Lett Drug Des Discov. 2011;8(1):93-99doi: 10.2174/157018011793663840.
Gramling, S., & Reisman, D. (2011). Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene. Letters in drug design & discovery, 8(1), 93-99. https://doi.org/10.2174/157018011793663840
Gramling, Sarah, and Reisman, David. "Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene." Letters in drug design & discovery vol. 8,1 (2011): 93-99. doi: https://doi.org/10.2174/157018011793663840
Gramling S, Reisman D. Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene. Lett Drug Des Discov. 2011 Jan 01;8(1):93-99. doi: 10.2174/157018011793663840. PMID: 23565070; PMCID: PMC3615482.
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A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents.

Letters in drug design & discovery

Winfield LL, Smith DM, Halemano K, Leggett CS.
PMID: 25568641
Lett Drug Des Discov. 2008;5(6):369-376. doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf.

PDK1 is pivotal in the development and progression of several cancers. A 3D pharmacophore was developed for pyrazole derivatives displaying anti-proliferative activity and PDK1 inhibition. The pharmacophore was utilized in the design of benzimidazole analogs. Our preliminary results indicate...

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Winfield LL, Smith DM, Halemano K, et al. A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Lett Drug Des Discov. 2008;5(6):369-376doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf.
Winfield, L. L., Smith, D. M., Halemano, K., & Leggett, C. S. (2008). A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Letters in drug design & discovery, 5(6), 369-376. https://doi.org/10.2174/157018008785777324#sthash.5mpkAcrR.dpuf
Winfield, Leyte L, et al. "A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents." Letters in drug design & discovery vol. 5,6 (2008): 369-376. doi: https://doi.org/10.2174/157018008785777324#sthash.5mpkAcrR.dpuf
Winfield LL, Smith DM, Halemano K, Leggett CS. A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents. Lett Drug Des Discov. 2008;5(6):369-376. doi: 10.2174/157018008785777324#sthash.5mpkAcrR.dpuf. PMID: 25568641; PMCID: PMC4283767.
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Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs.

Letters in drug design & discovery

Ganguly S, Murugesan S, Prasanthi N, Alptürk O, Herman B, Sluis-Cremer N.
PMID: 20535242
Lett Drug Des Discov. 2010 Jun 01;7(5):318-323. doi: 10.2174/157018010791163424.

There is still an urgent need to develop nonnucleoside reverse transcriptase (RT) inhibitors (NNRTI) with a high-genetic barrier to resistance that facilitate patient adherence and allow durable suppression of HIV-1 replication. In this study, we describe the synthesis of...

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Ganguly S, Murugesan S, Prasanthi N, et al. Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs. Lett Drug Des Discov. 2010;7(5):318-323doi: 10.2174/157018010791163424.
Ganguly, S., Murugesan, S., Prasanthi, N., Alptürk, O., Herman, B., & Sluis-Cremer, N. (2010). Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs. Letters in drug design & discovery, 7(5), 318-323. https://doi.org/10.2174/157018010791163424
Ganguly, Swastika, et al. "Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs." Letters in drug design & discovery vol. 7,5 (2010): 318-323. doi: https://doi.org/10.2174/157018010791163424
Ganguly S, Murugesan S, Prasanthi N, Alptürk O, Herman B, Sluis-Cremer N. Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs. Lett Drug Des Discov. 2010 Jun 01;7(5):318-323. doi: 10.2174/157018010791163424. PMID: 20535242; PMCID: PMC2882308.
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Anti-Amyloid Effects of Small Molecule Aβ-Binding Agents in PS1/APP Mice.

Letters in drug design & discovery

Cohen AD, Ikonomovic MD, Abrahamson EE, Paljug WR, Dekosky ST, Lefterov IM, Koldamova RP, Shao L, Debnath ML, Mason NS, Mathis CA, Klunk WE.
PMID: 20119496
Lett Drug Des Discov. 2009 Sep;6(6):437. doi: 10.2174/157018009789057526.

AIMS: One promising approach for treatment of Alzheimer's disease (AD) is use of anti-amyloid therapies, based on the hypothesis that increases in amyloid-beta (Aβ) deposits in brain are a major cause of AD. Several groups have focused on Aβ...

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Cohen AD, Ikonomovic MD, Abrahamson EE, et al. Anti-Amyloid Effects of Small Molecule Aβ-Binding Agents in PS1/APP Mice. Lett Drug Des Discov. 2009;6(6):437doi: 10.2174/157018009789057526.
Cohen, A. D., Ikonomovic, M. D., Abrahamson, E. E., Paljug, W. R., Dekosky, S. T., Lefterov, I. M., Koldamova, R. P., Shao, L., Debnath, M. L., Mason, N. S., Mathis, C. A., & Klunk, W. E. (2009). Anti-Amyloid Effects of Small Molecule Aβ-Binding Agents in PS1/APP Mice. Letters in drug design & discovery, 6(6), 437. https://doi.org/10.2174/157018009789057526
Cohen, A D, et al. "Anti-Amyloid Effects of Small Molecule Aβ-Binding Agents in PS1/APP Mice." Letters in drug design & discovery vol. 6,6 (2009): 437. doi: https://doi.org/10.2174/157018009789057526
Cohen AD, Ikonomovic MD, Abrahamson EE, Paljug WR, Dekosky ST, Lefterov IM, Koldamova RP, Shao L, Debnath ML, Mason NS, Mathis CA, Klunk WE. Anti-Amyloid Effects of Small Molecule Aβ-Binding Agents in PS1/APP Mice. Lett Drug Des Discov. 2009 Sep;6(6):437. doi: 10.2174/157018009789057526. PMID: 20119496; PMCID: PMC2812908.
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Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility.

Letters in drug design & discovery

Botelho MC, Alves H, Richter J.
PMID: 28018158
Lett Drug Des Discov. 2017;14(2):135-138. doi: 10.2174/1570180813666160720165057.

Urogenital schistosomiasis is a chronic infection caused by the human blood fluke Schistosoma haematobium. Schistosomiasis haematobium is a known risk factor for cancer leading to squamous cell carcinoma of the urinary bladder (SCC). This is a neglected tropical disease...

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Botelho MC, Alves H, Richter J. Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility. Lett Drug Des Discov. 2017;14(2):135-138doi: 10.2174/1570180813666160720165057.
Botelho, M. C., Alves, H., & Richter, J. (2017). Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility. Letters in drug design & discovery, 14(2), 135-138. https://doi.org/10.2174/1570180813666160720165057
Botelho, M C, et al. "Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility." Letters in drug design & discovery vol. 14,2 (2017): 135-138. doi: https://doi.org/10.2174/1570180813666160720165057
Botelho MC, Alves H, Richter J. Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility. Lett Drug Des Discov. 2017;14(2):135-138. doi: 10.2174/1570180813666160720165057. PMID: 28018158; PMCID: PMC5179139.
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Synthesis and antiproliferative activity of coumarin-estrogen conjugates against breast cancer cell lines.

Letters in drug design & discovery

Musa MA, Khan MO, Cooperwood JS.
PMID: 20556210
Lett Drug Des Discov. 2009 Mar;6(2):133-138. doi: 10.2174/157018009787582624.

The syntheses and cytotoxic activity of coumarin-estrogen conjugates are described. In vitro results indicated that conjugates 10, 11 and 13 show growth inhibitory activities at 5-dose concentration (100, 10, 1, 0.1, 0.01 muM) against the following NCI-7- human breast...

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Musa MA, Khan MO, Cooperwood JS. Synthesis and antiproliferative activity of coumarin-estrogen conjugates against breast cancer cell lines. Lett Drug Des Discov. 2009;6(2):133-138doi: 10.2174/157018009787582624.
Musa, M. A., Khan, M. O., & Cooperwood, J. S. (2009). Synthesis and antiproliferative activity of coumarin-estrogen conjugates against breast cancer cell lines. Letters in drug design & discovery, 6(2), 133-138. https://doi.org/10.2174/157018009787582624
Musa, Musiliyu A, et al. "Synthesis and antiproliferative activity of coumarin-estrogen conjugates against breast cancer cell lines." Letters in drug design & discovery vol. 6,2 (2009): 133-138. doi: https://doi.org/10.2174/157018009787582624
Musa MA, Khan MO, Cooperwood JS. Synthesis and antiproliferative activity of coumarin-estrogen conjugates against breast cancer cell lines. Lett Drug Des Discov. 2009 Mar;6(2):133-138. doi: 10.2174/157018009787582624. PMID: 20556210; PMCID: PMC2885731.
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Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents.

Letters in drug design & discovery

Cooperwood JS, Edwards J, Musa M, Simmons D, Mian AD, Park KK, Wan Z.
PMID: 20543998
Lett Drug Des Discov. 2010 Jul 01;7(6):389-394. doi: 10.2174/157018010791306551.

3-N-alkyloxyestradiol derivatives were synthesized, characterized and tested for activity in MCF-7 human breast cancer cells. Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon...

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Cooperwood JS, Edwards J, Musa M, et al. Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents. Lett Drug Des Discov. 2010;7(6):389-394doi: 10.2174/157018010791306551.
Cooperwood, J. S., Edwards, J., Musa, M., Simmons, D., Mian, A. D., Park, K. K., & Wan, Z. (2010). Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents. Letters in drug design & discovery, 7(6), 389-394. https://doi.org/10.2174/157018010791306551
Cooperwood, John S, et al. "Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents." Letters in drug design & discovery vol. 7,6 (2010): 389-394. doi: https://doi.org/10.2174/157018010791306551
Cooperwood JS, Edwards J, Musa M, Simmons D, Mian AD, Park KK, Wan Z. Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents. Lett Drug Des Discov. 2010 Jul 01;7(6):389-394. doi: 10.2174/157018010791306551. PMID: 20543998; PMCID: PMC2882686.
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Homology Modelling of Human E1 Ubiquitin Activating Enzyme.

Letters in drug design & discovery

Brahemi G, Burger AM, Westwell AD, Brancale A.
PMID: 20396627
Lett Drug Des Discov. 2010 Jan 01;7(1):57-62. doi: 10.2174/157018010789869316.

Human E1 is a key player in protein ubiquitination, however the E1 structure is not available. In this paper, we describe the derivation of a human E1 structure using molecular modelling based on the crystal structure of S. cerevisiae...

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Brahemi G, Burger AM, Westwell AD, et al. Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Lett Drug Des Discov. 2010;7(1):57-62doi: 10.2174/157018010789869316.
Brahemi, G., Burger, A. M., Westwell, A. D., & Brancale, A. (2010). Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Letters in drug design & discovery, 7(1), 57-62. https://doi.org/10.2174/157018010789869316
Brahemi, Ghali, et al. "Homology Modelling of Human E1 Ubiquitin Activating Enzyme." Letters in drug design & discovery vol. 7,1 (2010): 57-62. doi: https://doi.org/10.2174/157018010789869316
Brahemi G, Burger AM, Westwell AD, Brancale A. Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Lett Drug Des Discov. 2010 Jan 01;7(1):57-62. doi: 10.2174/157018010789869316. PMID: 20396627; PMCID: PMC2853970.
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Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: .

Letters in drug design & discovery

Yar M, Bajda M, Mehmood RA, Sidra LR, Ullah N, Shahzadi L, Ashraf M, Ismail T, Shahzad SA, Khan ZA, Naqvi SA, Mahmood N.
PMID: 24719609
Lett Drug Des Discov. 2014 Mar;11(3):331-338. doi: 10.2174/15701808113106660078.

Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer's disease....

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Yar M, Bajda M, Mehmood RA, et al. Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: . Lett Drug Des Discov. 2014;11(3):331-338doi: 10.2174/15701808113106660078.
Yar, M., Bajda, M., Mehmood, R. A., Sidra, L. R., Ullah, N., Shahzadi, L., Ashraf, M., Ismail, T., Shahzad, S. A., Khan, Z. A., Naqvi, S. A., & Mahmood, N. (2014). Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: . Letters in drug design & discovery, 11(3), 331-338. https://doi.org/10.2174/15701808113106660078
Yar, Muhammad, et al. "Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: ." Letters in drug design & discovery vol. 11,3 (2014): 331-338. doi: https://doi.org/10.2174/15701808113106660078
Yar M, Bajda M, Mehmood RA, Sidra LR, Ullah N, Shahzadi L, Ashraf M, Ismail T, Shahzad SA, Khan ZA, Naqvi SA, Mahmood N. Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: . Lett Drug Des Discov. 2014 Mar;11(3):331-338. doi: 10.2174/15701808113106660078. PMID: 24719609; PMCID: PMC3977535.
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L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis.

Letters in drug design & discovery

Tashiro K, Kaida Y, Yamagishi SI, Tanaka H, Yokoro M, Yano J, Sakai K, Kurokawa Y, Taguchi K, Nakayama Y, Inokuchi T, Fukami K.
PMID: 28670223
Lett Drug Des Discov. 2017 Jun;14(6):737-742. doi: 10.2174/1570180814666170216102632.

BACKGROUND: Depression is highly prevalent in uremic patients undergoing hemodialysis (HD). We previously found that low free-carnitine levels are associated with depression severity in male patients undergoing HD. However, whether L-carnitine supplementation improves the depression state in male patients...

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Tashiro K, Kaida Y, Yamagishi SI, et al. L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis. Lett Drug Des Discov. 2017;14(6):737-742doi: 10.2174/1570180814666170216102632.
Tashiro, K., Kaida, Y., Yamagishi, S. I., Tanaka, H., Yokoro, M., Yano, J., Sakai, K., Kurokawa, Y., Taguchi, K., Nakayama, Y., Inokuchi, T., & Fukami, K. (2017). L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis. Letters in drug design & discovery, 14(6), 737-742. https://doi.org/10.2174/1570180814666170216102632
Tashiro, Kyoko, et al. "L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis." Letters in drug design & discovery vol. 14,6 (2017): 737-742. doi: https://doi.org/10.2174/1570180814666170216102632
Tashiro K, Kaida Y, Yamagishi SI, Tanaka H, Yokoro M, Yano J, Sakai K, Kurokawa Y, Taguchi K, Nakayama Y, Inokuchi T, Fukami K. L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis. Lett Drug Des Discov. 2017 Jun;14(6):737-742. doi: 10.2174/1570180814666170216102632. PMID: 28670223; PMCID: PMC5470074.
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Challenges in the Discovery and Optimization of mGlu.

Letters in drug design & discovery

Fulton MG, Loch MT, Cuoco CA, Rodriguez AL, Days E, Vinson PN, Kozek KA, Weaver CD, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.
PMID: 32201485
Lett Drug Des Discov. 2019 Dec;16(12):1387-1394. doi: 10.2174/1570180815666181017131349.

BACKGROUND: This article describes the challenges in the discovery and optimization of mGlu2/4 heterodimer Positive Allosteric Modulators (PAMs).METHODS: Initial forays based on VU0155041, a PAM of both the mGlu4 homodimer and the mGlu2/4 heterodimer, led to flat, intractable SAR...

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Fulton MG, Loch MT, Cuoco CA, et al. Challenges in the Discovery and Optimization of mGlu. Lett Drug Des Discov. 2019;16(12):1387-1394doi: 10.2174/1570180815666181017131349.
Fulton, M. G., Loch, M. T., Cuoco, C. A., Rodriguez, A. L., Days, E., Vinson, P. N., Kozek, K. A., Weaver, C. D., Blobaum, A. L., Conn, P. J., Niswender, C. M., & Lindsley, C. W. (2019). Challenges in the Discovery and Optimization of mGlu. Letters in drug design & discovery, 16(12), 1387-1394. https://doi.org/10.2174/1570180815666181017131349
Fulton, Mark Gallant, et al. "Challenges in the Discovery and Optimization of mGlu." Letters in drug design & discovery vol. 16,12 (2019): 1387-1394. doi: https://doi.org/10.2174/1570180815666181017131349
Fulton MG, Loch MT, Cuoco CA, Rodriguez AL, Days E, Vinson PN, Kozek KA, Weaver CD, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Challenges in the Discovery and Optimization of mGlu. Lett Drug Des Discov. 2019 Dec;16(12):1387-1394. doi: 10.2174/1570180815666181017131349. PMID: 32201485; PMCID: PMC7059629.
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In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models.

Letters in drug design & discovery

Eyunni SK, Gangapuram M, Redda KK.
PMID: 25506297
Lett Drug Des Discov. 2014;11(4):428-436. doi: 10.2174/1570180811666131203002502.

The antiproliferative activities of new substituted tetrahydroisoquinolines (THIQs) are described. Their cytotoxicities against Ishikawa human endometrial cell line were determined after 72 h drug expose employing Celtiter-Glo assay at concentrations ranging from 0.01 to 100,000 nM. The antiproliferative activities...

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Eyunni SK, Gangapuram M, Redda KK. In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models. Lett Drug Des Discov. 2014;11(4):428-436doi: 10.2174/1570180811666131203002502.
Eyunni, S. K., Gangapuram, M., & Redda, K. K. (2014). In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models. Letters in drug design & discovery, 11(4), 428-436. https://doi.org/10.2174/1570180811666131203002502
Eyunni, Suresh Kumar V K, et al. "In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models." Letters in drug design & discovery vol. 11,4 (2014): 428-436. doi: https://doi.org/10.2174/1570180811666131203002502
Eyunni SK, Gangapuram M, Redda KK. In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models. Lett Drug Des Discov. 2014;11(4):428-436. doi: 10.2174/1570180811666131203002502. PMID: 25506297; PMCID: PMC4264606.
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Showing 1 to 12 of 19 entries