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Cancer Research, ISSN 0008-5472, 10/2017, Volume 77, Issue 20, pp. 5564 - 5575
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 11/2018, Volume 9, Issue 11, pp. 1088 - 1093
A series of structurally diverse azaspirodecanone and spirooxazolidinone analogues were designed and synthesized as potent and selective somatostatin receptor... 
Glucose-dependent insulin secretion (GDIS) | Metabolic stability | Somatostatin | Type 2 diabetes mellitus (T2DM) | SSTR5 antagonists | POTENT | CHEMISTRY, MEDICINAL | GLP-1 | SSTRS antagonists | 5 SSTR5 ANTAGONISTS | DISCOVERY
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2016, Volume 59, Issue 4, pp. 1271 - 1298
Bromodomains, small protein modules that recognize acetylated lysine on histones, play a significant role in the epigenome, where they function as "readers"... 
CHEMISTRY, MEDICINAL | SWI/SNF COMPLEXES | SMALL-MOLECULE INHIBITORS | PROSTATE-CANCER | SELECTIVE INHIBITORS | GENE-EXPRESSION | CHEMICAL PROBE | TUMOR-SUPPRESSOR | BET INHIBITORS | HISTONE ACETYLTRANSFERASE | PHD FINGER | Small Molecule Libraries - pharmacology | Antigens, Nuclear - metabolism | Humans | Drug Discovery - methods | CREB-Binding Protein - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - antagonists & inhibitors | DNA-Binding Proteins - metabolism | CREB-Binding Protein - metabolism | Protein Processing, Post-Translational - drug effects | Adaptor Proteins, Signal Transducing - antagonists & inhibitors | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Lysine - metabolism | Protein-Serine-Threonine Kinases - metabolism | RNA-Binding Proteins - antagonists & inhibitors | Nerve Tissue Proteins - antagonists & inhibitors | ATPases Associated with Diverse Cellular Activities | DNA-Binding Proteins - antagonists & inhibitors | Chromosomal Proteins, Non-Histone - metabolism | Carrier Proteins - antagonists & inhibitors | Adenosine Triphosphatases - metabolism | Models, Molecular | Nuclear Proteins - metabolism | Transcription Factors - antagonists & inhibitors | Nerve Tissue Proteins - metabolism | Transcription Factors - metabolism | Adenosine Triphosphatases - antagonists & inhibitors | DNA Helicases - metabolism | Small Molecule Libraries - chemistry | Acetylation - drug effects | Animals | Carrier Proteins - metabolism | Nuclear Proteins - antagonists & inhibitors | DNA Helicases - antagonists & inhibitors | Histones - metabolism | Adaptor Proteins, Signal Transducing - metabolism | RNA-Binding Proteins - metabolism
Journal Article
Cell Reports, ISSN 2211-1247, 08/2018, Volume 24, Issue 7, pp. 1722 - 1729
Acetylation of histone H3 at lysine 27 is a well-defined marker of enhancer activity. However, the functional impact of this modification at enhancers is... 
CBP | bromodomain | enhancer | P300 | histone acetylation | H3K27Ac | PROTEIN | INHIBITOR | TRANSCRIPTION | CELL BIOLOGY
Journal Article
by Sullivan, Patrick and Yuan, Maoli and Coleman, John and Destefano, Joanne and Zhang, Xinsheng and Yates, Nicole and Barouch, Dan and Ackerman, Margaret and Decamp, Allan and Alter, Galit and Tomaras, Georgia and Tomaras, Georgia and Montefiori, David and Montefiori, David and Rasmussen, Beth and Morrow, Gavin and Koff, Wayne and Kashuba, Angela and Kashuba, Angela and Mascola, John and Picker, Louis and Kent, Stephen and Selhorst, Philippe and Masson, Lindi and Ngandu, Nobubelo and Rademeyer, Cecilia and Karim, Quarraisha Abdool and Kijak, Gustavo and Barouch, Dan and Rasheed, Ata Ur and Havenar-Daughton, Colin and Pham, Matthew and Kovalenkov, Yevgeniy and Gumber, Sanjeev and Johnson, Matthew and Wrammert, Jens and Villinger, Francois and Haynes, Barton and Haynes, Barton and Fox, Christopher and Reed, Steve and Vasilakos, John and Tomai, Mark and Crotty, Shane and Ahmed, Rafi and Pulendran, Bali and Fukazawa, Yoshinori and Lifson, Jeffrey and Lifson, Jeffrey and Moore, Penny and Chatora, Kumbirai and Skorochod, Elisabeth and Madidi, Ngonidzashe and Gomez, Anabel and Ncube, Getrude and Sundaram, Maaya and Kretschmer, Steve and Pauthner, Matthias and Briney, Bryan and Lee, Jeong Hyun and Saye-Francisco, Karen and Hsueh, Jessica and Ramos, Alejandra and Le, Khoa and Jones, Meaghan and Jardine, Joseph and Bastidas, Raiza and Sarkar, Anita and Liang, Chi-Hui and Wilson, Ian and Ward, Andrew and Zhu, Jiang and Poignard, Pascal and Burton, Dennis and Krebs, Shelly and Law, Wiliam and Gift, Syna and Chenine, Agnes and Rolland, Morgane and Moody, M. Anthony and Jarosinski, Marissa and Georgiev, Ivelin and Chuang, Gwo-Yu and Chuang, Gwo-Yu and Asokan, Mangaiarkarasi and Bailer, Robert T and Cale, Evan M and Louder, Mark and Kwong, Peter D and Polonis, Victoria and Tovanabutra, Sodsai and Robb, Merlin and Mascola, John R and Wibmer, Constantinos Kurt and Wibmer, Constantinos Kurt and Madzorera, Vimbai S and Doria-Rose, Nicole A and Morris, Lynn and Moore, Penny L and Anthony, Colin and ...
AIDS Research and Human Retroviruses, ISSN 0889-2229, 10/2016, Volume 32, Issue S1, pp. 1 - 409
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 12/2016, Volume 59, Issue 23, pp. 10549 - 10563
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2016, Volume 59, Issue 11, pp. 5391 - 5402
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 06/2016, Volume 291, Issue 25, pp. 13014 - 13027
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2017, Volume 60, Issue 22, pp. 9162 - 9183
Journal Article
Cell Reports, ISSN 2211-1247, 04/2019, Volume 27, Issue 1, pp. 269 - 281.e4
Myeloid-derived suppressor cells (MDSCs) are found in most cancer malignancies and support tumorigenesis by suppressing immunity and promoting tumor growth.... 
CBP | bromodomain | EP300 | tumors | myeloid-derived suppressive cells | H3K27ac | INHIBITION | P300 | EXPANSION | CBP/P300 BROMODOMAIN | SUBSETS | MECHANISMS | SUPPRESSOR-CELLS | CANCER | EXPRESSION | CELL BIOLOGY
Journal Article
Cancer research, ISSN 0008-5472, 08/2019, Volume 79, Issue 15, pp. 3916 - 3927
Regulatory T cells (Treg) are immunosuppressive and negatively impact response to cancer immunotherapies. CREB-binding protein (CBP) and p300 are closely... 
B-CELLS | CBP | HIGH NUMBERS | DENDRITIC CELLS | ONCOLOGY | ACETYLATION | P300 | MUTATIONS | EXPRESSION | IL-10 | BROMODOMAIN INHIBITOR
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2018, Volume 28, Issue 1, pp. 15 - 23
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 06/2019, Volume 29, Issue 12, pp. 1522 - 1531
Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13... 
Janus Kinase | JAK | Atopic dermatitis | Structure-based design | Interleukin-13 | IL-13 | JAK2 | JAK1 | Asthma | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | IDENTIFICATION | Viral antibodies | Antibodies | Mutual fund industry | Interleukins
Journal Article